Systemic Pharmacology

Systemic Pharmacology
For Aid in Complete Preparation of
Residency/FCPS P-I/MPhil/Diploma

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Published by
Synapse Medical Academy

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Systemic Pharmacology

Published By
Synapse Medical Academy

Edited By
Synapse Publication Team

ISBN No
978-984-34-4631-2

4th Edition, 2024

July 2021
For Contact
Synapse Medical Academy
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77 Bir Uttam C.R Dutta Road, Hatirpool, Dhaka.
Phone: 01978303381, 01968206771

Copyright Ⓒ 2024. All rights reserved by the publisher. No part of this book may
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prior permission from author.

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Residency diploma

Contents

Sl. No. Topic List Page No.

CNS Pharmacology
1 Anti-Psychotics & 05
2 Mood Stabilizers 09
3 Anti-depressants &* 09
4 Sedative & hypnotics Diazepam 3 * 11
5 Anti-Perkinson Drugs 3 (Name only) 13
6 Anti-convulsants 3 * 13
7 Migraine pharmacology 3 * 15
Analgesic & Anesthetics
8 Anesthetics 15
9 Analgesics 19
10 Opioid Analgesic 20
11 NSAIDs 25
Anti-Microbials
12 Anti-Bacterial Drugs 28
13 Anti-tubercular drugs 37
14 Classification of antiviral drugs 38
15 Anti-fungal Drugs 39
16 Anti- Protozoal drugs 40
Cardio Pharmacology
17 Anti Anginal drugs (GTN Beta blocker) & *
,
43
18 Drugs Used in Heart Failure Digoxin X 45
19 Anti arrhythmic drugs 4 * 50
20 Antihypertensive agents (ACEI ARB)4*, CCB
, 3 51
21 Lipid lowering agents L* 56
Blood Pharmacology
22 Anti-platelet drugs 4 * 57
23 Anti-co-agulants 59
24 Hematinics 64
Renal Pharmacology
25 Diuretics L 65
26 Nephrotoxic Drugs 3 67
Respiratory Pharmacology
27 Anti-Asthmatic Drugs 68
28 Drugs causing Bronchoconstiction 70
GIT Pharmacology
29 Drugs used in peptic ulcer 70
30 Anti-Emitic Drugs 72
Autacoids
31 Prostaglandin 73

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Contents

Sl. No. Topic List Page No.

CNS Pharmacology
1 Anti-Psychotics 05
2 Mood Stabilizers 09
3 Anti-depressants 09
4 Sedative & hypnotics 2 # 11
5 Anti-Perkinson Drugs 13
6 Anti-convulsants * 13
7 Migraine pharmacology① Analgesic & Anesthetics
15

8 Anesthetics 3 * 15
9 Analgesics 19
10 Opioid Analgesic 3 * 20
11 NSAIDs 25
Anti-Microbials 2
12 Anti-Bacterial Drugs 28
13 Anti-tubercular drugs 37
14 Classification of antiviral drugs 38
15 Anti-fungal Drugs 39
16 Anti- Protozoal drugs 40
Cardio Pharmacology
17 Anti Anginal drugs * 43
18 Drugs Used in Heart Failure 45
19 Anti arrhythmic drugs 50
20 Antihypertensive agents * 51
21 Lipid lowering agents 56
Blood Pharmacology
22 Anti-platelet drugs 57
23 Anti-co-agulants
3 59
24 Hematinics 64
Renal Pharmacology
25 Diuretics 3 65
26 Nephrotoxic Drugs 67
Respiratory Pharmacology
27 Anti-Asthmatic Drugs 2* 68
28 Drugs causing Bronchoconstiction 70
GIT Pharmacology
29 Drugs used in peptic ulcer 2* 70
30 Anti-Emitic Drugs 72
Autacoids
31 Prostaglandin 73

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Sl. No. Topic List Page No.

32 Anti-Histamine * 73
Endocrine Pharmacology
33
34
Steroids
*
Drugs used in DM
75
78
35 Anti-thyroid drugs * 82
36 Classification oral pills 83
37 Ovulation inducing agent 3*- only for gyne 85
Others
38 Pharmacology Related to COVID 19 86
39 Causology 90
40 Adverse Effect 93
41 Summary Box 95
42. Exam Night Topic 102
43. Bibliography 104
44. Previous Questions 105

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Systemic Pharmacology
CNS Pharmacology
01. Anti-Psycotic Drugs
Dopamine hypothesis: Excessive dopaminergic activity in brain is responsible for
Psychosis or schizophrenia.
Anti- psychotic includes:
Anti-psychotic drugs/ drugs for schizophrenia/ D2 receptor antagonist in CNS:

A. Traditional or typical neuroleptic drugs (also called conventional or first -generation

antipsychotics) are competitive inhibitors at a variety of receptors, but their antipsychotic effects
reflect competitive blocking of dopamine receptors.
According to chemical nature
1. Phenothiazine derivatives • Chlorpromazine
• Prochlorperazine
• Thioridazine
• Perphenazine
• Trifluoperazine
• Fluphenazine
• Promethazine
[Link] derivatives • Thiothixene
• Flupentixol
[Link] derivatives • Haloperidol
[Link] structure • Pimozide
• Molindone
• Sulpiride

B. Atypical (or second-generation antipsychotics):

Atypical (or second-generation antipsychotics): [Link]
The newer antipsychotic drugs are referred to as atypical [Link]
(or second-generation antipsychotics), because they have [Link]
fewer extrapyramidal adverse effects than the older 4. Olanzapine
traditional agents. 5. Quetiapine
These drugs appear to owe their unique activity to 6. Paliperidone
blockade of both serotonin and dopamine (and perhaps, 7. Risperidone
other) receptors. [Link]
The atypical antipsychotic drugs are now the most widely 9. Ziprasidone
used type of antipsychotic drug 10. Zotepine
[Link]

Benefit of Using 2nd Line Antipsychotics:

 Weak D2 Blocking Property
 Potent 5 HT2 Antagonist

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 They May improve impaired cognitive function

 EPS Are Minimal
 H1 Blockade Activity is Minimal
Pharmacological effects of anti-psychotics/Chlorpromazine:
• Effects of dopaminergic receptor blocking: There are 5 important dopaminergic
pathways recognized in the brain

·
Dopaminergic pathways in the Effects on blocking the pathway
brain
Mesolimbic-mesocortical pathway: Antipsychotic action
Closely related to behavior No hallucination
No delusion
No aggressive behavior
Calmness
Tranquility
Normal sleep pattern.
Nigrostriatal pathway: Involved in Extra-pyramidal syndromes (EPS):
the coordination of voluntary Parkinson's syndrome
movements.: Akathisia
Acute dystonic reactions
Tardive dyskinesia
Seizure
3. Tuberoinfundibular pathway: Increased prolactin secretion, which causes in
Inhibits prolactin secretions. Women:
Dopamine - Prolactin inhibitor Amenorrhea
Galactorrhea.
False +ve pregnancy tests.
Increased libido.
Men:
Gynecomastia.
Decreased libido.
4. Medullary-periventricular Weight gain (due to altered eating behavior).
pathway: May
be involved in eating behavior,
5. Incertohypothalamic pathway: - It appears to regulate the anticipatory motivational phase of
Regulates copulatory behavior in rats. copulatory behavior in rats.
Effects of other receptors blocking property:
Types of blocking Effects of blocking
1. Muscarnic receptor • Tachycardia
• Urine retention
• Constipation
• Dry mouth & skin
• Dry mouth
2. α-adrenergic blocking • Postural hypotension
• Reflex tachycardia
• Cardiac arrhythmias
• Ejaculatory failure.
3. Histaminergic blocking • Sedation
• Anti-allergic action.
• Anti-emetic effect

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[Link] gated Na+ Channel • Anti-epileptic effects

blocking • Local anesthetics
• Arrhythmia
5. Peripheral conversion of Women
androgen to estrogen • Amenorrhea
• Galactorrhea
• False +ve pregnancy tests
• Increase libido.
Men
• Gynecomastia
• Decreased libido
[Link] (5-HT2) receptor • Antipsychotic action
blocking

Adverse effects of antipsychotics/ chlorpromazine/ haloperidol:

Type Adverse effects Mechanisms

ANS • Tachycardia Muscarinic receptor blockade
• Urine retention
• Constipation
• Dry mouth & skin
• Blurred vision
• Postural hypotension α-adrenergic blocking
• Reflex tachycardia
• Cardiac arrhythmias
• Ejaculatory failure
CNS Extra-pyramidal symptoms Dopamine receptor blocking
• Parkinson’s syndrome
• Akathisia
• Acute dystonic reactions
• Tardive dyskinesia
• Seizures
• Toxic confusional state Muscarinic receptor blockade
• Sedation H1 receptor blockade
• Weight gain Both H1 & 5-HT2 blockade
Endocrine Women: Hyperprolactinemia
• Amenorrhea
• Galactorrhea
• False +ve pregnancy tests
• Increased libido
Men
• Gynecomastia
• Decreased libido
Cardiac • Ventricular arrhythmia In case of overdose
• Cardiac conduction block
• Abnormalities in T-wave
Ocular Deposition in the anterior Common in chlorpromazine therapy
portion of the (eye & lens)
Others • Agranulocytosis Allergic reaction.
• Cholestatic jaundice
• Skin eruption

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Extra- Pyramidal symptoms of Neuroleptic drugs:

 Acute dystonia (spastic retro Collis or torticollis)
 Akathisia
 Parkinsonism
 Neuroleptic malignant syndrome
 Perioral tremor (rabbit syndrome)
 Tardive dyskinesia

Adverse effect of anti-psychotics

Weight gain due to increased appetite Ocular corneal and lens opacities
Effects due to dopamine blocked Effects due to cholinergic blockade
• Parkinsonism • Dry mouth
• Akathisia (motor restlessness) • Blurred vision
• Acute dystonia • Constipation
• Tardive dyskinesia • Urinary retention
• Gynecomastia, • Impotence
• Galactorrhea
Hypersensitivity reactions Serious adverse effect includes
• Cholestatic jaundice, photosensitive dermatitis • Neuropleptic malignant syndrome
• Blood dyscrasias (neutropenia with clozapine) • Prolongation of QT interval in ECG

Neuroleptic Malignant Syndrome:

This life threatening disorder occurs in pt who are extremely sensitive to the extra pyramidal effects
of antipsychotic agents.
Mechanism: Excessively rapid blockade of postsynaptic dopamine receptors.

Clinical presentation:
 Marked muscle rigidity
 Tremor
 Hyperthermia
 Autonomic instability with altered blood pressure and pulse rate.
Investigation:
 Leukocytosis
 Increased muscle type creatine kinase level
Treatment:
 Muscle relaxant: Diazepam, Dantrolene Sodium
 Dopamine agonist such as bromocriptine
 Switching to an atypical drug after recovery

Q. Recognized side effects of phenothiazine is/are- (Residency-2018)
a) Photosensitive dermatitis
b) Akathisia
c) Retinitis pigmentosa
d) Weight loss
e) Hypertension
Answer: T T F F F

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Q. The adverse effects of typical antipsychotic drugs due to “dopaminergic receptor

blockade” are (Residency-2013)
a) Galactorrhea
b) Orthostatic hypotension
c) Urinary retention
d) Neuroleptic Malignant syndrome
e) Sedation
Answer: T F F T F

02. Drugs used as Mood Stabilizers

Drugs used as mood stabilizers:

• Carbamazepine
• Divalproex
• Lamotrigine
• Lithium carbonate
• Topiramate
• Valproic acid
Lithium carbonate

Use –Bipolar disorder, schizophrenia

Adverse effects Toxicity
• Metallic taste • Slurred speech
• Anorexia and diarrhea • Coarse tremor
• Polyuria and polydipsia • Ataxia
• Nephrogenic diabetes insipidus • Confusion and fits
• Tremor
• Muscle weakness
• Goiter and hypothyroidism
• Leukocytosis
• ECG and EEG change
• Worsens psoriasis
• May be teratogenic

03. Anti-Depressants

Why depression occurs?

A) Mono Amine Hypothesis: Deficiency of monoamine neurotransmitters notably, nor adrenaline
& serotonin.

B) Neurotrophic Hypothesis: Background: The neurotrophic hypothesis of depression postulates

that neuronal plasticity is a key factor in the development of depression and in the clinical
response to antidepressants. Brain-derived neurotrophic factor (BDNF) is an important protein
in this process.

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Drugs Examples
Tricyclic antidepressant: Amitriptyline
blocks reuptake of serotonine, noradrenaline into nerve Imipramine
terminal. Dosulepin clomipramine
Significant first pass metabolism
Selective serotonin re-uptake inhibitors (SSRIs) Citalopram
Escitalopram
Fluoxetine
Fluvoxamine
Sertraline
Paroxetine
Monoamine oxidase inhibtors (MAOIs) Phenelzine
Tranylcypromine
Noradrenergic re-uptake inhibitors and SSRIs Venlafaxine, Duloxitine
Noradrenergic and specific serotonergic inhibitor mirtazapine

Comparison between SSRI & TCA

Traits TCA SSRI
Sedation + -
Anti histaminergic action + -
Anti-cholinergic action + -
Weight gain + -

Major Indications for Antidepressants

 Major Depressive disorder  Chronic Pain
 Bipolar depression  Tourette’s Disorder
 Obsessive compulsive Disorder  ADHD
 Anxiety  Eating disorders
 Panic disorder  Sleep disorders
 PTSD  Migraines
 Substance Abuse  Enuresis
Contraindication of TCA
 Epilepsy
 Arrythmia
 BEP
Cheese Reaction or Consequence of ingestion of tyramine containing food with MAOI:

Cheese, beer, red wine & banana contain tyramine

↓
In presence of MAOI, it escapes degradation
↓
Reaches systemic circulation
↓
Uptake by adrenergic neuron
↓
Enters storage vesicles & displaces NE
↓
Hypertensive crisis

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Anxiolytic Drugs:
Classification of benzodiazepine:

Ultra-short-acting Short acting (t1/2 <6 Intermediate acting Long acting (t1/2>24
hours) (t1/2 6-24 hours) hours)
• Clorazepate • Midazolam • Alprazolam • Diazepam
• Triazolam • Lorazepam • Clonazepam
• Oxazepam • Bromazepam • Flurazepam
• Estazolam • Quazepam
• Femazepam • Nitrazepam
• Parazepam
• Chlordiazepoxide

Barbiturates: (May act as both sedative & hypnotics)

Ultra-short acting (t1/2 <15min) • Thiopental sodium
• Methohexital
Short acting (t1/2 1-3 hours) • Pentobarbital
• Secobarbital
Intermediate acting (t1/2 4-6 hours) • Amobarbital
• Aprobarbital
• Butobarbital
• Butalbital
Long acting (t1/2 >6 hours) • Phenobarbital
• Mephbarbital

Q. The following are the anti-depressant drugs (Residency-2014)

a)Duloxetine
b)Risperidone
c)Mirtazapine
d)Venlafaxine
e)Clozapine
Answer: T F (Atypical antipsychotic) T T F (Atypical antipsychotic)

AnxietSee
04. Sedatives-Hypnotics t
Drugs used as sedative hypnotics=
• They includes –BDZ, barbiturates, newer agents
• BDZ enhances GABA activity &open CI channel causing hyperpolarization of cells
• It has anxiolytics, anesthetic anticonvulsant & muscle relaxants property
• They are better hypnotic than barbiturates

ABA
• Flumazenil is BDZ antidote,
• Comparison between BDZ & barbiturates.

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Traits BDZ Barbiturates

M/A Potentiate GABA GABA ergic & direct GABA mimetic
transmission action
GABA response Intensified Prolonged
Type of CNS Selective neuronal Generalized neuronal depression
depression depression
TI High Low
Hangover Less Marked
Tolerance Slowly develop Rapidly develop
Addiction liability Less More
Suicidal tendency Less More

Pharmacological effect of Benzodiazipines:

 Reduction of anxiety
 Sedation & hypnosis
 Reduces sleep latency of onset
 Increase NREM sleep (stage 2)
 Decrease REM sleep
 Anti convulsant effect
 Muscle relaxant
 Respiratory and cardiovascular depression
 Anesthetic (higher dose)

Adverse effect:
 Hangover
 Impaired judgement
 Confusion
 Ataxia at high dose
 Early morning insomnia
 Hallucination
 Nystagmus
 Tolerance – In case of BDZ by down regulation and in case of barbiturate by enzyme induction

Withdrawal Symptom of BDZ

 Anxiety
 Agitation
 Restlessness
 Rebound insomnia
 Orthostatic hypotension
 Hyperactive reflexes
 Generalized seizures
 Tremor
 Depression & suicide thinking
 Hallucination
 Hightened sensory perception
 Ataxia
 Paranoid delusions

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Q. Diazepam- (Residency-2017)
-
a) Is a sedative hypnotic drug
b) Has muscle relaxant effect
Bedil
c) Is effective in febrile convulsion
# d)
e)
Is a short acting benzodiazepine
Has active metabolite oxatpan
Febriks
Answer: T T T F T
Explanation: Effects of diazepam:Active
> -

 Sedation
 Hypnosis
 Anti-convulsion
 Anesthesia
 Muscle relaxation
 Long acting: half-life -30h

05. Anti-Perkinson Drugs

* In Parkinson disease dopamine is reduced, Ach concentration is increased, as dopamine has

regulatory effect on Achetylcholine
* D2 receptors are located in striatal neurons & substantia nigra on basal ganglia
* Dopamine does not cross BBB, So no therapeutic effect if given IV
Drug used in Parkinsonism:
Classification:
Dopamine analogues: Levodopa
 Peripheral deoxy decarboxylase inhibitor: Carbidopa, benserazide
 COMT-inhibitors: Tolcapone, Entacapone
 MAO-B inhibitors: Selegiline, Clorgyline
 Dopamine agonists: Rosipirole, Pergolide
 Central anti-cholinergics: Benzotropine, biperiden

06. Anti-Convulsant

Type of epilepsy & drug of choice- Generalized

Guideline for choice of anti-epileptic drug -
Epilepsy type First-time Second-time Third time
Focal onset
-

and/or O Lamotrigine Carbamazepine

Levetiracetam
Clobazam gabapentin oxcarbazepine
Phenobarbital phenytoin pregabalin
secondary GTCS Sodium valproate Primidone tiagabine
-
Topiramate
Zonisamide Focal
Oprimaryy
Lacosamide
GTCS Sodium Lamotrigine topiramate Carbamazepine phenytoin primidone
Valproate Zonisamide Phenobarbital acetazolamide
Levetiraceatam
o
Absence
-
Ethosuximide Sodium valproate Lamotrigine clonazepam
Myoclonic Sodium Levetiracetam Lamotrigine phenobarbital
valproate Clonazepam

Carbamazepine
N.B use as few drug as possible at the lowest possible dose

-
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Anti Convulsive
Classification of Anticonvulsants
Action on lon channels Enhance GABA Inhibit EAA Transmission
Transmission
Na+: Benzodiazepines (Diazepam, Felbamate
Phenytoin, Carbamazepine, clonazepam) Topiramate
Lamotrigine Barbiturates
Topiramate (Phenobarbital) Valproic acid
Valproic acid Gabapentin
Ca++: Vigabatrin
Ethosuximide Topiramate
Valproic acid Felbamate

Sodium valproate is useful in infantile epilepsy.

• It has low toxicity and lack of sedative action
• It may cause baldness, teratogenicity, coagulation disorder, pancreatitis.
Adverse effect of phenytoin
• CNS toxicity (Dose related) ataxia, diplopia nystagmus, vertigo, confusion
• Idiosyncratic- hepatic damages, rash. Megaloblastic anaemia, SLE, lymphadenopathy
• Teratogenicity- fetal hydantoin syndrome
• Effect due to chronic use- gingival hyperplasia, hirsutism, peripheral neuropathy,
osteomalacia
Adverse effects of carbamazepine
• Diplopia and ataxia
• Mild gastrointestinal upset
• Unsteadiness
• Drowsiness at higher dose
• Hyponatraemia and water intoxication have occasionally occurred and may be dose-related
• Mild and persistent leukopenia
• Erythematous skin rash

Side effects of Sodium Valporate:

Mnemonic

Valproate Side Effects

(VALPROATE)
V omitting
A lopecia
L iver
P ancreatitis/pantcytopenia
R etention of fat (weight gain)
O edema (edema)
A ppetite increase
T remor/thrombocytompenia
E nzyme inducer (liver)

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Q. Drug of choice in absence seizure:

a) Sodium valporate
b) Carbamazipine
c) Ethosuximide
d) Lamotrizine
e) Phenytoin
Answer: F F T F F

07. Migraine Pharmacology

Drugs used in acute attack of Migraine:

NSAII)
-
 NSAID



Antiemetics
-

5 HT1 agonist- Sumatriptan, Rizatriptan, Zolmitriptan.

Ergot alkaloids- Ergotamine
- -
P
aracetam
-

Drugs used in Migrane prophylaxis:



Verapamil
Valporic acid, Topiramate -
Triptan
 Pizotifen (Antihistamine & 5 HT antagonist)
 Amitriptyline, Dosulepine
 Flunarizine (Both Ca2+ & Na + channel blocker)
 Methysergide
 Propranolol

Q. Drugs used in migraine prophylaxis are (Diploma July 2019)

a) Sumatriptan
b) Ergotamine
c) Pizotifen
d) Propranolol
e) Methysergide
Answer: F F T T T

08. Anesthetics
Anesthetic: The agent that induces -
• Loss of pain.

S
• Adequate muscle relaxation
• Loss of reflexes
• With or without loss of consciousness & memory.
With loss of consciousness- General anesthesia
Without loss of consciousness- Local anesthesia.

Types:
1. Local anesthetics: Acts periphery. Blocks the conduction by peripheral nerve.
2. General anesthetics: Act on CNS.

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Classification of anesthesia:
1. Local anaethesia
A. According to chemical nature:

1. Ester compounds Short acting (1-2 hours) Long acting (16 hours)
• Cocaine •Tetracaine
• Procaine • Benzocaine
2. Amide compounds: Short acting (2-4 hours) Long acting (16 hours)
i
• Xylocaine •-Bupivacaine
• Lidocaine/Lignocaine: • Etidocaine
Most common, widely used • Ropivacaine

B. According to route of administration

1. Surface (Topical): Xylocaine, cocaine (as solution, jelly, cream or lozenge)
2. Infiltration anesthetics: Xylocaine, cocaine (To paralyze the sensory nerve endings & small
cutaneous nerves)
3. Regional anesthetics:
i. Nerve block: The drug is injected around the appropriate nerve, e. g pudendal block
ii. Intravenous: The drug is injected IV (with Ad) e.g. Anesthesia of arm.
iii. Extradural/Epidural: The drug is injected in the extradural/epidural space. It is widely used
in obstetrics.
Opoid analgesics may also be used intrathecally & extradurally. They are highly effective in skilled
hands for intractable pain, including post-surgical pain.

II. General anesthetics

-
Inhalation anesthetics -
Intravenous anesthetics
 No⑧  Barbiturates- Thiopental Na, Methohexital.
 Halothane  Benzodiazepines - Diazepam

=
 Enflurane  Opioid analgesics - Morphine, Fentanyl, Pethidine.
 Isoflurane  Propofol
 Desflurane  Ketamine
 Sevoflurane  Miscellaneous drugs: Droperidol, Etomidate.
 Cycloprofen
 Chloroform
O Ether

Mechanism of action of local anesthetic

 L.A prevents the initiation & propagation of nerve impulse (action potential)
 Local anesthetic
 Binds with specific receptor present in the cell membrane
 Blocks influx of Na+ through voltage gated Na+ channels
-

 Blocks the depolarization

 Increase the threshold of excitability
 Conduction is blocked at afferent nerve endings and by sensory & motor nerve fibers.
(Local anesthetic)

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Effects:
 Blocks different neurons (both sensory & motor fibres)
 Anti-consultant action (parental route)
 Acts as anti-arrhythmic drug (they block the pace maker activityanti-arrhythmic effect)

& LA action can be prolonged by

 Altering site of injection
 Increasing dose/repeated injection
-

 Adding vasoconstrictor (adrenaline /felypressin-1:200000/400000)

-

Adverse effects of local anesthetics

-
Central nervous system Sleepiness
-
Light headedness
-
Visual & auditory disturbance
Restlessness
Circumoral & tongue numbness
&Nystagmus

Neurotoxicity
E
Muscular twitching

O CVS Myocardial depression

Vasodilation
O
Hypotension
Hypertension, arrhythmias and acute myocardial failure
Hematological effects Methemoglobinemia (prilocainetoluidine blueHb is oxidized to
methaemoglobin. As a result chocolate colored cyanosed blood)
Allergic reactions

Preanesthetic medication
 In addition to general anesthetic agent, there are considerable number of drugs used before
and during surgical operation.
 This use of drug is called pre-anesthetic medication

Importance:
 To do a safe anesthesia-induction, maintenance & recovery
 To prevent per-operative complications
 To prevent post operative hazards
-

Drugs for premedication with use:

 O
To reduce anxiety & tension: Benzodiazepines – Diazepam, Temazepam
- -

 To prevent allergic reactions: Anti-histamine drugs

- -

 To reduce bronchial secretion: Atropine sulphate

-


-

To inhibit bronchospasm:
-
Atropine sulphate
 To inhibit bradycardia: Atropine
- -

 To decrease HCL secretion or neutralization: H2 blocker or Antacid

 To prevent vomiting: Domperidone, Metoclopramide
 To relieve pain: Morphine, pethidine, phentanyl.

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Intervenors Anesthetics at a Glance

Drug Advantages Disadvantages Use Contraindication ADRS
Thiopental Rapid onset Less analgesia & Induction of CVS disease, Apnea,
sodium (20-30sec) muscle GA Hypersensitivity, hypotension
Short acting(4- relaxation, COPD Hiccup
7min) Cumulation Hepatic Hangover
Anesthesia occur, causes dysfunction
without cardiorespiratory Addisons disease
excitement depression &
laryngospasm,
cannot be used
alone
Ketamine Duration lasts No muscle Burn HTN, CCF, Stroke HTN raised ICP &
for 10-15 min relaxation, post- dressing, BM raised ICP & IOP IOP, arrhythmia,
Analgesia (+) operative psychic sampling, pregnancy before CCF
Less vomiting phenomenon circumcision, term, psychosis Psychosis,
& patient with emergence,
bronchospasm, shock Phenomenon
useful in
children
propofol Rapid onset- No analgesic Balanced Hypotension,
recovery, effect anesthesia, apnea, injection
Antiemetic Cumulation surgery site pain,
action, costlier outpatient sedation, reduced
Onset is procedure ICP acidosis
similar to
thiopental
causes
euphoria

Inhalation Anesthetics:
Drug Advantages Disadvantages Indication Contraindication
/ADRS
Nitrous Rapid induction & Less potent, no Maintenance Increased ICP,
oxide recovery, strong analgesia, muscle relaxation, of anesthesia, postoperative nausea&
safe nonirritant, acts in used with other refractory vomiting, BM
low concentration, more potent drug, pain in suppression in prolong
nonflammable, no postoperative terminal exposure, teratogenicity
hangover hypoxia, expensive illness
Halothane Highly potent, non- Produce Maintenance Hangover,
explosive, nonirritant, cardiorespiratory of anesthesia cardiorespiratory
rapid & smooth induction depression, relaxes during depression,
(2,3min) less post- uterus causing PPH, surgery hepatotoxicity,
operative nausea & causes arrhythmia hypotension
vomiting, suitable in Raised ICP
pediatric & asthma patient

Adverse effect of spinal anesthesia:

 Bradycardia
 Hypotension
 Respiratory depression
 Post operative urinary retention

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Drugs Avoid before OT

 ACEI, ARB – Stop 24 hours before
 MAOI-2-3 Weeks before
 Metformin – 24 hours before
 Short acting insulin – avoid OT morning dose
 Levodopa – avoid on that day
 OCP -4 weeks before OT
 Antiplatelet – stop 7 days before OT
 LMWH-stop 24 hours before OT
 UFH – 2-6 hours before OT
 Any vitamin - 48 hours before OT

Q. Ketamine (Residency-2021)
a) Causes profound analgesia
b) Usually produces bradycardia and fall of BP
c) Produces muscle relaxation
d) Decreases intracranial and intraocular pressure
e) Causes hallucination
Answer:
a) T
b) F (It produces tachycardia, hypertension and increased cardiac output)
c) F (no muscle relaxation)
d) F (increases intracranial and intraocular pressure),
e) T
Q. Inhalational anesthetic drugs are (Residency-2020)
a) Propofol
b) Halothane
c) Ketamine
d) Nitrous oxide
e) Savoflurane
Answer: F T F T T
Explanation:
Others- Isoflurane, desflurane, chloroform

09. Analgesic Drugs

Analgesics: The drugs that relives pain are called analgesics.

Classification of analgesics:
1. Narcotic analgesics (opioid group)

[Link]: Opium alkaloids b. Semi-synthetic opoiats c. Synthetic

i. Morphine, Codeine, • Oxy-morphone • Meperadine (pethidine)
ii. Benzyl isoquinoline • Hydro-morphone • Alpha-prodine
group: • Oxy-codone • Methadoen
Papaverine, Narcotine • Hydro-codone • Pentazocine
• Heroin • Fentanyl

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2. Non-narcotic analgesics (NSAID group): (non-opioid)

 Para-aminophenol group: paracetamol
 Propionic acid group: ibuprofen, ketoprofen, Fenoprofen.
 Fenamic acid group: Mefenamic acid
 Salicylic acid group: aspirin, trisalicylate
 Acetic acid group: Indomethacin, Diclofenac, tolmetin
 Enolic acid group: phenylbutazone, Piroxicam, Tenoxicam
 Non-acidic drug: Nabumetone

Q. Non-opioid analgesics are (Residency – 2018)

a) Tramadol (Opioid)
b) Aspirin
c) Ibuprofen
d) Pethidine (Opioid)
e) Diclofenac
Answer: F T T F T

10. Opioid Analgesic

Difference between opioid & non – opioid analgesis

Opioid Non-opioid
[Link] in acute visceral sharp pain [Link] in dull (mild) pain like headache, bodyache,
(moderate, severe pain) toothache or join pain that is non-visceral or
somatic pain
[Link] pain by acting on CNS [Link] pain by peripheral mechanism
[Link] tolerance & physical [Link]’t produce
dependence
[Link] CNS 4. Don’t so
[Link]’t anti-inflammatory & anti-pyretic [Link] anti-inflammatory and anti-pyretic action
anction

Opioid
Function of opioid receptors
Receptor sub Functions
µ (mu) Supraspinal & spinal analgesia
Sedation
Respiratory inhibition
Slowed GT transit
Modulation of hormone & neurotransmitter release
δ (delta) Supra spinal & spinal analgesia
Modulation of hormone & neurotransmitter release
κ (kappa) Supra spinal & spinal analgesia
Psychomimetic effects
Slowed GT transit

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Morphine
• Morphious → Goddess of dream (Greek mythology)
• Morphine produces euphoria.
• Source: Pappaver somniferum → Unripen seed capsule → Longitudinal parallel incision →
Milky exudates → Dried in air → Brownish sticky mass → Powder of opium.
• Chemical nature: Alkaloid.

Pharmacological action of morphin:

CNS effects:
1. Selective depression of CNS: • Analgesia -
-
• Sedation
-

• Respiratory depression
-

• Cough suppression (Anti-tussive effect)

-

• Inhibition of heat regulatory centre

-

Euphoria.
E
-

2. Selective stimulation of CNS: • Edinger-westphel nucleus (3rd nerve) → Miosis

(constriction of pupil)
• Chemoreceptor trigger zone 0 (CTZ) → Vomiting, nausea.
• Hyperactive spinal cord reflex. -
• Convulsion.
=
• Truncal rigidity
3. Changes of the mood • Euphoria
• Dysphoria.
⑤
S
4. Dependence: • Physiological
-

• Psychological
Peripheral effects:
OCVS • Dilatation of resistance (arterioles) & capacitance (veins) vessels by
central action.
-

O
GIT • Constipation,
-
• ↑GIT tone.
• ↓Motility
• Decrease HCI secretion
• Diminish propulsive peristatic wave in the colon
-
Biliary tract • Contraction of biliary smooth muscle (Spasm) → Biliary colic.
-
• Constriction of sphincter of Oddi.
Ureter & urinary • ↑Ureteral & bladder tone.
bladder • ↑Sphincter tone → & Urinary retention.
&
Uterus • Prolongation of labour.
Neuro-endocrine • ↑ADH, Prolactin, Somatostatin secretion

②
• ↓H secretion
Respiratory • Bronchosecretion
system: • Bronchospasm (by releasing histamin)
-
Skin Due to CNS effects & peripheral histamine release
• Flushing
• Warming
• Itching
• sweating

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Analgesic mode of action of morphine

 By inhibiting the pain pathway
 By stimulatin the pain inhibitory pathway

>poid
Indications of morphine:

bun-
- Acute MI
 Severe somatic pai, e.g. extreme burn, fracture
 Chronic pain in terminal cancer patient
 Obstructive labour
 Diagnosed abdominal pain
-

 Acute LVF, acute pulmonary oedema.

-

 Pre-anaesthetic medication (as analgesic)

-

 Non-specific diarrhoea - Traveller's diarrhoea & Summer diarrhoea

 ey
Suppression of cough.
codeine
-
Contraindications:
 Undiagnosed acute abdominal pain.
 Head injury.
 Extreme age (metabolism of drug)
 Liver disease, kidney disease.
 Pt of poor respiratory reserve - Asthma, Emphysema, Bronchiectasis.
 Hypothyroidism, Myxedema.
 Convulsive disorder 8. Biliary colic
 Renal colic
 Pregnancy
 Addision's disease.

Adverse effects of Morphine:

 Tolerance, Dependance.
 Addiction
 Constipation
 Nausea, vomiting
 Myosis / ppp
 Respiratory depression.
 Bradycardia
 Convulsion
 Urinary retention. To
 Itching around nose, Urticaria.
 Behavioural restlessness, tremulousness
 Increase intracranial pressure
13. Postural hypotention.

Advantage of morphine as post operative analgesic,

 It is a very strong analgesic
 It has also hypnotic effect
 It produces powerful sense of contentment & well-being

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Disadvantage of morphine as post operative analgesic,

 It suppress cough reflex
 It can cause respiratory depression, bronchoconstriction
 It may cause emesis, constipation & urinary retention
 It can cause dependence

Tolerance of morphine not developed in following effect:

 Miosis /constricted
 Constipation
-
30
 Convulsion
-

Morphine vs pethidine
Points -
Morphine
10
Pethidine
-100mg
Source Natural opium Synthetic alkaloid
Analgesic potency 10 times more Less
Duration of analgesia 4-6 hours 2-3 hours
Cough suppression +++ +-
Effects on labor Delay labor. No delay in labor: so
Not as pethidine Used in labor
As antispasmodic Not as pethidine Superior due to its putative
(biliary and renal colic)
Effect on eye Miosis Mydrasis
Hypnotic/ respiratory Marked Less
Depressant/ broncho-constriction
effect
Histamine release ++ Large dose show
Antihistaminic action
Tolerance develops quickly Develops slowly
Addiction More risk Less risk
Safety Less safe More safe

Morphine poisoning:
3 Stages: excitation, stupor and narcosis
Death occur due to respiratory failure
3 cardinal/ pathognomonic sign:
 Pin point pupil (miosis)
 Respiratory depression
 Coma
Can be treated with
 Stomach wash
 Anti-dote= naloxone, naltrexone
Opioid withdrawal:
Sign & symptoms (narcotic abstinence syndrome):
 Irritability, aggression, sneezing
 Lacrimation, yawning chillis, hyperventilation, mydriais
 12-16hours after last dose of opiods

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24-72 hours after last dose of opiodis:

 Muscular aches
 BP crisis
 Grose spasm abdominal pain
Opioid administration immediately suppresses the symptoms
Can be treated with methadone.

Addicting drugs:
• Opioids
• Cnnabis indiaca
• Alcohol
• Nicotine
• Barbiturates
• Cocaine
• Amphetamine

Q. Following statement is / are true for Pregabalin (Residency March 2022)

a) Acts on CADA receptor
b) Used in the treatment of Generalized seizure
c) Used in the treatment of Neuropathic pain
d) Eliminated unchanged from the body
e) Induces Hepatic microsomal enzyme
Answer: F F T T F
Explanation:
a) Acts on Alpha 2 Delta receptor
b) Use of Pregabalin - Partial seizure
 Neuropathic pain
 Herpes zoster lesion
c) Is used
d) Renal excretion more mostly unchanged
e) Doesn’t induce.
Q. Tolerance may occur to the following effects of morphine (Residency – 2017)
-
a) Sedation -

-
b) Constipation X
c) Analgesia
-
d) Euphoria
e) Miosis
~

Answer: T F T T F
Explanation:
Degree of tolerance developed: High:
 Analgesia
 Euphoria
 Sedation
 Respiratory depression
 Antidiuresis
 Cough suppression
Intermediate:
 Bradycardia

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-
Limited/None:

-
 Miosis
 Constipation
 Convulsion
Tolerance may not develop on 3C:
 Constipation
 Coma
 Miosis

11. NASAIDs
1. Classification of NSAIDS:
1. According to their anti-inflammatory action
Drugs having weak anti- Para-aminophenol group, e.g. paracetamol
inflammatory effect
Drugs having mild to moderate Propionic acid group:
anti-inflammatory effect: • Fenoprofen
• Ketoprofen
• Naproxen
• Ibuprofen
Fenamic acid group:
Mefenamic acid
Non acidic drugs
• Nabumetone
Drugs having strong anti-inflammatory effects
Salicylic acid group  Aspirin
 Trisalicylate
Pyrazolone derivatives • Phenylbutazone
• Oxyphenbutazone
Acetic acid derivatives • Diclofenac
• Indomethacin
• Etodolac
• Sulindac
Oxicam derivatives • Piroxicam
• Tenoxicam
2. According to COX selectivity
COX-1 and COX-2 non selective • Diclofenac
• Indomethacin
• Aspirin
• Trisalicylate
• Naproxen
• Ibuprofen
Selective (COX-2 selective) • Etoricoxib
• Celecoxib
• Rofecoxib
• Valdecoxib
• Nlimesulide
• Meloxicam

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Recommendations for the use of NSAIDs:

• Current use of anticoagulants is a contraindication to NSAID use
• Avoid NSAIDs in the elderly and in those with important comorbidity including heart failure
and hypertension
• Start with the lowest dose of one of the safer established NSAIDs (e.g. ibuprofen) and only
increase the dose if required
• If an unsatisfactory result is obtained with one NSAID, a trial of another NSAID may be
warranted
• Never prescribe more than one NSAID at a time
• Allow a 2-3-week trial to assess efficacy of any particular NSAID or dose.
• For a patient with recognized risk factors for gastrointestinal ulceration consider co-
prescription with omeprazole or misorprostot.

Cox inhibitors
COX inhibitors:
• COX-I specific inhibitors: e.g. Low dose aspirin.
• COX nonspecific inhibitor (inhibitor COX-I & II): e,g. traditional NSAIDS.
 Propionic acid group: inuprofen, ketoprofen, fenoprofen, Flurbiprofen, Naproxen
 Fenamic acid group: Mefenamic acid
 Acetic acid group: Indomethacin, Diclofenac
 Enolic acid group: Phenylbutazone, Piroxicam, Tenoxicam
 Non-acidic drug: Nabumetone
Analgesics

E
=

COX-II preferential inhibitors (inhibition of COX-II but weak inhibition of COX-I)

• Meloxicam
• Etodolac
• Nofumetone
• Nimesulide

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COX-2 selective inhibitors:

• Celecoxib - for chronic pain.
• Roficoxib- for acute pain.
• Etoricoxib
• Valdecoxib
• Lumiracoxib
Features of nonselective e COX inhibitors and selestive COX-II inhibitors:
Action Cox-I/COX-2 Inhibitors Cox-2 Inhibitors
Analgesic + +
Antipyretic + +
Anti-inflammatory + +
Anti-plattelet aggregatory + -
Gastric mucosal damage + −
Renal salt/ water retention + +
Delay/ prolongation of labor + +
Ducts arterosus closure + ?
Aspirin sensitive asthma precipitation + ?
Gout
• NSAIDS
• Colchicine
• Allopurinol
• Febuxostat
• Uricosuric drugs, such as probenecid, sulfipyrazone and benzbromarone
• Pegloticase
• Oral or I/M steroid in acute attack

Side effects of some important DMARDs

Methotrexate Sulfasalazine Leflunomide
• GI upset • Nausea • Nausea
• Stomatitis • GI upset • GI upset
• Rash • Rash • Rash
• Alopecia • Hepatitis • Alopecia
• Hepatotoxicity • Neutropenia • Hepatitis
• Acute pneumonitis • Pancytopenia • Hypertension
• Hepatic fibrosis
• Bone marrow failure
• Aplastic anaemia
Ciclosporin Azathioprine Cyclophosphamide
• Nausea • Nausea • GIT upset
• GI upset • Vomiting • Ovarian failure
• Renal impairment • Bone marrow • Azospermia
• hypertension depression • Infertility
• Hepatic toxicity • Bone marrow
• Aplastic anaemia suppression
• Agranulocytosis
• Hemorrhagic cystitis

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Q. Drugs inhibit cyclooxygenase (Residency – 2016)

a) Diclofenac
b) Penicillamine
c) Chloroquine (Anti Malarial Drugs)
d) Valdecoxib (Selective Cox2 inhibitor)
e) Methotrexate (Cytotoxic)
Answer: T F F T F
Explanation:
a) NSAID
d. COX-2 selective NSAID

Anti Microbials
-

12. Anti-Bacterial

Mechanism of action of important ankmicobical:

Mechanism of action Drug
Inhibition of Cell wall synthesis
Antibacterial activity Penicillin, cephalosporins, imipenem,

Beto Inhibition of cross-linking (transpeptidation) of

peptidoglycan
aztreonam, vancomycin

Lactam Inhibition of other steps in peptidoglycan synthesis Cycloserine, bacitracin

- Antifungal activity Caspofungin
Inhibition of glucan synthesis
Inhibition of Protein Synthesis
70550 .

O
Action on 50S ribosomal subunit -

30
-
Chloramphenicol, erythromycin,
-

clindamycin, linezolid CML -

⑧
Action on 30S ribosomal subunit Tetracycline’s and aminoglycosides
Inhibition of nucleic acid synthesis Metronidazole
-

Inhibition of nucleotide synthesis 6

Sulfonamides,- trimethoprim I folate
poiso antagonish
-

Inhibition of DNA synthesis -Quinolones, e.g. ciprofloxacin

①
Inhibition of mRNA synthesis 6
Rifampicin
Alternation of cell membrane function
Antibacterial activity Polymyxin, daptomycin, colistin
Antifungal activity Amphotericin B, nystatin, terbinafine,
azoles, e.g. itraconazole
Other Mechanism of action
• Antibacterial activity
- - G ethambutol,
Isoniazid, metronidazole, -

pyrazinamide
-

• Antifungal activity Griseofulvin, pentamidine

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Antibiotics classification:
According to spectrum of activity
Broad spectrum antibiotics Ampicillin
Antibiotics that have wide range of Amoxicillin
antimicrobial activity on Tetracyclines
Gram (+) ve, gram (-) ve Cephalosporins
Narrow spectrum antibiotics Benzylpenicillin
Antibiotics that have narrow range Cloxacillin
Of antimicrobial activity

Antibiotic combination:
&
Aims: Useful in: Disadvantages:
-• To obtain synergism • Mixed infection • -Super infection
- -

• Prevent resistance • Unknown infection • Adverse effect

•-
- -

Broaden spectrum • Enhance anti- • eCostly

-

• Reduce
-
dose & microbial activity • antagonism
adverse effect of • Prevention of
- -

↑ -
individual drugs resistance
-

2+ 2 =
Antimicrobial effective against gram positive bacteria:
 Penicillin: =
-

-
Benzyl penicillin, Phenoxymethyl penicillin, Ticarcillin, Flucloxacillin,
-
Dicloxacillin.
 1st
-
& 2nd generation cephalosporin: Cephradine, cefalaxin, cefazolin, cefuroxime
 Macrolides : Erythromycin, Azithromycin, clarithromycin
-Carbapenem
-
 Vancomycin
 Chloramphenicol Quindone
-
 Aminoglycoside: Gentamycin
 Clindamycin
 Folate antagonist: co trimoxazole, Trimethoprim, sulphonamide
-
 Fluroquinolones: Moxifloxacin, Trovafloxacin ·
verofloxa -

Antimicrobial activity against gram negative Bacteria:

-
 Broad spectrum penicillin: Amoxicillin, ampicillin.
 Extended spectrum penicillin: Ticaracillin, pipercillin, Mezlocillin, Azlocillin.
 3rd & 4th generation cephalosporin: Ceftazidime, cefoperazone, cefipime.
 Monobactam: Aztronem
-
 Carbapenem: Itrapenem, Imepenem, Meropenem
 Clindamycin,
 Tetracyclin
 Folate antagonist: co trimoxazole, Trimethoprim, sulphonamide
-
 Floroquinolones: Ciprofloxacin, levofloxacin, lomefloxacin

Drug Resistance
Genetic: chromosomal & extra chromosomal (plasmid mediated & transposon mediated)

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Non- genetic
a) Production of enzymes that destroy the drug
 B lactamse by staphylococci-inactivates penicillin-G
 Acetyltransferase by gm (-) ve bact, inactivates-chloramphenicol
T Beta
lactamase

 Kinase inactivates –aminoglycoside

b) Alternation of receptor binding site
 Loss/alternation of 30s ribosomal subunit leads to aminoglycoside resistance,
 Loss/alternation of 50s ribosomal subunits leads to erythromycin resistance
 Loss/alternation of PBP leads to penicillin/cephalosporin resistance
c) Altered membrane permeability or uptake
d) Efflux of drug from cell
E.g.- ciprofloxacin
e) Development of altered metabolic pathway
e.g. utilization of folic acid rather PABA leads to sulfonamide resistance.
f) Production of altered enzyme that can affected by drug
e.g. DHF (dihydrofolate) reductase in trimethoprim resistant bacteria
talacta
-
staphytococci:
-
The following antimicrobial drugs are effective against penicillinase producing
-

• Methicillin -
• Cloxacillin-
-

• Nafcillin
• Dicloxacillin
• Oxacillin
• C
Flucloxacillin
• Imipenam
• Augmentin
• Dalfopristone
• Co amoxiclav

-
Limitation of penicillin G:
•
•
β lactum ring structure present
bactericidal
RSA
• water soluble
• Inactivation by gastric & B lactamase
• Infective against Gm-ve organism
• Short acting, poor penetration
• Injection is painful

Prophylactic use of penicillin includes:

• Rh. Fever
• Syphilis
• Surgical patient with valvular heart disease
• Infective endocarditis
• Gonorrhea

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Spectrum of cephalosporin activity:

& First generation cephalosporin-
#
Excellent activity against gram-positive organisms and some activity against gram negatives
Oral Parenteral
• Cephradine • Cefazolin
• Cefadroxil • Cephradine
• Cephalexin

⑧ Second generation cephalosporin

Gram positive activity but have activity against anaerobic, gram negative bacilli.
Oral Parenteral
• Cefuroxime • Cefuroxime
• Cefaclor • Cefoxitin

Third generation cephalosporin:

Further improve activity against gram negative bacteria.
Ceftazidime and cefoperazone are useful against [Link]

Oral Parenteral
• Cefixime • Ceftriaxone
• Ceftibuten • Ceftazidime
• Cefotaxime • Cefoperazone
• Cefpodoxime • Cefotaxime

Fourth generation cephalosporine:

Agents have an extremely broad spectrum of activity, including pseudomonas spp. Staph aureus and
streptococci

Only parenteral
• Cefepime
• Cefpirome

Fifth generation:
Ceftobiprole
Ceftaroline

Anti-pseudomonal antibiotics:

i)Anti-pseudomonal penicillin ii) anti-pseudomonal cephalosporin’s:

Carboxy penicillin ceftazidime, cefoperazone (3rd generation)
Carbenicillin cefepime, cefpirome (4th generations)
Ticarcillin
Ureidopenicillin iii) others:
Mezlocillin Carbapenems
Azlocillin Gentamicin
piperacillin Quinolones

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↑

Mnemonic: CAMPFIRE
 Carbapenems
 Aminoglycosides
 Monobactams
 Polymyxins (eg, polymyxin B, colistin)
 Fluoroquinolones (eg, ciprofloxacin, levofloxacin)
 Third-and fourth –generation cephalosporins (eg. Ceftazidime, cefepime)
 Extended-spectrum penicillins (eg, piperacillin, ticarcillin)

Following antibiotics used to treat MRSA:

 Linezolid
-

 Vancomycin
 Streptogramin
 Daptomycin
 Tigecycline
-

 Cotrimoxazole
 Rifampicin

 Doxy opeline
Tetracycline
Clindamycin

Aminoglycosides:
Basic information of aminoglycosides:
 Gentamicin: isolated from micromonospora purpurea & streptomycin from a strain of
Streptomyces griseus
 Polycationic water soluble, irreversible protein synthesis inhibitor, have low therapeutic index,
mainly extracellular distribution, having concentration dependent killing & post antibiotic
effect.
-

 All are narrow spectrum except gentamycin, tobramycin & netilmycin all are teratogenic,
ototoxic, nephrotoxic, neurotoxic
-

 Acts by interfering initiation complex formation, misreading of mRNA, breakdown of polysome

into non functioning monosomes
 Relatively inactive against anaerobs, useful in combination with penicillin to treat Gm-ve
infections, sepsis, endocarditis & some topical indications
6
 Vestibilar damage is reversible comes earlier & cochlear damage is irreversible comes later,
=
nephrotoxicity is reversible. -

Pharmacokinetics:
 Bactericidal
02
-
dependent
 hydrophilic
 Negligible oral absorption
Ami
 Negligible CSF and corneal penetration
 Peak plasma levels 30 minutes after infusion
 Monitoring of therapeutic levels required.

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Nucleic acid synthesis inhibitors

DNA gyrase inhibitors (Quinolone) Folic acid synthesis inhibitors
First generation Inhibitors of folate synthesis
 Nalidixic acid • Sulfonamide
Second generation • Trimethoprim
 Ciprofloxacin • Pyrimethamine
 Pefloxacin
 Ofloxacin
=
 Levofloxacin

Florine
Third generations
 Clindafloxacin wroflox
 Gatifloxacin -
 Sparfloxacin
Fourth generation
 Moxifloxacin
 Trovafloxacin

Side effects of all antibiotics:

> Diarrhea
Penicillin Macrolides: - -
Hypersensitivity 1. Gastrointestinal upset, especially in young adults
• Allergic reactions include anaphylactic (erythromycin 30%).
shock (very rare-0.05% of recipients); 2. Cholestatic jaundice with erythromycin estolate.
serum sickness-type reactions (now -
3. Prolongation of QT interval on ECG, potential for
[ fever, joint swelling,
rare—urticaria, torsades de pointes.
angioneurotic edema, intense pruritus, 4. Clindamycin predisposes to C. difficile infection
and respiratory embarrassment occurring
7-12 days after exposure) Tetracycline:
-
pseutoment
• A variety of skin rashes. Oral lesions, • Superinfection
fever, interstitial nephritis (an 08
• Bone & Teeth disease (Hyperplasia, Pigmentation
autoimmune reaction to a penicillin- caries, retarded growth)
protein complex), eosinophilia, hemolytic • Hepato & Nephrotoxicity
anemia and other hematologic • Photosensitivity
disturbances, and vasculitis may also • GI upset
occur.  Fanconi syndrome
• Nafcillin is associated with neutropenia;
oxacillin can cause hepatitis; and -
Chloramphenicol:
methicillin causes interstitial nephritis  Bone marrow suppression
(and is no longer used for this reason).  Greybaby syndrome
• Large doses of penicillins given orally 
-

GI upset
may lead to gastrointestinal upset,  Neuritis
particular! nausea, vomiting, and ①
diarrhea. Ampicillin has been associated
with pseudomembranous colitis.
• Secondary infections such as vaginal
candidiasis may occur.
• Ampicillin and amoxicillin can cause skin
 ashes that are not allergic in nature.
These rashes frequently occur when
arninopenicillins are inappropriately
prescribed for a viral illness
Sulfonamides antibiotics: Amino glycosides:

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 Hypersensitivity 1. Renal toxicity (usually reversible) accentuated by

 Crysrtalluria other nephrotoxic agents.
 Renal tubular necrosis 2. Cochlear toxicity (permanent) more likely in older
 Haemolytic people and those with a predisposing mitochondrial
 Aplastic anaemia gene mutation.
 Kernicterus, 3. Neuromuscular blockade after rapid intravenous
infusion (potentiated by calcium channel blockers,
myasthenia gravis and hypomagnesaemia)
4. Teratogenesis
Amphotericin B Quinolones:
 Fever and chills: 1. Gastrointestinal side-effects in 1-5%.
 Renal impairment 2. Rare skin reactions (phototoxicity)
 Hypotension 3. Achilles tendon rupture is reported, especially in
 Anemia- caused by a reversible older people.
suppression of erythrocyte production 4. CNS effects (confusion, tremor, dizziness and
may occur occasional seizures in 5-12%), especially in older
 Thrombophlebitis people.
5. Reduces clearance of xanthines and theophyllines,
potentially inducing insomnia and increased seizure
potential. 6. Reports of prolongation of QT interval on
-
6. Cases of hypo- or hyperglycaemia in association with
gatifloxacin, so glucose monitoring is needed in
patients with diabetes or those with severe hepatic
dysfunction.
7. Ciprofloxacin use is associated with the acquisition
of MRSA and emergence of C. difficile ribotype 027

Fluoroquinolones:

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Irrational prescribing = Pathological prescribing

 Use of drugs when no drug therapy is indicated
 Use of wrong drug for specific condition
 Use of drugs with doubtful or unproven efficacy
 Use of drugs of uncertain safety status
 Failure to provide available, safe & effective drugs
 Use of correct drugs with incorrect administration, dosages & duration
Examples of inappropriate
Prescribing practices
 Overuse of antidiarrheals for nonspecific childhood diarrhea
 Indiscriminate use of injections, e.g. in malaria treatment
 Multiple or over-prescription
 Excessive use of antibiotics for treating minor acute respiratory tract infections
Factors Underlying Irrational use of Drugs
Patients
 Drug misinformation
 Misleading beliefs
 Patient demands/expectations
 Marketing pressures
 Economic considerations
 Lack of access to proper health care
Prescribers
 Lack of education and training
 Inappropriate role models
 Lack of objective drug information
 Generalization of limited experience
 Misleading beliefs about drugs efficacy
 Delayed lab results, fear of clinical failure Inappropriate peer norms
 Local medical culture
 Economic incentives
 Patient demand of “quick fix”

Q. Which of the following drugs may cause SIADH?

a) Alpha lipoic acid
b) Carbimazole
c) Cisplatin
d) Desmopressin
e) Tricyclic antidepressant
Answer: F F T T T
Q. Following is / are crucial measures to contain antimicrobial resistance (Residency
March 2022)
a) Prescribing of newer antimicrobials
b) Recycling of antimicrobials
c) Adherence to local antimicrobial guideline
d) Prescribing of injectable antimicrobials
e) Availability of culture sensitivity
Answer: F F T F T

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Q. Inhibitors of protein synthesis that target 50S ribosomal subunit are (Diploma
July 2019)
a) Azithromycin
b) Amikacin
c) Clindamycin
d) Linezolid
e) Cephalosporin
Answer: T F T T F
Explanation:
Inhibitors of 50S ribosomal subunit: (CEC L)
 Chloramphenicol, Clindamycin
 Erythromycin, Linezolid

Inhibitors of 30S ribosomal subunit:

 Tetracyclines
 Aminoglycosides
 Spectinomycin

Q. Penicillin G is (Residency-2020)
a) A synthetic penicillin
b) β-lactam antibiotic
c) Responsible for type hypersensitivity reaction
d) A nucleic acid synthesis inhibitor
e) Effective in treating gas gangrene
Answer: F T T F T
Explanation:
a. Natural
d. Cell wall synthesis inhibitor
e. Others
Tetanus, syphilis, gonorrhea, pneumococcal, streptococcal infection, Meningococcal meningitis
Q. Antipseudomonal antibiotics include (Residency-2016)

-I
a) Ticarcillin
b) Flucloxacillin
c) Cephradine
d) Ciprofloxacin
e) Amoxicillin
Answer: T F F T F
Camp Fire
 C-cabapenem
 Aminoglycosides
 M- Monobactam
 P-Polymyxin (polymyxin B, colistin)
 F-Fluroquinolones
 IR- 3rd Generation (Ceftazidime, Cefoperazone) & 4th Generation cephalosporins (Cefepime)
 E-Extended spectrum penicillin
 Piperacillin, ticarcillin.

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13. Anti-TB Drugs

Classification of anti TB drugs-
First line drugs Second line drugs
 Isoniazid  Amikacin
 Rifampicin  Amino salicylic acid
 Pyrazinamide  Capreomycin
 Ethambutol  Ciprofloxacin, levofloxacin
 streptomycin  Clofazimine
 Ethionamide
 Rifabutin
 Rifapentine

Anti TB drugs at a glance

Isoniazid Rifampicin pyrazinamide streptomycin ethambutol
Mode of Cell wall DNA Unknown Protein Cell wall
action synthesis transcription Synthesis synthesis
Major Peripheral Febrile reactions Hepatitis 8th nerve Retrobulbar
adverse neuropathy Hepatitis Gastrointestinal damage Neuritis 3
reactions Hepatitis Rash Disturbance Rash Arthralgia
rash Gastrointestinal hyperuricaemia
Disturbance
Less Lupoid Interstitial Rash Nephrotoxicity Peripheral

Sep
common reactions Nephritis Photosensitizati agranulocytosis Neuropathy
adverse Seizures Thrombocytopen on rash
reactions psychoses ia Hemolytic gout
anaemia
Adverse effect:
Rifampicin • Harmless orange/red coloration of body fluid, such as saliva,tear urine sweat etc
• Liver damage-cholestatic jaundice, hepatitis
• Flu-like syndrome-fever, chillis , muscle pain, respiratory wheeze etc
• Haemolytic anaemia
• Rash
• Thrombocytopenia
• Nephrotoxicity
INH/Isoniazid • Liver [Link] is more common in rapid acetylates
• Peripheral neuropathy,
• CNS toxicity: restless, numbness, insomnia, muscle twitching, convulsion unpleasant
sensation
• Gastro-intestinal irritation-nausea, vomiting, diarrhea
• Blood dyscrasias
• Allergic reactions-fever, rash, SLE
Ethambutol Retrobulbar neuritis-loss of visual acuity, color blindness (red –green)
What is your advices to Pt?
And: read regularly. Nif it is difficult to read, stop the drug & consult with the physician.
Pyrazinamide • Hepatotoxicity
• Hyperuricemia-acutegouty arthritis reversible
Streptomycin • Ototoxicity-deafness, vertigo, nystagmus
• Nephrotoxicity
• Myotoxicity

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Common adverse effects of antituberculous drugs

Hypersensitivity INH more, rifampicin, ethambutol, streptomycin
Hepatotoxicity INH, rifampicin, pyrazinamide (high dose)
Optic neuritis Ethambutol, INH
Arthralgia gout Pyrazinamide, ethambutol
GIT upsets Pyrazinamide, rifampicin
Peripheral neuropathy INH, ethambutol
ototoxicity Streptomycin

Drugs used in Leprosy

 Dapsone
 Rifampicin
 Clofazimine

Q. Anti-tubercular drugs causing hepatotoxicity are (Diploma July-2019)

a) Pyrazinamide
b) Streptomycin
c) Isonicotinic acid hydrazide
d) Ethambutol
e) Rifampicin
Answer: T F T F T
Explanation:
Hepatotoxic anti-TB drug: (RIP)
 Rifampicin
 INH
 Pyrazinamide

Nephrotoxic anti-TB drug: (SR)

 Streptomycin
 Rifampicin

14. Anti-Viral Drugs

Classification of Anti-Viral Drugs (Anti-HIV drugs): The Anti-HIV drugs can be classified into
1. Nucleoside reverse transcriptase inhibitors (NRTIs):
Zidovudine, Stavudine, Lamivudine, Abacavir, Zalcitabine, Emtricitabine, Didanosine.
2. Non nucleoside reverse transcriptase inhibitors (NNRTIs):
f
Etavirenz, - Delaviridine
Nevirapine,
3. Nucleotide reverse transcriptase inhibitors (NTRTIs):
Tenofovir
o Indinavir,
4. Protease inhibitors (PIs): Saquinavir,
--
Nelfinavir, Amprenavir, Fosamprenavir,
Ritonavir, Lopinavir, Atazanavir
-

5. Entry/Fusion inhibitors:- Enfuvirtide

u
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UNRTI
-
 Systemic Pharmacology

Q. Remdesivir (Residency-2021)
a) Is a broad spectrum antiviral agent
b) Inhibits DNA dependent RNA polymerase
c) Has ability to inhibit SARS –COV-2 in vitro
d) Is highly efficacious in COVID 19
e) May shorten the time to recover from COVID-19 infection
Answer: T F T F T

15. Anti-Fungal Drugs

Classification of antifungal drugs

Systemic antifungal drugs for systemic infections
a. Amphotericin B
b. Flucytosine
Tinea
-
c. Azoies:
 Itraconazole
 Fluconazole
 Ketoconazole
 Voriconazole

d. Echinocandins
 Anidulafungin
 Caspofungin
 Micafungine

Systemic antifungal drugs for mucocutaneous infections

-
 Griseofulvin

E
 Terbinafine

Topical antifungal drugs

 Nystatin
-

 Topical azoles or imidazole (clotrimazole, miconazole)

 Ciclopiroxolamine -

 Haloprogen
 Topical allylamines (terbinafine, naftifine)
-

Side effects of fluconazole:

 Headache
 Nausa
 Vomiting
 Diarrhoea
 Abdominal discomfort
 Hepatic failure may lead to death
 It is highly teratogenic

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Go
- ~
-
-
=
- -

Q. Antifungal drugs are

a) Cotrimoxazole
b) Miconazole
c) Fluconazole
d) Clotrimazole
e) Rifampicin
Answer: F T T T F
Explanation:
a) Anti biotics
e) Anti TB

16. Anti-Protozoal Drugs

Classification Anti-Protozoal Drugs

-
Metronidazole:
Indications of Metronidazole
- Anaerobe infections

GET-
 C. difficile
--
 H. Pylori
 Bacterial vaginosis
 Trichomonas vaginitis

3 il ↓
Entameben
 Amebiasis
 Giardiasis
Adverse effect of metronidazole: -
 Metalic
-
taste
 Furred tongue, glossitis
 Nausia, vomiting, diarrhea
-
 Dizziness, headache, Vertigo, Ataxia, Numbness
 -
Peripheral neuropathy

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 Systemic Pharmacology

 Dysuria & dark urine

 Disulfiram like effect
Antimalarial Drugs:
Classification of anti malarial drugs
For clinical attack Chloroquine (first choice), Quinine
(Blood schizonticidals) s-p combination (sulfadoxine, pyrimethamine)
quinine+ tetrycycline, M-S-P combination
For radical cure Pyrimethamine,
(causal prophylaxis tissue Primaquine
schizonticidal) Proguanil
For chemoprophylaxsis Chloroquine sensitive area: chloroquine + proguanil,
Chloroquine resistant: mefloquine, malarone
Anti relapse (prevent Primaquine, proguanil,
transmission i.e. gameticides) pyrimethamine

Indication of quinine Adverse effect of quinine

• severe falciparum malaria • GIT: nausea, vomiting peptic ulcer
• chloroquine resistant • CNS disturbance: (Cinchonism)-headache, dizziness nausea,
malaria tinnitus, visual disturbance
• anti-arrhythmic agent • Haemmatological: hemolysis, agranulocaytosis, HSP
• anti-epileptic agent • Severe hypotension
• severe babesiosis • Hypoglycaemia
• Others –hypersensitivity,
• Black water fever

Q. Metronizazole (Residency-2021)
a)Is effective in both aerobic with anaerobic infection
b)Is a safe medicine in pregnancy
c)Produces disulfiram like action with alcohol
d)Causes ataxia
e)Needs nitro-reductase enzyme for reduction
Answer: F (Obligate anaerobic, not in aerobe) F T T T
Explanation:
Indication of Metronidazole:
 Amoebiasis
 Giardiasis
 Trichomoniasis
 Preparation of the colon for surgery
 After bowel surgery
 Anaerobic infections
 Genital infections
 Septicaemia, intabdominal infection
 Osteomyelitis
 Brain abscess

Adverse effects of metronidazole:

 Metallic taste in the mouth
 Glossitis

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 Nausea, vomiting arbamaz

 CNS
 Ataxia
 Dizziness
 Headache
 Vertigo
 Numbness
Peripheral neuropathy (prolonged treatment)

Cardio Pharmacology

17. Anti-Anginal Drugs

Cardiovascular pharmacology
Cardiovascular pharmacology concerns the effects of drugs on the heart, the vascular system,
and those parts of the nervous and endocrine system that participate in regulating
cardiovascular function. There are 7 classes of cardiac drugs grouped according to their
physiologic action

Inotropic Anti-arrhythmic
• Digitalis glycosides • Class I-IV anti-arrhythmic
• Sympathomimetic amines • Adenosine
• Phosphodiesterase inhibitors Diuretics
Vasodilators • Loop diuretics
• ACE inhibitors • Thiazide diuretics
• ARB • Potassium-sparing diuretics
• Direct acting vasodilators Anti-thrombotic
• Organic nitrates • Platelet inhibitors
Anti-adrenergic • Anti-coagulants
• Central adrenergic inhibitors Lipid regulating
• Sympathetic nerve ending antagonists • HMG CoA reductase inhibitors
• Peripheral alpha-R antagonists • Bile acid binding agents
• Beta-adrenergic receptor antagonists • Niacin
• Fibrates

Rationale for treating:

Increase oxygen delivery:
• Coronary vasodilators
• Anti-thrombotic drugs
Decrease oxygen demand:
• Vasodilators (reduce afterload and preload)
• Cardiac depressants (reduce heart rate and contractility)
Pharmacological agents used to treat the various form of anginal attack include:
• Nitrates (nitrodilators)
• Cardioinhibitory drugs (reduce heart rate and contractility): β-blockers, CCB
• Ranolazine (blocker of late sodium current)
• Anti-thrombotic drugs (prevent thrombus formation): Anti-platelet and anti-coagulants

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• Fibrinolytic agents (dissolve blood clots/thrombi)

• Coronary vasodilators.
Drugs used anginal pain (Ischemic heart disease- IHD):
I. Organic nitrates Mechanism of action
Glyceryl trinitrate (GTN) Reduce preload
Isosorbide dinitrate Reduce afterload
Isosorbide mononitrate Coronary vasodilation
Coronary vasodilation
Use: For acute attack and prophylaxis
II. Calcium channel blockers Mechanism of action
-Verapamil Reduce contractility
-Nifedipine Reduce afterload
-Diltiazem Coronary vasodilation
III. Beta -adrenoceptor blockers Mechanism of action
-Atenolol Reduce myocardial
-Propranolol Contractility
Decrease heart rate
IV. Dipyridamole Used as coronary vasodilator
(prophylactic use)
[Vision/7th/106-107]
New drugs or drug groups under investigation for use in angina:
Drugs
• Amiloride • Potassium channel activators e.g. Nicorandil
• Capsaicin • Protein kinase G facilitators e.g. Detanonate
• Direct bradycardic agents e.g. • Rho-kinase inhibitors e.g. Fasudil
Ivabradine • Sulfonylureas e.g. Glibenclamide
• Inhibitors of slowly inactivating sodium • Thiazolidinediones
current e.g. Ranolazine • Vasopeptidase inhibitors
• Metabolic modulators e.g. • Xanthine oxidase inhibitors e.g. Allopurinol
Trimetazidine
• Nitric oxide donors e.g. L-arginine
[Katzung/14th/207]
Pharmacological actions of GTN:
Cardiovascular effects Toxicity (Side effects)
Cardiac • Headache: Due to cerebral vasodilation

I
• Reduce preload • Flashing of face: Due to dilation of blood
• Reduce afterload vessels in the facial region
• Net effect: reduce myocardial work and • Throbbing headache: Pressing of sensory
thus reduce myocardial O2 demand nerve due to vasodilation
Systemic vasculature • Postural hypotension: Due to reduction of
• Vasodilation (venous dilation> arterial central pressure (venodilation)
dilation) • Syncopal attack
• Reduce venous and arterial pressure
Coronary vasculature
• Reflex tachycardia
• Nitrate tolerance
vasodilation
• Prevents/reverses vasospasm • Methaemoglobinaemia
• Vasodilation • Drug rash
• Improves subendocardial perfusion
• Increased O2 delivery
[Katzung/14th/191]

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Secondary prevention drug therapy of IHD:

• Anti-platelet therapy (Aspirin and/or • Additional therapy for control of
clopidogrel) diabetes and hypertension
• Β-blocker • Mineralocorticoid receptor antagonist:
• ACE inhibitor/ARB Spironolactone or eplerenone.
• Statin

Q. Drug to be given within 6 hours of myocardial infarction-

a) Aspirin
b) Metoprolol
c) Streptokinase
d) Diltiazem
e) Statin
Answer: T F T F T

Q. β-blockers exert anti-anginal effect by- [MS/Basic- March’16]

a) Decreasing cardiac contractility
b) Increasing coronary blood flow
c) Decreasing heart rate in tachycardia
d) Decreasing preload
e) Decreasing afterload
Answer: T F T F F

Q. Nitroglycerine in angina pectoris- [MD/MS/Basic- March’15]

a) Decreases preload
b) Decreases afterload
c) Decreases heart rate
d) Increases myocardial contractility
e) Increases coronary collateral circulation
Answer: T T F F T

Q. Vasodilation due to nitroglycerine causes- [MS/Basic- March’16]

a) Hypotension
b) Tachycardia
c) Nitrate tolerance
d) Headache
e) Methaemoglobinaemia
Answer: T T F T F

Q. Drugs used in secondary prevention of IHD- [MPhil/Diploma- July’12]

a) Aspirin
b) Verapamil
c) Statins
d) Fibrates
e) Nitrates
Answer: T F T F F

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18. Drugs Used in Heart Failure

Basic pathology of heart failure: The heart is unable to pump blood around the body to meet its
metabolic needs due to-
 Increase cardiac preload and afterload
 Decrease myocardial contractility
 Increase heart rate.

⑧ Drugs used to treat heart failure

Renin-angiotensin system
blockers
β-blockers
-
• Atenolol
Inotropic agents
-
• Amrinone
ACE inhibitors • Carvedilol • Digoxin, Digitoxin
- • Captopril • Metoprolol • Dopamine, Dobutamine
• Enalapril • Milrinone
• Fosinopril Diuretics
• Lisinopril - • Bumetanide Aldosterone antagonists
• Quinapril • Frusemide • Spironolactone
• Ramipril • Metochlorothizide
ARB • Metolazone
- • Olmesartan
• Candesartan Direct vasodilators
• Losartan • Hydralazine
• Telmisartan • Isosorbide dinitrate
• Valsartan • Sodium nitroprusside

Therapies used in heart failure

Chronic heart failure Acute heart failure
 Diuretics  Diuretics
 Aldosterone receptor antagonists  Vasodilators
 Angiotensin converting enzyme inhibitors  Beta-agonists
 Angiotensin receptor blockers  Bipyridines
 Beta blockers  Natriuretic peptide
 Cardiac glycosides  Left ventricular assist device
 Vasodilators, neprilysin inhibitor
 Resynchronization and cardioverter therapy

Drugs used in heart failure:

• Those reduce preload: Diuretics, nitrate- GTN,
• Those reduce afterload: Vasodilators Hydralizins, Diazoxide, Minoxidil, Sodium
nitroprusid
• Those reduce both preload and afterload: Nitrate, ACEi, ARB, β Blocker, Spironolactone
• Those increase contractility: Cardiac glycosides, β-agonists, Milrinon
• Those decrease HR: Selective β1 blockers and both α & β receptor blocker.
[Katzung/14th/224]

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Differences between in systolic and diastolic heart failure

Variable or therapy Systolic heart failure Diastolic heart failure
Cardiac output Decreased Decreased
Ejection fraction Decreased Normal
Diuretics ↓Symptoms; first-line therapy if Use with caution
edema present
ACEIs ↓Mortality in chronic HF May help to ↓LVH
ARBs ↓Mortality in chronic HF May be beneficial
ARNI ↓Symptoms and NT-proBNP ↓Symptoms and NT-proBNP
Aldosterone inhibitors ↓Mortality in chronic HF May be useful
Beta-blockers - ↓Mortality in chronic HF Useful to ↓HR,↓BP
Ivabradine- Reduces hospitalizations
Calcium channel blockers No or small benefit Useful to ↓HR,↓BP
Digoxin May reduce symptoms Little or no role
Nitrates May be useful in acute HF Use with caution
PDE inhibitors May be useful in acute HF Very small study in chronic HF was
positive
Positive inotropes ↓Symptoms, hospitalizations Not recommended

Cardiotonic agents
Cardiac glycosides (Digitalis) • From leaves of foxglove:
1. Digitalis purpura: Digoxin, digitoxin
2. Digitalis lanata: Digoxin, lanatoside-C
• From seeds of foxglove: Ouabin

Sympathomimetic agents Dobutamine

Dopamine
Adrenaline
Isoprenaline
Xemoterol
Phosphodiesterase inhibitors Inamrinone
Milrinone
Calcium sensitizers Levosimendin

Effects of digitalis in heart failure

• Positive inotropic action
• Increased cardiac output
• Decreased heart rate
• Decreased venous pressure
• Diuresis and relief of edema
• Negative chronotropic action
• Slow the ventricular rate in atrial fibrillation and flutter

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Digoxin
Mechanism of action of digoxin:
Cardiac glycosides (digoxin)
↓
Inhibition of Na++-K+-ATPase enzyme
(Glycosides bind with K+ binding site of the enzyme)
↓
Decrease Na+ - k+ pump
↓
Decrease RMP Increase intracellular Na+ K+ flows out of cell
↓ ↓ ↓
Increase excitability Inhibit Na+/ Ca++ exchange Slowing of AV conduction
↓
Increase intracellular Ca++
↓
Arrhythmia Interaction of actin & myosin Bradycardia
↓ Heart block
Increase cardiac contractility
↓
Decrease heart size

Indications:
CCF (ischaemic, hypertensive or vulvular Benefiting by increasing the myocardial contractility
disease)
Atrial fibrillation Benefiting by reducing AV conduction
Atrial flutter Benefiting by shortening atrial refractory period
Paroxysmal supraventricular tachycardia Benefiting by the vagal effect on SA node
Left ventricular failure By increasing myocardial contractility

Adverse effects /Toxicities of Digoxin

A cardiac:
[Link]
2. arrhythmias:
a) ventricular arrhythmias:
• ventricular premature ectopic beat
• ventricular tachycardia
• ventricular fibrillation due to hypoalaemia
b) atrial arrhythmia paroxysmal atrial tachycardia
3. A-V heart block
B Extra-cardiac
1. GIT: anorexia, nausea, vomiting, diarrhea
2. CNS: headache, drowsiness, insomnia, dis-orientation, hallucination, depression
3. eye
• Blurring of vision
• Photophobia
• Diplopia
• Disturbance in perception of color

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4. Miscellaneous:
• Skin rash
• Hypokalemia
• Gyneacomastia
• eosinophilia
Adverse effects of cardiac glycosides (Digoxin):
Cardiac side effects Extra-cardiac side effects
Toxic effects PR interval prolongation • GIT: Anorexia, nausea, vomiting, feeding
Sinus bradycardia or SA block intolerance, diarrhea, pain
Atrial or nodal ectopic beats • CNS: Headache, drowsiness, insomnia,
Ventricular arrhythmias: fatigue, weakness, neuralgia, paraesthesia,
I. Ventricular ectopic beat depression, confusion, hallucination
II. Ventricular tachycardia • Eye: Blurring of vision, photophobia, diplopia,
III. Ventricular fibrillation disturbance of color vision
due to hypokalemia. • Miscellaneous: Skin rash, hypokalemia,
Non-toxic QT interval shortening gynaecomastia and eosinophilia.
effects ST segment sagging
T-wave amplitude damping
Heart rate slowing
[Vision/7th/136]
Factors aggravate Digoxin Toxicity
Condition Effect
Hypercalcemia Increased intracellular calcium already exists
Hyperkalemia Increases conduction delay
Hypokalemia Inhibits Na+, K+ -ATPase pump, exacerbates pump inhibition
action of digoxin
Hypomagnesemia Increases digoxin uptake by myocardium
Renal insufficiency Primary route of digoxin excretion

Drugs having mortality benefit in heart failure:

[According to latest guideline 2021]
 Spironolactone
 ACE Inhibitor
 Beta blocker
 ARB
 Nprilysin inhibitor
 SGLT2 inhibitor [Newly added in guideline]
 Cardiac Devices

Q. Drugs reducing preload on the heart are- [MPhil/Diploma- July’15]

a) GTN
b) Sodium nitroprusside
c) Lisinopril
d) Hydralazine
e) Minoxidil
Answer: T T T F F

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Q. Drugs increasing survival of patients with heart failure are-

a) Frusemide
b) Carvedilol
c) Milrinone
d) Digoxin
e) ACEi
Answer: F T F F T

Q. Digoxin toxicity includes- [MD/MS/Basic- March’16]

a) Altered color vision
b) Bradycardia
c) Constipation
d) Atrial fibrillation
e) Ventricular tachycardia
Answer: T T F F T

Q. An increase in heart rate occurs following the therapeutic use of-[MS March’13]
a) Atropine
b) Digoxin
c) Dopamine
d) Isoprenaline
e) Sotalol
Answer: T F T T F

Q. The beneficial effects of digoxin in congestive cardiac failure are- [MS/Basic-

March’16]
a) Increased force of myocardial contractility
b) Reduction in preload
c) Reduction in afterload
d) Slowing of AV nodal conduction
e) Increased myocardial automaticity
Answer: T F F T F

Q. Inotropic drugs to be used for compromised cardiac function are-

[MPhil/Diploma- July’12]
a) Dopamine
b) Noradrenaline
c) Digoxin
d) Adrenaline
e) Ephedrine
Answer: T F T T T

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19. Anti-Arrhythmic Drug

Traditionally, the Vaughan Williams system has been used to categorise anti-arrhythmic drugs
based on their effects on the action potential.
Classification of anti-arrhythmic drugs by effect on the intracellular action potential
-
Class I: Membrane stabilising agents (sodium channel blockers)
• Block Na+ channel and prolong action potential
• Quinidine, disopyramide
• Block Na+ channel and shorten action potential
• Lidocaine, mexiletine
-

• Block Na+ channel with no effect on action potential

• Flecainide, propafenone
Class II: β-adrenoceptor antagonists (β-blockers)
-
• Atenolol, bisoprolol, metoprolol
6 Class III: Drugs whose main effect is to prolong the action potential >
- kt
•- Amiodarone, dronedarone, - Sotalol
& Class IV: Slow calcium channel blockers
• Verapamil, diltiazem- Cartio eB
-

*Some drugs such as digoxin, ivabradin and adenosine have no place in this classification, while
others such as amiodarone have properties in more than one class.
[Davidson/23rd/479]
Adverse effects of amioderone: Vaso


Blueman syndrome
Interstitial lung disease
-
 Bradycardia
 Tremor
 Photophobia
 Muscle weakness
 Hepatotoxicity
 Corneal deposit
 Thyroid dysfunction
Mnemonics
6Ps
 Prolongs action potential duration
 Photosensitivity
 Pigmentation of skin
 Peripheral neuropathy
 Pulmonary alveolitis and fibrosis
 Peripheral conversion of T4 to T3 is inhibited ->hypothyroidism
Q. The anti-arrhythmic property of the following drugs is due to blockade of the Na+
channels-
a) Sotalol
b) Verapamil
c) Lidocaine
d) Quinidine
e) Amiodarone
Answer: F F T T T

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Q. Following are the adverse effects of amiodarone- [Non-residency- 07]

a) Myocardial depression
b) Corneal deposits
c) Alveolitis
d) Nystigmus
e) Torsades de pointes
Answer: F T T F T

20. Antihypertensive Agents

Vasodilators:
• Alpha-blockers
• ACE inhibitors -
•-
-

ARB - -
RAAS
• Angiotensin II inhibitors
Am blocker
Alpha
• Calcium
- channel blockers
• Directly acting arterial dilators
• Ganglionic blockers
• Nitrodilators
• Potassium channel openers
• Renin inhibitors Betabled
Angiotensin converting enzyme inhibitors (ACE inhibitors):
• O
Captopril • Quinapril
-

• Enalapril
- • Ramipril
• Fosinopril • Benazepril
• Lisinopril • Trandolapril

Pharmacological actions of ACE inhibitors Cardiorenal effects of ACE inhibitors

 Vasodilation (reduction of peripheral resistance) • Vasodilation (arterial and venous)
 Reduce preload and afterload (used in CCF)  Reduce arterial and venous pressure
 Reduction of aldosterone secretion; so, reduce  Reduce ventricular preload and afterload
salt and water retention • Decrease blood volume
 Desirable increase in renal blood flow  Natriuretic
 Prevents the breakdown of bradykinin  Diuretic
• Depress sympathetic activity
• Inhibit cardiac and vascular hypertrophy

Indications of ACE inhibitors Contraindications of ACE inhibitors

1. Hypertension: 1. Systolic blood pressure <100 mmHg
 Moderate to severe hypertension 2. Bilateral renal artery stenosis
 Renovascular hypertension 3. Second and third trimester of pregnancy
4. Renal failure.
 Malignant hypertension
 Hypertensive crisis of scleroderma
(AkI)
 Dialysis resistance hypertension in end stage
renal failure
2. Refractory heart failure (CCF)
3. Ischaemic heart disease
4. Protect against renal vascular injury in DM by-
 Improving intrarenal perfusion
 Diminishing proteinuria
 Reducing efferent arteriolar resistance and thus
reducing intaglomerular capillary pressure.

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Adverse effects of ACE inhibitors:

• First dose hypotension
• Dry cough
• Angioneurotic edema
• Hyperkalaemia
• Loss of appetite
• Stomatitis
• Abdominal pain
• Neutropenia
• Proteinuria
• Blood disorder

Angiotensin receptor blockers (ARBs):

• Losartan • Candesartan
• Irbesartan • Telmisartan
• Olmesartan • Tasosartan
• Valsartan • Eprosartan

• ARBs block the actions, not the formation of angiotensin II. Blockage of AT1 receptors directly
causes vasodilation, reduces secretion of vasopressin, and reduces production and secretion
of aldosterone, among other action. The combined effect reduces blood pressure.
• They inhibit cardiac and vascular remodeling associated with chronic hypertension, heart
failure and myocardial infarction.
• As they do not inhibit the breakdown of bradykinin, they do not cause dry cough.
• They have similar physiological effects to ACE inhibitors and produce similar falls in blood
pressure.
• There is synergism of antihypertensive effect with thiazide diuretics.
• They may regresses left ventricular hypertrophy and proteinuria.
• The main advantage of the ARBs is their apparent lack of side effects (e.g. dry cough,
angioedema) like the ACE inhibitors.

Therapeutic uses:
• Hypertension
• Heart failure
• Post myocardial infarction

Adverse effects:
• Orthostatic hypotension
• Dizziness and headache
• Hyperkalaemia
• Dyspepsia
• Myalgia and muscle cramps
• Contraindication: Pregnancy, bilateral renal artery stenosis.

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Category Calcium channel blocker:

On the basis of chemical structures: On the basis of clinical uses:
I. Dihydropyridine family: smooth muscle Antianginal:
selective
• Nifedipine • Amlodipine • Amlodipine • Nifedipine
• Nicardipine • Isradipine • Isradipine • Verapamil
• Nimodipine • Felodipine • Felodipine • Diltiazem
• Nisoldipine • Mibefradil • Nicardipine • Bepridil

II. Non- dihydropyridines: Antiarrhythmic: Diltiazem, verapamil

• Verapamil: myocardium selective Antihypertensive:
• Diltiazem: intermediate between • Amlodipine • Nifedipine
verapamil & dihydropyridines in its • Isradipine • Verapamil
selectivity for vascular calcium channel • Felodipine • Diltiazem
• Nicardipine
Subarachnoid hemorrhage therapy:
• Nicardipine
• Nimodipine
• Flunarizine
Vascular headache (migraine) prophylactic:
• Flunarizine
• Verapamil
III. Miscellaneous: Bepridil. Hypertrophic cardiomyopathy therapy
adjunct:
• Verapamil

Pharmacological action of calcium channel blockers:

A. On CVS:
• Coronary vasodilation: improve myocardial perfusion
• Negative chronotropic action: cardiac slowing and AV block
• Negative inotropic action: decrease force of contraction
• Vasodilation: decrease total peripheral resistance
So, main action:
• Increase myocardial oxygen delivery (antianginal)
• Decrease blood pressure (antihypertensive)
B. On smooth muscle:
• Vascular smooth muscle: generalized vasodilation; so reduce afterload
• Coronary vasodilation: antianginal action
• Visceral smooth muscle: relaxation of biliary tract, uterus and bladder.
CCBs cause vasodilation of the arterial vascular bed, thus reduce afterload. But CCBs have
minimal effect on venous bed and thus have little effect on preload.
Indications of CCBs:
• Angina pectoris (variant) (ischaemic heart disease)
• Hypertension (systemic and pulmonary)
• Congestive heart failure
• Cardiac arrhythmia

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• Raynaud’s disease
• Prevention of ischaemic neurological damage following SAH (heart attacks, stroke)
• Migraine prophylaxis
• Subarachnoid and intraventricular hemorrhage (nimodipine)

Adverse effects of CCBs: Contraindications of CCBs:

I. Due to vasodilation: II. GIT side effects: • Heart failure
• Postural hypotension • Constipation • Where there is bradycardia
• Reflex tachycardia • Nausea • 2nd or 3rd degree AV block
• Bradycardia • Vomiting • Sick sinus syndrome
• Palpitation • Gum hypertrophy • Wolf-parkinson-white syndrome.
• Headache (Nifedipine)
• Flushing, dizziness
• Ankle edema
[Vision/7th/112]

000
HER NEW LAB METHOD DONE

& Medication
Labetalol
-
Mechanism of action
α and β blocker
Nifedipine, amlodipine Calcium channel blocker
=
Methyldopa Central action
Doxazosin Α-receptor blocker

O
-

Other: Hydralizine, Prazosine, Clonidine

[Davidson/23rd/1276]

Drug causing hypertension: Drugs causing postural hypotension:

• Corticosteroid • Reserpine
• Oral contraceptives • Prazosin, terazosin, oxazosin
• NSAIDs • Sodium nitroprusside
• MAOi with sympathomimetic agents • ACEi/ARB
• Clonidine and methyldopa withdrawal • CCBs
• Leflunamide • Morphine, nicotine
• Cyclosporine • Phenoxybenzamine
• Nitrates, guanethidine
• Chlorpromazine, TCA
• MAOi, L-dopa, Ergolines

Q. Drugs used for the management of hypertension in pregnancy are-

[MD/MS/Basic/ Paedi- March’19, 17, MPhil/Diploma- July’17]
a) Hydrochlorothiazide
b) Atenolol
c) Labetalol
d) Captopril
e) α-methyldopa
Answer: F F T F T

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Q. The antihypertensive drugs that lower diastolic blood pressure by inhibiting renin
angiotensin system are- [MPhil/Diploma- July’13]
a) Losartan
b) Amlodipine
c) Hydralazine
d) Ramipril
e) Atenolol
Answer: T F F T F

Q. The antihypertensive drugs that commonly cause postural hypotension are-

[MPhil/ Diploma- July’12]
a) Lisinopril
b) Prazosin
c) Amlodipine
d) Losartan
e) Carvedilol
Answer: T T T T F
Q. Hypertension is a recognized complication in the use of following drugs-
[MPhil/Diploma- March’10]
a) Oral contraceptives
b) Anti-inflammatory steroids
c) Adrenergic nerve blockers
d) Beta-blockers
e) TCA
Answer: T T F F F
Q. Following drugs produce reflex tachycardia- [Jan-10]
a) Noradrenalin
b) Atenolol
c) Dopamine
d) GTN
e) Phenoxybenzamine
Answer: F F T T T
Q. Regarding ACE inhibitors- [MD/MS/Basic- March’17]
a) Drug of choice in CCF
b) Increase preload and afterload of heart
c) May cause dry cough
d) Drug of choice in HTN with COPD
e) Contraindicated in pregnancy
Answer: T F T F T
Q. Angiotensin converting enzyme inhibitors- [MS/Basic- March’16]
a) Decrease cardiac output significantly
b) Reduce preload
c) Reduce afterload
d) Decrease bradykinin
e) Are not teratogenic
Answer: F T T F F

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Q. ACE inhibitors are absolutely contraindicated in- [MD/Basic- March’15]

a) End stage renal disease
b) Pregnancy
c) Acute heart failure
d) Asthma
e) Bilateral renal artery stenosis
Answer: T T F F T
Q. The mechanism of antihypertensive action of Ca++channel blockers involve-
[MD/MS - Jan’10]
a) Decrease cardiac output
b) Anti-renin activity
c) Decrease peripheral resistance
d) Increase bradykinin activity
e) Decrease aldosterone activity
Answer: T F T F F

21. Lipid Lowering Agents

Type Reduce Reduce Reduce LDL Rise HDL

cholesterol TG
HMG-co A reeducates inhibitor: + Up to 40% Up to 60% Up to 10%
Statins
Fibric acid derivatives: Fibrates No Up to 50% Variable Up to 20%
Bile acid sequestrants: + May rise + +
cholestyramine
Cholesterol absorption inhibitor: + No No No
Ezetemibe
Nicotinic acid derivatives: Niacin + + + +
PUFA (long chain W-3 FA) fish oil. No +up to Variable
50%

Statins:
• Atorvastatin
• Lovastatin
• Simvastatin
• Rosuvastatin
Indications:
• Primary hypercholesterolemia and mixed dyslipidemia
• Hypertriglyceridemia
• Homozygous familial hypercholesterolemia
Adverse effects:
• Headache, dizziness
• Diarrhea, flatulence
• LFT abnormality
• Myalgia, myopathy, rhabdomyolysis and
• Asymptomatic rise in CPK.

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Fibrates:
• Gemfibrozil,
• Bezafibrate,
• Fenofibrate,
• Beclofibrates,
• Ciprofibrates.
Adverse effects:
 Myalgia,
 Myopathy,
 LFT abnormality,
 Cholelithiasis &
 prolong anticoagulant action

***Monitoring of therapy by lipid response

 CPK & LFT, done after 6wks for statins & 12wks for fibrates.
 Stop therapy if CK if elevated with symptoms (>5-10 times), ALT>2-3 time.
[Vision/7th/428]

Q. Simvastatin (Residency March 2022)

a) Lowers LDL cholesterol
b) Acts by stimulating HMG co A reductase
c) Is associated with rhabdomyalisis
d) Reduces creatinine kinase
e) Can be used safely in pregnency
Answer: T F T F F

Blood Pharmacology
22. Anti-Platelet Drugs
Drugs in blood disorder
Modes of action of anticoagulant and antithrombotic drugs
Mode of action Drug
Antiplatelet drugs
Cyclo-oxygenase (COX) inhibition Aspirin
Adenosine diphosphate (ADP) receptor Clopidogrel
inhibition Prasugrel
Ticagrelor
Glycoprotein IIb/IIIa inhibition Abciximab
-

Tirofiban
Eptifibatide
Phosphodiesterase inhibition ⑤ Dipyridamole
Oral anticoagulants
Vitamin K antagonism
-
⑧
Warfarin/coumarins
Direct thrombin inhibition Dabigatran

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-
Direct Xa inhibition Rivaroxaban
Apixaban
Edoxaban
Injectable6
anticoagulants
Antithrombin-dependent inhibition of
On
thrombin and Xa
Heparin

Antithrombin-dependent inhibition of Xa
O LMWH -
Fondaparinux
Danaparoid
Direct thrombin inhibition Argatroban
Bivalirudin

Aspirin:
Aspirin is now rarely used as an anti- inflammatory medication and used only for its anti-platelet
effects (doses of 81-325 mg once daily). Aspirin is absorbed from stomach & upper part of small
intestine, rapidly hydrolyzed to acetic acid and salicylate by esterases in tissue and blood. Salicylate
is bound to albumin. Alkalinization of the urine increases the rate of excretion of free salicylate and
its water soluble conjugates.

Mechanisms of action:
Aspirin irreversibly inhibits platelet activation by inhibiting COX enzyme. This prevents the synthesis
of thromboxane A2 which normally causes platelet aggregation. The anti-platelet effect of aspirin
lasts 8-10days, the lifespan of the platelet.

Clinical uses:
Aspirin decreases the incidence of transient ischemic attacks, unstable angina, coronary artery
thrombosis with myocardial infarction, and thrombosis after coronary artery bypass grafting.
Epidemiologic studies suggest that long term use of aspirin at low dosage is associated with a loser
incidence of colon cancer, possibly related to its COX inhibiting effects.

***Although previously not recommended during pregnancy, aspirin may be valuable in treating
pre-eclampsia.

Adverse effects:
• Gastric and duodenal ulceration
• Impaired clotting
• Hepatic and renal damage
• Tinnitus, deafness
• Reye’s syndrome
• Allergic menifestations (rhinitis, urticaria, angioedema)

-
Q. Anti-platelet drugs include- [MD/MS/Basic- March’17]
a) Clopidogrel

# **
b) Streptokinase
c) Enoxaparin
d) Low dose aspirin
- e) Abciximab
Answer: T F F T T

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Q. Low dose aspirin- [MD/MS/Basic- March’12]

a) Has anti-inflammatory effect
b) Prolongs Prothrombin time
c) Is indicated in arrhythmic patients
d) Inhibits prostacycline synthesis
e) Inhibit the enzyme thromboxane A2
Answer: F F F F F

Q. Pharmacological effects of aspirin include- [MD/MS/Basic- March’15]

a) Vasodilatation
b) Chemotaxis
c) Phagocytosis
d) Leukocyte migration
e) Inhibition of COX enzyme
Answer: F F F F T
[Vision/7th/421]

23. Anti-Coagulants

Natural anti-coagulants: Anti thrombin-III, protein- C, protein-S, heparin sulfate, α2 macroglobulin,

α1-antitrypsin, α1-antiplasmin.

Classification of anti-coagulant agents

Anticoagulants acting in 1st group 2nd group
vitro Citrate, oxalate, EDTA Heparin, dextran sulfate
Anticoagulants acting in Coumarin derivatives: Dicoumarol, warfarin
vivo Indandione derivatives: Phenindione
Acting in both vivo and Heparin, dextran sulfate, anchord
vitro
According to mechanism of Directly acting: Heparin, dextran sulfate
action Indirectly acting: Coumarin derivatives, Indandione derivatives
According to routes of Injectable: Heparin, anchord, hirudin, bivalirudin, lepirudin,
administration agatroban
Oral: Warfarin, dicoumarol

Heparin:
• First obtained from liver.
• Highly acidic, negatively charge.
• Source: Mast cell, basophil.
• Heparin potentiates the action of anti-thrombin III, which inhibits thrombin (IIa) and Xa, IXa,
XIa, XIIa; therefore prevent coagulation.
• Protamine-S04 and toluidine blue are heparin antagonists.
• Heparin action should be monitored by APTT.
• Common adverse effects of heparin are thrombocytopenia, osteoporosis, alopecia.
• LMWH have greater activity against Xa but less effect on thrombin, long duration of action &
requires no monitoring, so suitable for home treatment.
• LMWH includes enoxaparin, dalteparin, tinzaparin, danaparoid.
• Not contraindicated in pregnancy.

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Unfranctioned heparin Low molecular weight heparin

• Associated with more adverse effects • Associated with less adverse effects
• Monitoring required with APTT • Monitoring is not required with APTT
• Heparin induced thrombocytopenia- • Thrombocytopenia is less common
common • Less chance of bleeding
• More chance of bleeding • Bioavailability 90%
• Bioavailability 20% • Can be given in hospital & OPD setting
• Should be given in hospital setting • Anticoagulant response is predictable
• Anticoagulant responds is • No antidote is needed
unpredictable
• Protamine is an antidote

Adverse effects:
• Alopecia
• Bleeding complications
• Hypersensitivity reactions: heparin preparations are obtained from porcine source and,
therefore may be antigenic. Possible adverse reactions include chills, fever, urticaria or
anaphylactic shock
• Thrombocytopenia
• Abnormal liver functions tests
• Osteoporosis on long term heparin therapy

Contraindication: Heparin is contraindicated for patients who are hypersensitive to it, have
bleeding disorder, are alcoholics or are having or have had recent surgery of the brain, eye or spinal
cord, and any form of bleeding.

O Warfarin:
• Warfarin is Coumarin derivative. &
Extrin PENR
• Warfarin has the structural similarity of vit-K. It is vit-K antagonist.
-
.

• Warfarin competitively inhibits the enzyme vit-K epoxide reductase, thus inhibits the synthesis
&
of vit-K dependent clotting factor (II, VII, IX, X).
• Warfarin is rapidly absorbed after oral administration (100% bioavailability with little
individual patient variation). Although food may delay absorption.
• Warfarin is 99 percent bound to plasma albumin, which prevents its diffusion into the
& cerebrospinal fluid, urine, and breast milk.

Hep • However, drugs that have a greater affinity for the albumin binding site, such as sulfonamides,
can displace the anticoagulant and lead to a transient, elevated activity.
• Warfarin readily crosses the placental barrier. It is teratogenic.

a
• Its onset of action is delayed.
• The mean half life of warfarin is approximately 40 hours, but this value is highly variable among
individuals.
• Prothrombin time, a measure of the extrinsic pathway, may be used to monitor warfarin
therapy. The result is reported as international normalized ratio (INR). Normal INR is 1. In
warfarin therapy, INR should increase to 2.5-3.5.
 INR <2.5: dose of warfarin should be increased
 INR >3.5: drugs to be stopped.
Fate: The products of warfarin metabolism, catalyzed by the cytochrome P 450 system, are inactive.
After conjugation to glucuronic acid, they are excreted in the urine and stool.

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Therapeutic uses:
Warfarin is used to prevent the progression or recurrence of acute deep vein thrombosis or
pulmonary embolism after initial heparin treatment. It is also used for the prevention of venous
thromboembolism during orthopaedic or gynecologic surgery. Prophylactically, it is used in patients
with acute myocardial infarction, prosthetic heart valves, or chronic atrial fibrillation.

Adverse effects:
• Bleeding disorders- treated by withdrawal of the drug and administration of oral vitamin K1;
severe bleeding requires that greater doses of the vitamin be given intravenously. Whole blood,
frozen plasma, or plasma concentrates of the blood factors may also be employed to arrest
hemorrhaging.
• Skin lesions and necrosis are rare complications of warfarin therapy and are observed primarily
in women.
• Purple toe syndrome, a painful, blue-tinged discoloration of the toe caused by cholesterol emboli
from plaques, has also been observed with warfarin therapy.

Contraindications:
• Recent trauma, injury
• Active internal bleeding
• Severe hypertension
• Non-thromboembolic stroke
• Major surgery
• Pre-existing hemostatic defects
• Pregnancy as it is teratogenic
• Lactating mother
• Threatened abortion
• Severe liver and renal disease
• Hypoprothrombinemia.

Drug interaction Warfarin:

Warfarin- therapeutic failure occurs with Warfarin- toxicity occurs with concomitant use
concomitant use of/ following conditions- of/following conditions-
• Barbiturates • NSAIDs
• Phenytoin • Oral hypoglycaemics
• Rifampicin • Metronidazole
• Carbamazepine • Cotrimoxazole
• Griseofulvin • Ampicillin
• Oral contraceptives • Cephalosporins
• Vitamin K • Erythromycin
• Cholestyramine • Clofibrate
• Nephritic syndrome • Salicylates
• Also: hypothyroidism. • Chloramphenicol
• Alcohol (acute)
• Phenylbutazone
• Cimetidine
• Amiodarone
• Salicylates (high dose)
• Broad-spectrum antibiotics (neomycin)
• Also: age, biliary disease, congestive heart failure,
hyperthyroidism.

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Difference between heparin & warfarin/dicoumarol:

Points Heparin Warfarin
Sources Animal Plant
Acts in Vivo and vitro Only in vivo
Route of administration Injectable Oral /injectable
Onset of action Immediate (10-18 min of Delayed (36 – 48 hr of
administration) administration)
Duration of action 4-6 hours 2-6 days
Dose Bolus infusion followed by Small daily doses
continuous drip
Anticoagulant action Directly acting Indirectly acting
Adverse effect
Hypersensitivity ++ -
Osteoporosis ++ -
Alopecia ++ -
Teratogenicity Cannot cross the placenta Can cross the placenta
No teratogenicity So teratogenic
Antidote Protamine sulfate Vitamin K1, Whole blood
Toluidine blue Transfusion
[Vision/7th/402]

Fibrinolytic drugs

Fibrinolytic agents are:

Streptokinase
Anistreptase
Tissue plasminogen activator [tPA] family
• Alteplase
• Retaplase
• Tenecteplase
Recombinant prourokinase
Urokinase
First generation agent: Streptokinase
Second generation agent: Alteplase
Third generation agent: Retaplase

Indication of fibrinolytic agents Adverse effect of fibrinolytic agents

• Acute deep vein thrombosis • Hemorrhage
• Acute pulmonary embolism • Hypotension
• Acute myocardial infarction • Allergic reaction
• Arterial thromboembolism • Anaphylaxis
• Acute ischaemic stroke • Cardiac arrhythmia
[Vision/7th/416]

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Anti-fibrinolytics

Anti-fibrinolytic drugs:
• Aminocaproic acid (EACA): It acts by blocking of the binding of plasmin to target fibrin.
• Tranexamic acid-It acts by inhibition of plasminogen activator.
• Aprotinin
• Phytomonadion
• Ethamsylate

Indication of anti-fibrinolytic drugs:

 Treatment of upper GIT bleeding
 Haemorrhage after prostatic surgery
 Disseminated intravascular coagulation
 Acute pancreatitis
 Menorrhagia
Q. Heparin- [MD/MS/Basic- March’15]
a) Can be given sublingually
b) Acidic in nature
c) Antagonized by vit K
d) Better than LMWH
e) Used in emergency
Answer: F T F F T

Q. Heparin- [MD/MS- March’14]

a) Is a strongly negatively charged organic acid
b) Acts by inhibiting the enzyme epoxide reductase
c) Toxicity is antagonized by Protamine sulfate
d) Is obtained synthetically from laboratory source
e) Therapy is monitored by APTT
Answer: T F T T T

Q. Recognized adverse effects of heparin- [MS- March’16]

a) Osteoporosis
b) Diarrhea
c) Alopecia
d) Thrombocytopenia
e) Fetal anomalies
Answer: T F T T F
Q. Indications of warfarin includes- [MS/Basic- March’14]
a) Venous thromboembolism
b) Arterial embolism
c) Myocardial infarction
d) Atrial fibrillation
e) Mechanical prosthetic heart valves
Answer: T T T T T

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Q. Followings are anticoagulants- [MPhil/Diploma- July’15]

a) Enoxaparin
b) Warfarin
c) Aspirin
d) Clopidogrel
e) Unfractionated heparin
Answer: T T F F T
Q. Thrombolytic agents are- [MPhil/Diploma- July’14]
a) Streptokinase
b) Urokinase
c) Aspirin
d) Clopidogrel
e) Warfarin
Answer: T T F F F
Q. Anti-fibrinolytic drugs include- [MD/MS- March’12]
a) Heparin
b) Aprotinin
c) Tranexamic acid
d) Desmopressin
e) Warfarin
Answer: F T T F F

24. Hematinics
Hematinic: Iron, Vit-B12, Folic acid, Hematopoeitic growth factor.
Iron:
• Iron is absorbed from duodenum and upper jejunum in ferrous form
• Vit C increases Fe absorption and phosphate food decreases.
Indication of iron therapy:
• Iron deficiency anemia
• Prophylactic uses: Pregnancy, menstruation, early infancy, blood donors
• Chronic blood loss
• Glossitis, stomatitis.
• Iron dextran & sorbitol are the parenteral iron preparation out of which dextran is suitable
for TDI
• GI upset in the commonest adverse effect.
• Desferrioxamine is chelating agent.
Vitamin B 1 2 :
• Site of absorption: Distal ileum
• Site of store: Liver
• Effects of deficiency: Megaloblastic anemia & neural tube defect
• Indication of administration: Pernicious anemia & other causes of deficiency, after total
gastrectomy.
Folic acid:
• Folic acid is absorbed from proximal jejunum. Principally stored in the liver.
• Deficiency leads to megaloblastic anemia & neural tube defect.
[Vision/7th/394]

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Renal Pharmacology
25. Diuretics
Classification of diuretics according to site of action:

O
Site-I: (PCT) Osmotic diuretics:
-
 Mannitol, lsosorbide, Urea
Carbonic anhydrase inhibitors:
=  Acetazolamide
 Ethoxzolamide
 Methozolamide
 Dorzolamide
-
 Topiramate

00
Site-II: ALLH
-
High ceiling diuretics (Excrete 15-25% of filtered Na+)
 Frusemide

E
3
 Torsemide
 Bumetanide
 Piretanide
-

 Ethacrynic acid

O
-
Site-III: DCT Moderate
-
efficacy diuretics (Excrete 5-10% of filtered Na+)

Nate
 Thiazides and related diuretics:
--
 Chlorothiazide
 Hydrochlorothiazide
-

E -
 Trichlomethiazide
 Chlorthalidone
 Quinethazone
 Metolazone
 Indapamide
O
Site-IV: CDs K+ sparing/low efficacy diuretics (Excrete <5% of filtered Na+)
-

 Aldosterone antagonists: Spironolactone, Eplerenone

= ①I
 Epithelial Na- channel blocker: Amiloride, triamterene

Mechanism of action:

Loop diuretics: Inhibition of NaCl reabsorption in the thick ascending limb of the loop of Henle by
inhibiting the Na+-K+-2CI− co-transport (symport) system in the luminal membrane.
Thiazides: Inhibit NaCl reabsorption by inhibiting Na+-CI− transport at the DCT.
Potassium-sparing diuretics: Inhibit the effects of aldosterone at the cortical collecting tubule and
late distal tubule.

Osmotic diuretics: Cause water to be retained within the proximal tubule and descending limb of
loop of Henle.

Carbonic anhydrase inhibitors: Blockade of carbonic anhydrase activity - decreases sodium

bicarbonate reabsorption from PCT, cause diuresis.

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Indications of diuretics
Loop diuretics Thiazide diuretics K+ sparring diuretics
Congestive cardiac failure Congestive cardiac Given with K+ losing diuretics in the
Acute pulmonary edema failure management of HTN.
Moderate hypertension Hypertension Management of refractory edema
Management of edema (e.g. liver Nephrogenic Primary aldosteronism
cirrhosis, nephrotic syndrome) diabetes insipidus Secondary aldosteronism due to-
Oliguric phase of ARF Idiopathic • Nephrotic syndrome
Hypercalcaemia hypercalciuria • Cardiac failure
Hyperkaelemia Liver cirrhosis • Liver cirrhosis
SIADH Nephrotic syndrome
[Vision/7th/155]

#Adverse effects of loop and thiazide diuretics

Renal side effects
• Hypovolaemia - • Hyperuricaemia (gout)
-

• Hyponatraemia- • Hypomagnesaemia
-

• Hypokalaemia • Hypercalciuria (loop)

• Metabolic O
-

alkalosis • Hypocalciuria (thiazide)

-

Metabolic side effects

&
• Glucose intolerance/hyperglycemia • Hyperlipidemia
Miscellaneous
• Hypersensitivity reactions • Acute pancreatitis/cholecystits
&
• Erectile dysfunction
[Davidson/23rd/355]
Ed
Side effects of spironolactone:
• Hyperkalaemia
Epkrenone
-
Ephe
• Endocrine abnormalities are:
2
• Gynaecomastia
• Impotence
• Benign prostatic hyperplasia
• Amenorrhea
• Metabolic acidosis in cirrhotic patient.

Q. Diuretics can cause hyponatremia with hypokalemia are- (Residency – 2018)

a) Amiloride
b) Hydrochlorothiazide
c) Spironolactone
d) Furosemides
e) Mannitol
Answer: F T F T T
Explanation:
K Sparing drugs:
 Aldosteron receptor Antagonist: Spironolactone, Eplerenone
 Na channel Blocker: Amiloride, Triamterene

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26. Nephrotoxic Drugs

Mechanisms and examples of drug-induced renal disease/dysfunction

Mechanism Drug of toxin
Acute tubular necrosis Aminoglycosides, Amphotericin
Paracetamol Overdose
Radiographic contrast media
Glomerulonephritis Penicillamine, gold, Allowpurinal
(Immune-mediated) Pneicillamine, propylthiouracil, hydralazine
NSAIDs Cyclophosphamide, Donorable
Interstitial nephritis (immune- NSAIDs, Penicillins, proton pump inhibitors,
mediated) Mesalassion
Interstitial nephritis- Lithium
Ciclosporin, Tacrolimus
Chronic Interstitial Nephritis: Tenofovir, Tacrolimus, Ciclosporin Lithium
Acute Interstitial nephritis + TCL Toxicity
Ref: Davidson’s 23rd P-427, Box-15
Nephrotoxic Drugs:
 Aminoglycosides
 Amphotericine
 NSAIDs, ACEI, Paracetamol
 Radiographic contrast media
 Lithium, Cisplatin, Ciclosporin, Penicillamine
 Penicillin, Rifampicin, PPI

Q. Long term frusemide therapy should be monitored for- [MD/MS/Basic- March’13]

a) Hypocalcaemia
b) Hypomagnesaemia
c) Hyperphosphataemia
d) Hypercalcaemia
e) Hyperkalaemia
Answer: F T F T F
Q. Followings are the loop diuretics- [FCPS- Jan’19]
a) Frusemide
b) Indapamide
c) Bumetanide
d) Ethacrynic acid
e) Amiloride
Answer: T F T T F

Q. The electrolyte changes followed by prolong thiazide therapy-[MD/Basic March’11]

a) Hyponatraemia
b) Hypercalcaemia
c) Hyperkalaemia
d) Hypermagnesaemia
e) Hypocalcaemia
Answer: T T F F F

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Respiratory Pharmacology
27. Anti-Asthmatic Drugs
Drugs used in bronchial asthma:
A. Bronchodilators:
1. Adrenergic drugs:
i. Selective B2 agonist:
• Salbutamol
• Salmeterol (long acting)
• Terbutaline
• Formoterol (Long acting)
ii. Non-selectives: (in severe acute asthma only & given IV)
• Adrenaline
• Isoprenaline
• Ephedrine
[Link] derivatives
• Aminophylline
• Theophylline
• Doxyphylline
3. Antimuscurinic drug: (nebulizer)
• Ipratropium
• Oxytropium
• Tiotropium
B. Drugs that inhibit the release of bronchoconstrictor mediator/ anti-inflammatory:
1. Glucocorticoids: (To face the stressful condition in severe acute attack of asthma.
• Hydrocortisone (Inj)
• Prednisolone (tablet)
• Beclomethasone (Inhaler)
• Betamethasone (Inhaler)
• Triamcilone (Inhaler)
2. Mast cell stabilizer:
• Disodium chromoglycate
• Nidocromil sodium.
3. Antihistaminic drug: Ketotifen
C. Others
1. Leukotriene pathway inhibitor: zileuton, Zafirlukast, Montilukast
2. Anti IgE monoclonal antibody: Omalizumab
Acute asthma Chronic Asthma
1) Inj. Aminophyllin by infusion (in normal saline 1) Aminophylline (oral)
or dextrose saline)- IV 2) Theophylline (oral)
2) Adrenalin (IM) 3) Salbutamol (Oral/ Inhalation)
3) Isoprenaline (IM) 4) Ephidrin (oral)
4) Salbutamol (Inhalation)
5) Steroid (Inj)
6) Ipratropium bromide

Prophylaxis of asthma
1. Disodium charomoglycate (Inhalation)
2. Nidocromil sodium (Inhalation)
3. Steroid- prednisolone (oral) or bechlomethasone (inhalation)
4. Anti-histaminic: Ketotifen (Oral)
5. Leukotrien inhibitors: Zaferlukast, montelukast
6. Theophylline
7. Salmetrol

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Effects of beta 2 agonist:

• Relaxation of smooth including bronchial, uterine and vascular
• Inhibition of release of inflammatory mediator
• Increased mucocilliary clearance
• Increase in heart rate, force of myocardial contraction, speed of impulse conduction and enhanced
production of ectopic foci in the myocardium and automaticity in pacemaker tissue. This can cause
dysrhythmias and symptoms of palpitations
• Muscle tremor
• Vasodilatation in muscle, part of this effect in indirect via activation of endothelia NO biosynthesis
• Desensitization
Adverse effects:
Ipratropium bromide Theophylline
Bitter taste (this may compromise compliance) Gastro-intestinal: nauses, vomiting, anorexia
Acute urinary retention (in patients with prostatic Cardiovascular (1) dilatation of vascular
hypertrophy) smooth muscle
Acute glaucoma has been precipitated when Headache, flushing and hypotension (2)
nebulized tachycardia and cardiac dysrhythmias
Doses are given via a face mask Central nervous system: insomnia, anxiety,
Paradoxical bronchoconstriction due to agitation
sensitivity to benzalkonium chloride, shinc is the Hyperventilation, headache and fits
preservative in the nebulizer solution
Inhaled steroid Montelukast
Candidiasis of the pharynx or larynx occurs in 10- Gastro-intestinal upsets
15% of patients Rash, fever, arthralgia’s
A hoarse voice may develop due to a laryngeal Elevation of serum transaminases
myopathy at high doses
Iatrogenic Cushing
Posterior sub capsular cataracts

Q. A child with asthma is treated with adrenoceptor agonist, side effects might be (Residency –
2019)
a) Sedation
b) Palpitation
c) Muscle tremor
d) High blood pressure
e) Blurred vision
Answer: F T T F F
Explanation: Side effects of adreno receptor agonist (Salbutamol):
 Tremor
 Weakness
 Tachycardia
 Headache
 Hypokalemia
 Peripheral vasodilation Weakness

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28. Drugs Causing Bronchoconstriction

Respiratory Pharmacology
Drugs causeing Broncho constriction:
 Beta blocker
 Cholinergic agonist
 Atracurium
 Thiopentonate
 Aapirin
 NSAID
 Fentanyl
 Morphine
 Propofol
 Acctylcholine
 TPS
 Opioid
 Adenosine
 Tamoxifin
 Dipyridamole

GIT Physiology

29. Drugs used in Peptic Ulcer

Drugs for Peptic Ulcer
Drugs for Peptic Ulcer

&
Gastric acid secretion inhibitors Gastric acid neutralizers Anti H. Pylori
e (Antacids) drugs

E
Amoxicillin
Clarithromycin

>
- Metronidazole
H2 Antihistamines Proton Pump Prostaglandin Ulcer
Analogue
Tinidazole
inhibitors protectives Tetracycline
Cimetidine
CBS
Ranitidine Omeprazole Misoprostol Sucralfate
Famotidine Esomeprazole Colloidal
Roxatidine Pantoprazole bismuth
-
Lansoprazole Subcitrate (CBS)
Rabeprazole
Dexrabeprazol
e
Systemic Non systemic

& Anticholinergics

O Sod. Bicarbonate
Sod. Citrate
=
Mag. Hydroxide
Mag. Trisilicate

=
Pirenzepine Alumin.
Propantheline -
Hydroxide
Oxyphenonium Magaldrate
Cal. Carbonate

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Drugs used cytoprotective in PUD:

 Bismuth Chelate
 Carbenoxolone
 Sucralphate
 Misoprostol
 Bismuth Subcitrate Potassium

Triple therapy /H. eradication therapy

 PPI=12 hourly
 Amoxicillin= 1gm /12hrly. For 7 days
 Clarithromycin =500mg/12hhrly, for 7 days
It is indicated in:
 PUD,
 Pylori positive dyspepsia,
 MALToma
Not indicated in:
• GERD
• Asymptomatic people without risk factor
Adverse effect of [Link] eradication therapy
• Diarrhoea
(30-50% of patients, usually mild but clostridium difficile-associatee colitis can occur)
• Flushing and vomiting when taken with alcohol (metronzadole)
• Nausea, vomiting
• Abdominal cramp
• Headache
• Rash
Quadruple Therapy – Backup (first-line where [Link] resistance to
clarithromycin>to metronidazole)
 Tetracyfline
 Protein synthesis inhibitor
 Metronidazole
 Source of intracellular free radicals
 Bismuth subsalicylate (Pepto-Bismol) or bismuth citrate
 Toxic to H. pylore and protects stomach lining from acid
 PPI
 Continue for 14 days
Q. Cytoprotective drugs used in PUD are (Residency – 2017)
a) Pantoprazole
b) Ranitidine
c) Bismuth chelates
d) Misoprostol
e) Sucralfate
Answer: F F T T T
Explanation:
a) PPI
b) H2 antagonist

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Cytoprotective agents:
 Bismuth chelates/Bismuth Subsalicylate
 Sucralfate
 Misoprostol

30. Antiemetic Drug

Receptors for Emesis

Chemical transmitters & Receptors involved in vomiting include
 Ach (Muscarinic receptors)
 Dopamine (D2)
 Histamine (Histaminergic receptors H1)
 Serotonin (5-HT3)
 Substance P (Neurokinin receptors, NK1)
 Opioid (Opioid receptors)

Antiemetic drugs

Antihistamines, Dopamine D2 Serotonin 5HT3

Anticholinergics receptor antagonisits receptor antagonists
 Dimenhydrinate • Metoclopramide • Ondansetron
 Hydroxyzine • Chlorpromazine • Granisetron
 Cyelizine • Prochlorperazine • Dolasetron
 Meelizine • Promethazine • Ramosetron
 Scopolamine • Haloperidol • Tropisetron
 Trimethobenzamide • Droperidol

Neurokinin-1 Others
receptor antagonists • Cannbinoids
• Aprepitant • Nabilone
• Fosaprepitant • Dronabinol
• Rolapitant • Nabiximol
• Dexamethasone
• Netupitant/
Palonosetron
Q. Anti-emetic drugs are (Residency – 2016)
a) Meclizine
b) Metformin
c) Dopamine
d) Domperidone
e) Ondansetron
Answer: T F F T T

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Anti-emetic drugs are:

 5HT3 Blocker ondansetron
 Dopamine antagonist Domperidone, Metoclopramide
 Anti-histamine-Meclizine
 Anti-cholinergic-Hyoscine
 Nk1-Aprepitant

Autacoids
31. Prostaglandin

Prostaglandins Synthetic Indication / use

analogues
PGE1 Alprostadil [Link] mainatain the patency of patency of ductus arterious
before surgery
[Link] in erectile dysfunction
Misoprostol To prevent gastric & duodenal ulcer
Gemeprost Termination of pregnancy
PGE2 Dinoprostone Induction of labour
Termination of pregnancy
PGI Epoprostenol Inhibits platelet aggregation
Used in primary pulmonary HTN
PGF2α Dinoprost Termination of pregnancy
Carboprost Used in postpartum haemorrhage for its oxytocin action

32. Anti Histamine

Setation
O
Classification of histamine antagonist:
H1 receptor antagonist:
First generation
Ethanolamines Carbinoxamine
Dimenhydrinate
~
Diphenhydramind
Piperazine derivatives Hydroxyzine
Cycline
-
Meclizine
Alkylamines
&
Brompheniramine
chlorpheniramine Histacin
Phenothiazine derivatives Promethazine
Miscellaneous Cyproheptadine
Second generation
-
Piperidine Fexofenadine-
Miscellaneous Cetirizine, Ketotifen, Loratadine, Levocacastin
- -

u
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H2 receptor antagonist:
• Cimetidine
• Ranitidine
• Famotidine
• Nizatidine

H3 receptor antagonist
• Thioperamide
• Impromidine

Different between 1st & 2nd generation antihistamine

1st generation 2nd generations
Short to intermediate action  Long acting
BBB cross  Poor penetration
Sedative action  No
Produce anti muscurnic side effects  No
Also block aunomic receptors  No
Cheap  Relatively expensive

&
Indications of H1 receptor antagonist
-
Use Drugs
of
Allergic condition
• Allergic rhinitis
Loratadine
Cetirizine
• Urticaria Diphenhydramine
• Insect bites
• Atopic dermatitis
• Drug hypersensitivity
Motion sickness and Diphenhydramine They are also used in muscular
-
vestibular disturbances (3,4 Promethazine syndrome
hours before journey) Cyclizine
Meclizine
Nausea and vomiting Piperazine derivatives
M - Doxylamine
&
For sedation
Rx of parkinsonism
Promethazine
For anti-muscarinic effect
Pre-anaesthetic medication
Local anaesthetic - Promethazine
diphenhydramine

Drugs that are used for motion sickness:

• Antimuscarinic agents
• Cinnarizine
• Cyclizine
• Diphenhydrinate
• Scopolamine
• Hyoscine
• Promethazine

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Drugs causing histamine release:

 Penicillin
 Morphine
 D tubocurarine
 Polymixin B
 Dextran
 Radio contrast media
Q. Antihistamines having less sedative effect are (Residency-2017)
a) Chlorpheniramine maleate
b) Loratadine
c) Meclizine
d) Fexofenadine
e) Promethazine
Answer: F T F T F
Explanation:
1st generation are more lipid solubleenter into CVSsedation
 Promethazine
 Diphenhydramine
 Chlorpheniramine maleate
 Promethazine
 Dimenhydrinate
2nd & 3rd generation antihistamines are less lipid soluble. So less enter into CVS- less sedating
2nd generation:
 Loratadine
 Cetirizine
 Ketotifen
 Cyclizine
3 generation:
rd

 Fexofenadine
 Levocetirizine
 Desloratadine

Endocrine Pharmacology
33. Steroids
Classification of glucocorticoids
[Link] (Less potent) Cortisol (t1/2: 1-5 hr)
Hydrocortisone
Corticosterone
[Link] A. short acting Cortisone
(more potent) (8-12 hours) Prednisone
Prednisolone
Methyl-prednisolone
B. Intermediate acting Flu-prednisolone
(12 -36 hours) Paramethasone
Triamcinolone
C. long acting Dexamethasone
(36-72 hours) Betamethasone
Beclomethasone

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Effects of glucocorticoids:
1. Physiological effects.
2. Pharmacological effects.

Effects of glucocorticoids on metabolism:

1. Physiological effects:
A. Effect on carbohydrate metabolism: ↑Blood glucose level.

i. Stimulate gluconeogenesis: ↑Uptake of amino acids in the cell → neoglucogenesis → ↑glucose

in the cell → glucose is released in circulation → ↑Blood glucose level.
ii. Inhibit glucose uptake in the cell.
iii. It also ↑the conversion of glucose to glycogen.
In fasting, hypoglycemia, stress, tension →↑secretion of glucocorticoids (sp. cortisol) →↑Blood
glucose level. → Thus, glucocorticoid supplies energy (fuel) to brain in those conditions.

B. Effect on protein metabolism: It enhances protein catabolism. i.e. break down of protein to
amino acids. So, prolong steroid therapy results in -
1. Muscle wasting.
2. Destruction of bone matrix (osteoporosis)
3. Removal of skin protein specially from dermis → skin becomes thin.
4. Tin capillary permeability → bruise & striae in the skin. Plethoric (red) face.

C. Effect of fat metabolism:

It enhances lipolysis & mobilizes fat from periphery to upper part of the trunk & face, resulting in
- moon face, buffalo hump, Pendolus abdomen.

D. Effects on electrolytes:
i. Cortisol → DCT →↑reabsorption of Nat & water → ↑Blood volume.
ii. Permissive role of glucocorticoids:
iii. Glucocorticoids directly act on the cell. They also regulates the activity of other substances in
the body e.g.
a. The effect of adrenaline on bronchial smooth muscles is reduced in the absence of cortisol.
b. The effect of adrenaline of blood vessels is also reduced in the absence of cortisol.
c. The effect of adrenaline on lipolysis is reduced in the absence of cortisol.

2. Pharmacological effects:
A. Anti-inflammatory effects:
Mechanism: Glucocorticoids
08
1. Inhibit phospholipase A2 enzyme inhibit the synthesis of inflammatory mediators (PG & LT).
2. Stabilizes the lysosomal membrane → No release of enzymes responsible for inflammatory
response
3. Permissive action: With Catecholamines it causes bronchodilation and pressor effect.
4. Inhibits the capillary permeability → Leukocytes can not migrate to the area of inflammation.
5. Limit the ability of macrophage to phagocytose & kill miro-organisms.
5. Inhibit the release of IL-I from macrophage & IL-2 from T-lymphocytes.
6. Result in movement of circulating lymphocytes, monocytes, eosinophils & basophils to
lymphoid tissue.
7. Also inhibit cyclo-oxygenase enzyme, responsible for release of inflammatory mediators.

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-B. Immuno-suppressive effect: Glucocorticoids

1. Inhibit the formation of Ab.
2. Result in movement of circulating lymphocyte, monocytes, eosinophils & basophils to
lymphoid tissue → Cell Mediated Immunity ↓.
3. Limit the ability of macrophage to phagocytose & kill microorganisms.
4. Inhibit the release of IL-1 from macrophage & IL-2 from T-lymphocytes.
5. Inhibit the activity of complement.
6. Impair delayed hypersensitivity reaction.
7. Result in reduction of lymphoid tissue in the body due to protein catabolism.

C. Hyperacidity: Glucocorticoids inhibit phospholipase A2 enzyme & thus inhibit synthesis of

-
PG:
1. HCl secretion.-
2. ÎPepsin secretion
3. Mucous secretion May lead to peptic ulcer.

E
D. Osteoporosis:
1. Catabolism of matrix protein of bone.
2. ↓absorption of Cat from GIT due to presence of anti-vitamin D activity.
3. Increase excretion of Ca++ leading to hypocalcaemia. May lead to back pain, rib fracture due to
long use.

E. ↑Number of RBC & platelets in circulation → Hyper-coagulability.

F. Glucocorticoids for prolong period → Electrolytes imbalance in CNS → Euphoria, psychosis.
G. Renal stone: Due to - Twater retention & ↑Ca++ excretion.
H. Growth reterdation in children.
I. HTN due to - -↑Nа & water retention
- ↑vascular response to nor-adrenalin.
J. DM due to- - Na retention → TK+ excretion → Hypokalaemia →↓ Insulin secretion.
-Neoglucogenesis → ↑Blood glucose level.
Adverse effect of steroid use:
I. Physiological-- Adrenal and /or Pituitary suppression by negative feedback
-
II. Pathological—

* Cardiovascular - Increase blood pressure by Na+ retention

*Gastrointestinal:
-

 Peptic ulceration exacerbation by inhibiting PG synthesis & increasing acid secretion

 Pancreatitis
*Bone and muscle: - Osteoporosis by Ca++ mobilization from bone
 Osteonecrosis, Pathological fracture
 Muscle wasting by protein catabolism
* Endocrine: Weight gain, Diabetes mellitus by hyperglycemia, impaired growth, Amenorrhea
*Skin: Thinning, Easy bruising increased susceptibility to infection:
 Delayed wound healing due to anti-inflammatory action
 Septicemia, Fungal infection, Tuberculosis due to immune suppression

G*Eye: Cataract G
*CNS: Depression, Euphoria, Steroid Psychosis, Insomnia

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• Sudden withdrawal of steroid causes:

 Adrenocortical insufficiency
 Weight loss
 Arthalgia
 Itchy skin nodule
 Conjunctivitis
 Rhinitis
 Steroid should not be used in: PUD. HTN, DM, Active infection, glaucoma, Cushing syndrome

34. Drugs used in DM

I. classification of insulin:
A. According to onset & duration of action:
Duration of action (in hours) of insulin preparations

-Rapid-acting (Insulin
Insulin
analogues: lispro,
Onset
<0.5
Peak
0.5-2.5
Duration
3-4.5
aspart, glulisine)
-

Short-acting (Soluble (regular)) 0.5-1 1-4 4-8

O
-

Intermediate-acting (isophane (NPH), lente) 1-3 3-8 7-14

Long-acting (bovine ultralente) 2-4 6-12 12-30
Long-acting (insulin analogues: glargine,
-
1-2 None 18-26
detemir, degludec)
--
B. According to source:

1. Mixed species insulin: 70% bovine + 30% porcine insulin (& other combinations)
2. Monospecies insulin (porcine):
• Actrapid
• Monotard
• Semitard.
3. Newer insulin preparation: (DU-055)
Human insulin:
• Enzyme modified porcine insulin (EMP)
• Chain recombinant bacterial Insulin (CRB)

-Human proinsulin
Adverse effects/ complication of insulin:
 Hypoglycemia:
-
Hypoglycemic reaction, hypoglycemic shock.
 Insulin allergy -

 Lipodystrophy.
C
 Insulin edema.
 Rebound hyperglycemia.
 Insulin resistance.
EObesity
 -
Hypokalaemia.
 Alopecia (loss of hair)

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Antidiabetic
Oral hypoglycaemic agents

&
A. Anti-diabetic drugs producing hypoglycemia:
-
[Link]:
a. Sulforamide derivatives: 1st generation: old Tolbutamide (Safest)
&
Sulfonylures Chlorpropamide
Acetohexamide
Tolazamide
2nd generation: New Glyburide
Glipizide
Glbenclamide
Glicazide
①b. Meglitinide Repaglinide, Nateglinide

Anti-diabetic drugs producing euglycemia:

&[Link] derivaitives
-

Phenformin (banned)
Metformin (used) Buformin
-

[Link] Troglitazone
Rosiglitazone
-

Pioglitazone
3.α glucosidase Inhibitors
-
&
Acarbose
Migilitol

Sulfonylurea:
1st generation: old Tolbutamide (safest)
Chlorpropamide
Aceetohexamide
Tolazamide
2nd generation: New Glyburide
Glipizide
Glipalamide
Glibenclamide
Glicazide
3rd generation Glimepiride

Advantage of 2nd generation over 1st generation:

1. 2nd generatio drugs are 100-150 times more potent
2. Plasma half-life is long, so can be used once a day
3. Can be given in renal insufficiency
4. More safer (TI) and less adverse effect

Adverse effects:
1. Hypoglycemia
2. GIT upset Nausea, Vomiting, Diarrhoea
3. Allergic reaction, Rash
4. Blood disorders: Agranulocytosis, aplastic anemia
5. Teratogenesis (So strictly contraindicated in pregnancy. During pregnancy, only insulin is
indicated is DM pt)

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6. Cholestatic jaundice
7. Alcohol intolerance: sulfonylurea causes alcohol intolerance. It inhibits metabolism of alcohol
& produces disulfiram like action (i.e. the pt. cannot tolerate)

Metformin
The activity of Biguanide is not dependent on the presence of functioning pancreatic β-cells for their
hypoglycemic action.
They are appropriately termed ‘englycemic agents'. Because they cause hypoglycemia in
hyperglycemic condition. The effect on normal blood glucose level is more or less zero.
They act by
 Direct stimulation of glycolysis in tissue which increase glucose removal from blood.
 ↓hepatic gluconeogenesis.
 Slowing of glucose absorption from gut.
 ↓Plasma glucogon level.
 Increasing insulin binding to insulin receptor.

Indication:
 Type II DM
 Obese patient
 When Sulfonylureas fail.

Adverse effect of metformin:

• Anorexia
• Nausea, vomiting
• Diarrhoea
• Abdominal pain
• Lactic acidosis
• Decrease
•↓Vitamin-B12 absorption
• Erythema
• Pruritus and urticaria
• Hepatitis

SGLT2 Inhibitor:
 The sodium and glucose transporter 2 (SGLT2) inhibitor, dapagliflozin, was licensed for use in
2012. Subsequently, canagliflozin and empagliflozin have also been licensed.
 Glucose is filtered freely in the renal glomeruli and reabsorbed in the proximal tubules. SGLT2
is involved in reabsorption of glucose.
Inhibition results in approximately 25% of the filtered glucose not being reabsorbed, with
consequent glycosuria.
 Although this helps to lower blood glucose and results in calorie loss and subsequent weight
loss, the glycosuria does also lead to genital fungal infections.
 There has been increasing use of these agents over the last few years; however, the recent
announcement of the Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2
 Diabetes (EMPA-REG Outcomes) trial has the potential to change dramatically the way these
drugs are now used. Empagliflozin therapy resulted in a 35% reduction in cardiovascular
mortality and a similar reduction in admissions to hospital with heart failure. As such, these
drugs should now, at the very least, be used in all patients who fulfil the inclusion criteria of the

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trial – prior myocardial infarction, coronary artery disease, stroke, unstable angina or occlusive
peripheral arterial disease.
 Euglycaemic diabetic ketoacidosis (i.e. DKA not associated with marked hyperglycaemia) has
been recognised as a rare complication of this class of drugs.

Effects of drugs used in Treatment of type 2 diabetes:

Insulin Sulphonylur Metformin Alpha- Thiazolidinedi DPP-4 GLP SGLT2
eas and glucosidase ones inhibitors receptor inhibitors
meglitinides inhibitors (glitazones (gliptins) agonists
Fasting blood ↓ ↓ ↓ ↓ ↓ ↓ ↓
glucose
Post-prandial ↓ ↓ ↓ ↓ ↓ ↓ ↓ ↓
blood glucose
Plasma ↑ ↑ ↓ ↓ ↓ ↑ ↑ ↑
insulin
Body weight ↑ ↑ → → ↑ → ↓ ↓
Cardiovascul No No Possible No Probable No Yes Yes
(pioglitazone)
ar benefit?
Risk of ++ + - - - - - -
hypoglycaemi
a
Tolerability Good Good Moderate Moderate Moderate Good Moderate Limited
experience
( = Small reduction: DPP.4 = dipeptidyl peptidase 4; GLP-1 = Glucagon-like peptide 1; SGL T2 = sodium and glucose
transporter 2)

& Safe antidiabetic during Pregnancy

② Insulin
-
 Metformin
 Glibenclamide -
Q. Sulfonylureas (Residency-2013)
a) Increase the secretion of insulin by β-cell
b) Decrease the number of insulin receptors
c) Decrease serum glucagon
d) Exhibit high affinity for plasma binding
e) Can be used in renal disease
Answer: T F T T F
Explanation:
a. Insulin secretagogues
c. By inhibition of ∞-cell
d. So drug interaction occurs ē protein binding drugs
e. It can’t be use in hepatic & renal impairment

Q. Side-effects of insulin therapy are (Residency-2013)

a) Hypoglycemia
b) Hypertension
c) Weight gain
d) Hyperkalemia
e) Chronic renal failure
Answer: T F T F F

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Explanation:
a. Common complication of insulin therapy
c. By increase storage of fat
d. Insulin cause influx of K+ into cells

Side effect of insulin:

 Hypoglycemia
 Weight gain
 Insulin antibodies
 Local allergy
 Lipodystrophy/Lipoatrophy
 Immune insulin resistence
 Peripheral oedema

35. Anti-Thyroid Drugs

Classification of Antithyroid Drugs

Inhibitor of hormone synthesis
-

 Carbimazole
-
 Methimazole
-

 Propylthiouracil
-

Radioactive iodine
 131 (Radioactive iodine)

Inhibitor of hormone release

 Iodine
 Iodides of Na, k
 Organic iodides

Ionic inhibitors
 Thiocynate (-SCN)
 Perchlorates (-ClO4) (
East
-

 Nitrates (NO3)

Side effects of Anti thyroid drugs: Lactatio

Carbimazole
• Skin rash
⑧
Prophylthiouracil (PTU)
• Gastrointestinal distress nausea
• Agranulocytosis • Skin rash
C
> • Teratogenicity
- • Aplasia cutis • Agranulocytosis
• Hepatitis
• hypothyroidism • Hypothyroidism

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36. Classification Oral Pills

[Link] pill i. Standard pill Ethenyl estradiol
Norgestrel
ii. Low dose pill Ethenyl estradiol
Norgestrel
iii. Ultra low dose pill Ethenyl estradiol
Norgestrel
[Link] pill 1st two week Ethenyl estradiol
Next one week Norethedrone
[Link] i. Progesterone only pill Norgestrel
ii. Estrogen only pill Diethyl-stuvvustrol (post-coital)
[Link] coital/ 2 tab as early as possible, then 2 Diethyl-stibbistrol
morning after pill more tab. After 12 hours of 1st Combined pill
dose
[Link] pill Gossypol

6
Mechanism of action of OCP:
-
1) Inhibition of Ovulation:
00
 Both hormones act on Hypothalamo pituitary axis, suppress release of FSH & LH from Ant.
Pituitary:
Estrogen – Inhibits FSH
Progesterone
= – Inhibits preovulatory LH Surge, less effect on FSH
2) Endometrial Hyperplasia:
 Stromal oedema, decidual reaction & regression of glands making endometrium
nonreceptive to embryo
-3) Cervical mucus:
 Thick, Viscid, Scanty
 Impaired sperm transport & Penetration

4) May affect tubal motility & alter tubal transport

Major -

[Link] effects OCP causes increased risk of

a. Thromboembolism
b. Coronary artery diseases
c. Atherosclerosis
d. HTN
[Link] effects ↓HDL
↑Cholesterol
↑LDL
3. Hepatic effects Ca of liver
Cholestatic jaundice
4. Psychological effects Depression due to lack of vit B6
5. Suppress lactation
[Link] Fibro-adenoma of breast
Fibroid uterus

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Minor.
 Nausea, vomiting
 Headache
 Leg crump
 Wt. gain
 Pigmentation of face, forehed, cheek, around eye (cloasthma)
 Mastalgia (heaviness & tenderness of breast)
 Break through bleeding (spot bleeding)
 Hypomenorrhea
 Amenorrhoea
 Menorrhea
 ↑Due to sence of well being
 Libido
 ↓Due to dryness of vagina

Contra-indications of OCP
Absolute Relative Special precaution
[Link] of CVS disease O
[Link] 1. DM
O
-
2. Liver disease (ch. 2. Obesity 2. Collagen diseases
Hepatitis) 3. Migraine 3. Osteosclerosis
-
3. Breast cancer
-
4. Endogenous smoking
5. Heavy smoking
4. Severe varicose veins
5. Sickle cell disease
6. Surgical operation
[Link] of depression
[Link] over 35 years

Adverse effect of OCP

Mild Moderate Severe
Nausea Breakthrough bleeding Venous thromboembolism
Mastalgia
Breakthrough bleeding
Weight gain
Skin pigmentation \acne
= 8
Risk of myocardial infraction, CVD
Gallstones, cholestasis jaundice
-
Hirsutism Depression
Vaginal infections
&Breast and cervical cancer

①
Oxitocics/ecbolics-stimulate uterine muscles Tocolytics –relax uterine muscles

-
= S
• Oxytocin (gravid) Beta agonist/salbutamol
• Ergometrine (birth)
• Prostaglandin (both) I
Glycerin tri nitrate
MgS04
• Ketamine Alcohol
• Quinine (3rd) Progesterone (natural)
-

-
po
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MgSO4
Indication- Contraindication-Hepatic & renal
• Ventricular arrhythmia specially associated with impairment

S
Mg & K depletion Pregnancy category
• Torsade de pointes Short term-safe
• Pre-eclampsia, eclampsia for management of Long term-fetal respiratory depression
seizure
• Mg deficiency
• Bronchial asthma-acute & resistant cases
Side effects Antidote- calcium gluconate
Hypotension, respiratory depression, arrhythmia,
drowsiness, coma, pain at injection site, conduction Monitoring of Rx- respiratory rate,
anomalies urine output, knee jerk, BP
Sign of overdose
Loss of patellar reflex, muscle weakness, nausea,
sensation of warmth, flushing, drowsiness, double
vision, slurred speech.

Causes of Lactic Acidosis

• Cyanide
• Carbon monoxide
• Ibuprofen
• Isoniazid
• Metformin
• Salicylates
• Valporic acid
• Any drug induced seizures, hypoxia of hypotension

37. Ovulation Inducing Agent

Drugs used in induction of ovulation:

Stimulation of ovulation: receptor
modulator SERM
estrogen
 Clomiphine citrate -selective inhibitor
-

 Letrozole Aromatase

Xerogen
-

 hMG -
H
OFSH
L  hCG activity
LH like
-

=
-
 GnRH
 GnRH analogue Gosevelin naturelin
,
, Leuprolide

-Est
--
Correction of biochemical abnormality:

S
 Metformin-insulin
-
residtance
 Dexamithasone-Androgen excess
 Bromocryptine-hyperprolectinaemia

Substitution therapy:
 Hypothyroidism – Thyroxin
 DM – Anti diabetic drug

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Q. Drugs induced ovulation in infertile women are (Residency – 2016)

a) Ethinyl estradiol
b) Clomiphene citrate
c) Human chorionic gonadotropin
d) Danazol
e) Follicle stimulation hormone
Answer: F T T F T
Explanation:
Ovulation inducing drugs
 Clomiphene
 Bromocriptine
 Human chorionic gonadotrophin
 Gonadotrophin releasing hormone
 Estrogen
 Partial agonist e weak pregestational functions

38. Pharmacology Related to Covid 19

Possible Therapeutic Interventions in COVID-19

Lopinavir/ritonavir
Remdesivir
Chiloquin/Hydroxychloroquine (With or without azithromycin) Anti-JAK
(baricitinib) Tocizilumab Methylprednisolone
Stem cells
IV immunoglobulins
Convalescent plasma
Fabipiravir
Ivermectin
Carrimycin
Bromhexine
Thalidomide
Oseltamivir (Tamiflu)
Umifenovir (Arbidol)
Angiotensin
Thalidomide
Sildenafil
Traditional Chinese medicines: Yinhu qingwen, haaier

Remdesivir
 It was used earlier in the treatment of SARS & MERS caused by member of coronoa virus
family.

Mechanism of action:
 It inhibit RNA Dependent RNA Polymerase
 Remdesivir decrease viral RNA

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Dose:
 In Adult: 40 kg or more - Loading dose 200 mg/ day & maintenance dose 100 mg/ day.
 In Child: less than 40 kg - loading dose 5 mg / kg/ day & maintenance dose 2.5 mg / kg/ day.
Benefit:
1. May reduce viral load when given early during diseases.
2. May be used to avoid prolonged hospitalization.
3. Improves condition of some patient.
Adverse Effect:
 Yellow eyes
 Dark Urine
 Pain in the upper stomach
Indicated in patients with RA who have not responded adequately to first-line therapy or to TNF
inhibitors.
It is sometimes employed as a third-line treatment when TNF inhibitors have been ineffective.
An exception is when patients are MTX intolerant, in which case it is often used as a first-line therapy,
based on a randomised trial in which it showed greater efficacy than the TNF inhibitor adalimumab.
Adverse effects include leucopenia, abnormal
LFTs, hypercholesterolaemia, hypersensitivity reactions and an increase risk of diverticulitis.
Pharmacotherapeutics
Mild cases:
Mild case may be treated in isolation in a single room at home. (Above mentioned home isolation
protocol should be strictly followed)
Symptomatic patients (bed ridden): Admitted in isolation ward (especially in risk group like
DM, HTN, IHD, Prior Asthma/COPD/ILD patients, Known CKD, CLD, Known
Malignancy, High Risk pregnancy, Obesity (BMI>25.)
 Tab Paracetamol (500mg) 1 tab if temp is more than 1010F
 Antihistamine if there is rhinorrhea
 Antitussive of there is dry cough
 For thromboprophylaxis (mild cases with risk group): Exoxaparin-For patients with creatinine
clearance (CrC1) > 30 mL/Min, 40 mg SC once daily; for CrCl 15 to 30mL/min, 30 mg once daily.
Therapeutic dose as follows: enoxaparin 1 mg/kg every 12 hours SC if creatinine clearance
(CrCl) > 30 mL/min.
 Monitor closely

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Moderate case: Isolation ward (any clinical or radiological pneumonia

case) Mild symptomatic case Treatment Protocol
Plus
 Oxygen through nasal canula 2L /min if required (man 6L/min possible).
 Tab Favipiravir: 1600 mg on day 1 followed by 600 mg BID from day 2 to day 10
 Pruning- Prone position at least 4-6 hrs/day
 LMW heparin (In) enoxaparin) Enoxaparin 1mg/kg SC twice daily/ day (dose adjust with
CrCl< 30m1/min) Or if LMWH can’t be given or contraindicated, In) Unfractionated heparin
(UFH): 60U/kg bolus+12units/kg/hr infusion-for ACS 80U/Kg bolus +18units/kg/hr
infusionfor VTE and AF
 Thromboprophylaxis should be given until symptom resolves or improves and followed by
Tab rivaroxaban 10 mg once daily for 1 month
 Any Moderate case on treatment — if no response or deterioration at 24 hours in hospital,
Oral Methylprednisolone (60-80 daily) in single or two divided doses for? days with
antiolcerant coverage

Severe cases with respiratory symptoms (S08; hypoxia: admit to ICU or even in
ward/makeshift ICU): Preferably in Secondary care/Tertiary care

Management of Moderate case protocol (Except oral steroid) Plus

 Steroids- In) Methylpredniolone-250 mg daily for 5 days (switch to IV from oral if already
started)
 Maintain euvolaemia (Avoid fluid load)
 Early Norepinephrine for hypotension
 Broad spectrum antibiotics—Inj Meropenam 1gm BD
 Inj Remdesavir: 200 mg IV infusion within 30 min-2 hours on Day 1 followed by 100 mg
infusion within 30 min to 2 hours from Day 2 to Day 5. Remdesivir should be used at the
discretion of consultant working in the hospital. (If favipiravir started in moderate case, it
should be stop)
 Consider for cytokine storm/ HLH (Hemophagocytic lymphohiocytosis) picture:
1. Tocilizumab
2. Convalescent Plasma therapy
Hypercoagulability in COVID 19:

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ANTICOAGULANT

Indicaion of LMWH:
1. Prophylaxis / treatment of DVT
2. Presurgical / post surgical
3. Pulmonary embolism

Adverse Reactions
• Hemorrhage
• Anemia
• Thrombocytopenia – (decreased platelet count)
• Diarrhea
• Nausea
• LD50 46.4 mg/kg

Contraindications
• Active, major bleeding
• Thrombocytopenia
• Sensitivity to:
 Heparin
 Pork or pork products
• Dose adjustment in hepatic or renal impairment

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Others

39. Causology

* Drugs causing peripheral Neuropathy * Drug causing lactic acidosis

* Nephrotoxic Drugs * Drug causing Gynecomastia
* Drug causing optic neuritis * Drug causing SLE
* Drugs having hangover effect * Drug causing Hyperglycemia
* Hepatotoxic Drugs * Drug causing Alopecia
* Ototoxic drug * Drug causing Lung fibrosis
* Drug causing Gout * Drug causing Weight gain
* Drug decreasing libido * Drug causing Hyperkalemia
* Drug causing postural hypotension * Drug causing Myalgia
* Drug causing Hypertension * Drug causing Hirsutism
* Drug causing acute pancreatitis * Drug causing Gum Hypertrophy
* Drug causing acute haemolysis * Drugs causing SIADH

• Radioactive contrast media

• Vancomycin
• Penicillamine, gold
• Rifampicin (RS)
Peripheral neuropathy • Acyclovir
• Amiodarone • Cabergoline
• Antibiotics → Metronidazole,, dapsone,
INH, sthsmhutol, quinolomes,
streptomycin, nitrofurantoin Optic neuritis :
chloramphenicol, linezolid • Ethambutol
• Anti-malarial → Chloroquine, • Streptomycin
Mefloquine • INH
• Anti-fungal → Grieseofulvin • Digoxin
• Cytotoxic → vincristine, vinblastine, • Achohol
cisplatin, thalidomide • Chloramphenicol
• Phenytoin
• Sulphonylurea Hangover effect:
• TCA, MAOI • Barbiturates
• Halotthene
Nephrotoxic • SSRI
• Penicillin, cephalosporin
• NSAID, Paracetamol, Paraquat Hepatotoxic
• PPI • Anti TB → Rifampicin, INH, PZ( RIP)
• Amphotericin, Aminoglycoside • Macrolides
• ACEi, ARB • Tetracycline
• Cyclosporin, Tacrolimus • Co-amoxiclav
• Lithium • Flucloxacillin
• Tenofovir Hepatotoxic (Contd.)
• Mesalasine • Anti convulsant → Na valproate
• Cisplatin (Chemotherapy) • Amiodarone (Non alcoholic
• Tetracycline steatohepatitis)

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• Azathioprime (Alkylating agent) HTN:

• Busulphan (vencus out flow • Corticosteroid
obstruction) • OCP
• Metotrexate (Fibrosis)) • NSAID
• Methylolopa, MADI • MAOI ӗ sympathomimetic agents
• High estrogen → OCP, HRT (cholestasis • Clonidine & methyldopa withdrawal
alone) • Ketamine
• Chlorpromazine • Cyclosporine
• Phenothiazine
• Halathane Acute haemolysis:
• NSAID, Paracetamol • Analgesics → Aspirin,
• Anabolic steroid, statins • Antibiotics → Ciprofloxacin
• Sulphonylurea Nitrofurantoin
• Herbal, coccaire, ccetasy Sulphonamides
• Ant: malaria → Primaquine
Ototoxic:
Chloroquine
• Aminoglycoside
Quinine
• Quinine
Pyremethamine
• Quinidine
• Quinidine, Vitk, Dapsone, Probenacid
• Chloroquine
• Salicylates
Acute Pancreatitis:
• Fllusemide
• Azathioprime
• Anti-Ca drug
• Mercaptopurine
• Cisplatin
• Thiazide
• Cyclophosphamide
• Na valproate
• Blemycin
• Na Stibogluconate
• Macrolides
• Cortico steroid
• Auphotericin-B,
• Oestragen
Hyperuricaemia/ Gout: • Anti-HIV therapy
• PZ • Alpha methyldopa
• Low doseAspirin • Tetracycline
• Loop & thiazide diueretics • Sulphonamide
• L-dopa
Lactic acidosis :
Libido (Decrease): • Metformin
• SSRI • Salicylates
• TCA • Valporic acid
• BDZ & barbiturates • INH
• Anti psychotics in men • Ibuprofen
Postural hyprotension/reflex techycardia: • CO
• All vasodilators [Link], Minoxidil • CN poisoning
• @1 blocker eg, oxazosin, terazosin,
proposing ***Gynaecomastia:
• Phenoxybezamine • Spironolactone
• Chlorpromazine • Cimetidine
• GTN • Digoxin
• Morplne, nicotine • Anti-androgen→ Cyproterone acetate
• TCA, MAOI, • Exogenous anabolic steroid
(Diethystillbesterol)
• Cannabis

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• Methyldopa, Cytotoxic agents,  Bad → Busalfan

Grisiofulvin, reserpine, Phenothiazine,  Air → Amiodarone
TCA, INH.
**** SLE, SJS, TEN: Weight gain:
• Hydralazine (90%) • Insulin
• Procainamide • Sulfonylurea
• Phenytoin, carbamazepine • Steroid
• Phenothiazine, quinidine • OCP
• INH • Anti psychotics
• Penicillamine • Antidepressant (except SSRI)
• OCP • Lithium
• Methyledopa
• Minocycline Hyperkalaemia
• ACE • NSAID
• Cyclosporin
Hyperglycacimia: • β blocker
• Antibiotics → Floroquinoloncs • ACEi
• Β blocker, thiazide • Heparin
• Steroid, cyclosporine • Digoxin
• Alypical antipsychotic • K sparing diuretics
• Anti-retroviral → Protease inhibitors • Sulfamethoxazole
• Diazonide • Trimethoprim
• Theophyiline
• Somatostatin Myalgia
• Streptozocin • Alchohol, cocaine
• Pentamidine • Statins, fibrate
• Penicillamine
Alopecia: • Zidovudine
• Heparin • H2 tlockers → Cimetidine ratitidine
• Chloroquine • Propanolol
• Any chemotherapcatic agents • Immunosuppressive drugs
• Na-valproate
• Insuline Hirsutism
• Colchine • Diasoxide
• Minoxidil
Lung Fibrosis:
• Steroid
 My→ Methotrexate
• Androgen
 Nose → Nitrofurantoin
• Phenytoin
 Cant → Carustine
• Cyclosporin
 Breath → Bleomycin
• OCP

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Drug causing SIADH:

ADH analogues Antineoplastics Cardiovascular agents Psychotropics
Desmopressin Alemtuzumab ACE inhibitors Antipsychotics
(DDAVP) Cilazapril Chlorpromazine
Enalapril Haloperidol
Lisinopril Fluphenazine
Ramipril Risperidone
Oxytocin Chlorambucil Amiodarone Lorazepam
Vasopresin Carboplatin Clofibrate SSRIs
Sertaline
Analgesics Cisplatin Clonidine Duloxetin
Diclofenac Cyclophosphamide Methyldopa Tricyclic
antidepressant
Fentanyl Etoposide Phenoxybenzamine Venlafaxine
Ibuprofen Melphalan Propafenone Viloxazine
Antiparkison Rituximab Thiazides Other
agents
Amantadine Vidarabine IFN-α
Levodopa Vincristine Anti-infectives MDMA (ecstasy)
Anticonvulsants Vinblastine Azithromycin Nicotine
Carbamazepine Hypoglycemic agents Micronazole Omeprazole
Oxcarbazepine Glimepiride Rifabutin Tacrolimus
Valproic acid Metformin Theophylline

Gum hypertrophy
• Cyclosporin
• Phehytoin (Anti-convulsant)
• Ca2 cannel blocker

40. Adverse Effect

Busulfan:
• Nausea, vomiting
• Skin pigmentation
• Lung fibrosis
• Adrenal insufficiency

Bleomycin:
• Allergic reaction
• Fever
• Hypotension
• Skin toxicity
• Lung fibrosis
• Mucositis
• Alopccia

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Cyclophosphamide
• Pancytopenia
• Haemorrhagic cystitis
• Hepatocyte necrosis
• Marrow toxicity
• Infertility,
• Alopecia
• Teratogenicity
• Nausca
• ↑ risk of Carcinoma of bladder
• GIT upset
• Overian failure
• Azoospermia

Azathioprine
• Marrow Suppression
• Pancytopenia
• Skin: Rash
• Drug fever
• Nausea, Vomiting
• Hepatotoxicity
• Atopecia
• ↑ risk of cancer
• A. Pancreatitis

GIP-1 (W) Exenatide, Liraglutide

• Nausea
• ↓G1 Motility
• Wt. loss

DPP-4 (Gliptin)
• Nasopharyugitis
• Headache
• Nausea
• Hypersensivity
• Skin reaction
• Pancreatitis

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41. Summary

1. Classification of Anti-Psychotic drugs

According to chemical nature

1. Phenothiazine derivatives • Chlorpromazine

• Prochlorperazine
• Thioridazine
• Perphenazine
• Trifluoperazine
• Fluphenazine
• Promethazine
[Link] derivatives • Thiothixene
• Flupentixol
[Link] derivatives • Haloperidol
[Link] structure • Pimozide
• Molindone
• Sulpiride

2. Classification of Anti-Depressant Drugs

Drugs Examples
Tricyclic antidepressant: Amitriptyline
blocks reuptake of serotonine, noradrenaline into nerve Imipramine
terminal. Dosulepin clomipramine
Significant first pass metabolism
Selective serotonin re-uptake inhibitors (SSRIs) Citalopram
Escitalopram
Fluoxetine
Fluvoxamine
Sertraline
Paroxetine
Monoamine oxidase inhibtors (MAOIs) Phenelzine
Tranylcypromine
Noradrenergic re-uptake inhibitors and SSRIs Venlafaxine
Noradrenergic and specific serotonergic inhibitor mirtazapine

3. Anxiolytic and hypnotic Drugs:

Classification of benzodiazepine
Ultra-short-acting Short acting (t1/2 <6 Intermediate acting Long acting (t1/2>24
hours) (t1/2 >24 hours) hours)
• Clorazepate • Midazolam • Alprazolam • Diazepam
• Triazolam • Lorazepam • Clonazepam
• Oxazepam • Bromazepam • Flurazepam
• Estazolam • Quazepam
• Femazepam • Nitrazepam
• Parazepam
• Chlordiazepoxide

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4. Drug used in Parkinsonism:

Classification:
 Dopamine analogues: Levodopa
 Peripheral deoxy decarboxylase inhibitor: Carbidopa, benserazide
 COMT – inhibitors: Tolcapone, Entacapone
 MAO-B inhibitors: Selegiline, Clorgyline
 Dopamine agonists: Rosipirole, Pergolide
 Central anti – cholinergics: Benzopropine, Biperiden

5. Type of epilepsy & drug of choice-

Guideline for choice of anti-epileptic drug
Epilepsy type First-time Second-time Third time
Focal onset Lamotrigine Carbamazepine Clobazam gabapentin oxcarbazepine
and/or Levetiracetam Phenobarbital phenytoin pregabalin
secondary GTCS Sodium valproate Primidone tiagabine
Topiramate
Zonisamide
Lacosamide
GTCS Sodium Lamotrigine topiramate Carbamazepine phenytoin primidone
Valproate Zonisamide Phenobarbital acetazolamide
Levetiraceatam
Absence Ethosuximide Sodium valproate Lamotrigine clonazepam
Myoclonic Sodium Levetiracetam Lamotrigine phenobarbital
valproate Clonazepam
N.B use as few drug as possible at the lowest possible dose

6. Anesthetics
Inhalation anesthetics Intravenous anesthetics
 No  Barbiturates- Thiopental Na, Methohexital.
 Halothane  Benzodiazepines - Diazepam •Opioid analgesics -
 Enflurane Morphine, Fentanyl, Pethidine.
 Isoflurane  Propofol
 Desflurane  Ketamine
 Sevoflurane  Miscellaneous drugs: Droperidol, Etomidate.
 Cycloprofen
 Chloroform
 Ether

Analgesics

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7. Mechanism of action of important ankmicobical

Mechanism of action Drug
Inhibition of Cell wall synthesis
Antibacterial activity Penicillin, cephalosporins, imipenem, aztreonam,
Inhibition of cross-linking (transpeptidation) of vancomycin
peptidoglycan
Inhibition of other steps in peptidoglycan Cycloserine, bacitracin
synthesis
Antifungal activity Caspofungin
Inhibition of glucan synthesis
Inhibition of Protein Synthesis
Action on 50S ribosomal subunit Chloramphenicol, erythromycin, clindamycin, linezolid
Action on 30S ribosomal subunit Tetracycline’s and aminoglycosides
Inhibition of nucleic acid synthesis
Inhibition of nucleotide synthesis Sulfonamides, trimethoprim
Inhibition of DNA synthesis Quinolones, e.g. ciprofloxacin
Inhibition of mRNA synthesis Rifampicin
Alternation of cell membrane function
Antibacterial activity Polymyxin, daptomycin, colistin
Antifungal activity Amphotericin B, nystatin, terbinafine, azoles, e.g.
itraconazole
Other Mechanism of action
• Antibacterial activity Isoniazid , metronidazole, ethambutol, pyrazinamide
• Antifungal activity Griseofulvin, pentamidine

Antibiotics classification:
According to spectrum of activity
Broad spectrum antibiotics Ampicillin
Antibiotics that have wide range of antimicrobial Amoxicillin
activity on Tetracyclines
Gram (+) ve, gram (-) ve Cephalosporins
Narrow spectrum antibiotics Benzylpenicillin
Antibiotics that have narrow range Cloxacillin
Of antimicrobial activity

8. Anti TB drugs at a glance

Isoniazid Rifampicin pyrazinamide streptomycin ethambutol

Mode of Cell wall DNA Unknown Protein Cell wall synthesis
action synthesis transcription Synthesis
Major Peripheral Febrile reactions Hepatitis 8th nerve damage Retrobulbar
adverse neuropathy Hepatitis Gastrointestinal Rash Neuritis 3
reactions Hepatitis Rash Disturbance Arthralgia
rash Gastrointestinal hyperuricaemia
Disturbance
Less Lupoid Interstitial Rash Nephrotoxicity Peripheral
common reactions Nephritis Photosensitization agranulocytosis Neuropathy
adverse Seizures Thrombocytopenia gout rash
reactions psychoses Hemolytic
anaemia

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8. Anti-fungal
Classification of antifungal drugs
Systemic antifungal drugs for systemic infections
a. Amphotericin B
b. Flucytosine
c. Azoies:
 Itraconazole
 Fluconazole
 Ketoconazole
 Voriconazole

d. Echinocandins
 Anidulafungin
 Caspofungin
 Micafungine

Systemic antifungal drugs for mucocutaneous infections

 Griseofulvin
 Terbinafine

Topical antifungal drugs

 Nystatin
 Topical azoles or imidazole (clotrimazole, miconazole)
 Ciclopiroxolamine
 Haloprogen
 Topical allylamines (terbinafine, naftifine)

9. Drugs used to treat Heart failure

Drugs used to treat heart failure
Renin-angiotensin system β-blockers Inotropic agents
blockers • Atenolol • Amrinone
ACE inhibitors • Carvedilol • Digoxin, Digitoxin
• Captopril • Metoprolol • Dopamine, Dobutamine
• Enalapril • Milrinone
• Fosinopril Diuretics
• Lisinopril • Bumetanide Aldosterone antagonists
• Quinapril • Frusemide • Spironolactone
• Ramipril • Metochlorothizide
• Metolazone
ARB
• Olmesartan Direct vasodilators
• Candesartan • Hydralazine
• Losartan • Isosorbide dinitrate
• Telmisartan • Sodium nitroprusside
• Valsartan

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10. Classification of anti arrhythmic drugs

Classification of anti-arrhythmic drugs by effect on the intracellular action potential

Class I: Membrane stabilising agents (sodium channel blockers)
• Block Na+ channel and prolong action potential
• Quinidine, disopyramide
• Block Na+ channel and shorten action potential
• Lidocaine, mexiletine
• Block Na+ channel with no effect on action potential
• Flecainide, propafenone
Class II: β-adrenoceptor antagonists (β-blockers)
• Atenolol, bisoprolol, metoprolol
Class III: Drugs whose main effect is to prolong the action potential
• Amiodarone, dronedarone, Sotalol
Class IV: Slow calcium channel blockers
• Verapamil, diltiazem
*Some drugs such as digoxin, ivabradin and adenosine have no place in this classification, while
others such as amiodarone have properties in more than one class.
[Davidson/23rd/479]

11. Drugs in blood disorder

Modes of action of anticoagulant and antithrombotic drugs
Mode of action Drug
Antiplatelet drugs
Cyclo-oxygenase (COX) inhibition Aspirin
Adenosine diphosphate (ADP) receptor Clopidogrel
inhibition Prasugrel
Ticagrelor
Glycoprotein IIb/IIIa inhibition Abciximab
Tirofiban
Eptifibatide
Phosphodiesterase inhibition Dipyridamole
Oral anticoagulants
Vitamin K antagonism Warfarin/coumarins
Direct thrombin inhibition Dabigatran
Direct Xa inhibition Rivaroxaban
Apixaban
Edoxaban
Injectable anticoagulants
Antithrombin-dependent inhibition of Heparin
thrombin and Xa LMWH
Antithrombin-dependent inhibition of Xa Fondaparinux
Danaparoid
Direct thrombin inhibition Argatroban
Bivalirudin

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12. Indications of diuretics

Loop diuretics Thiazide diuretics K+ sparring diuretics
Congestive cardiac failure Congestive cardiac Given with K+ losing diuretics in the
Acute pulmonary edema failure management of HTN.
Moderate hypertension Hypertension Management of refractory edema
Management of edema (e.g. Nephrogenic diabetes Primary aldosteronism
liver cirrhosis, nephrotic insipidus Secondary aldosteronism due to-
syndrome) Idiopathic • Nephrotic syndrome
Oliguric phase of ARF hypercalciuria • Cardiac failure
Hypercalcaemia Liver cirrhosis • Liver cirrhosis
Hyperkaelemia Nephrotic syndrome
SIADH
[Vision/7th/155]

Adverse effects of loop and thiazide diuretics

Renal side effects
• Hypovolaemia • Hyperuricaemia (gout)
• Hyponatraemia • Hypomagnesaemia
• Hypokalaemia • Hypercalciuria (loop)
• Metabolic alkalosis • Hypocalciuria (thiazide)
Metabolic side effects
• Glucose intolerance/hyperglycaemia • Hyperlipidaemia
Miscellaneous
• Hypersensitivity reactions • Acute pancreatitis/cholecystits
• Erectile dysfunction
[Davidson/23rd/355]
13. Adverse effect of steroid use:
I. Physiological-- Adrenal and /or Pituitary suppression by negative feedback
II. Pathological—
* Cardiovascular - Increase blood pressure by Na+ retention
*Gastrointestinal:
 Peptic ulceration exacerbation by inhibiting PG synthesis & increasing acid secretion
 Pancreatitis
*Bone and muscle: - Osteoporosis by Ca++ mobilization from bone
 Osteonecrosis, Pathological fracture
 Muscle wasting by protein catabolism

* Endocrine: Weight gain, Diabetes mellitus by hyperglycemia, impaired growth, Amenorrhea

*Skin: Thinning, Easy bruising increased susceptibility to infection:
 Delayed wound healing due to anti-inflammatory action
 Septicemia, Fungal infection, Tuberculosis due to immune suppression
*CNS: Depression, Euphoria, Steroid Psychosis, Insomnia
*Eye: Cataract

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• Sudden withdrawal of steroid causes:

 Adrenocortical insufficiency
 Weight loss
 Arthalgia
 Itchy skin nodule
 Conjunctivitis
 Rhinitis
14. Effects of drugs used in type 2 DM:
Insulin Sulphonylur Metformin Alpha- Thiazolidinedi DPP-4 GLP SGLT2
eas and glucosidase ones inhibitors receptor inhibitors
meglitinides inhibitors (glitazones (gliptins) agonists
Fasting blood ↓ ↓ ↓ ↓ ↓ ↓ ↓
glucose
Post-prandial ↓ ↓ ↓ ↓ ↓ ↓ ↓ ↓
blood glucose
Plasma ↑ ↑ ↓ ↓ ↓ ↑ ↑ ↑
insulin
Body weight ↑ ↑ → → ↑ → ↓ ↓
Cardiovascul No No Possible No Probable No Yes Yes
(pioglitazone)
ar benefit?
Risk of ++ + - - - - - -
hypoglycaemi
a
Tolerability Good Good Moderate Moderate Moderate Good Moderate Limited
experience
( = Small reduction: DPP.4 = dipeptidyl peptidase 4; GLP-1 = Glucagon-like peptide 1; SGL T2 = sodium and glucose
transporter 2)

15. Oxitocics:
 Oxytocin (gravid)
 Ergometrine (birth)
 Prostaglandin (both)
 Ketamine
 Quinine (3rd)
Tocolytics:
 Beta agonist/salbutamol
 Glycerin tri nitrate
 MgS04
 Alcohol
 Progesterone (natural)

16. Drugs used in induction of ovulation:

Stimulation of ovulation:
 Clomiphine citrate
 Letrozole
 hMG
 FSH
 hCG
 GnRH
 GnRH analogue

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Correction of biochemical abnormality:

 Metformin-insulin residtance
 Dexamithasone-Androgen excess
 Bromocryptine-hyperprolectinaemia

Substitution therapy:
 Hypothyroidism – Thyroxin
 DM – Anti diabetic drug
17. Antiemitic drugs

Antiemetic drugs

Antihistamines, Dopamine D2 Serotonin 5HT3

Anticholinergics receptor antagonisits receptor antagonists
 Dimenhydrinate • Metoclopramide • Ondansetron
 Hydroxyzine • Chlorpromazine • Granisetron
 Cyelizine • Prochlorperazine • Dolasetron
 Meelizine • Promethazine • Ramosetron
 Scopolamine • Haloperidol • Tropisetron
 Trimethobenzamide • Droperidol

Neurokinin-1 Others
receptor antagonists • Cannbinoids
• Aprepitant • Nabilone
• Fosaprepitant • Dronabinol
• Rolapitant • Nabiximol
• Dexamethasone
• Netupitant/
Palonosetron

42. Exam Night Topic

Systemic Pharmacology:
From here we may get 15 to 20 question. Though the syllabus is huge you need to clear your
conception and memorize classificaton & drugs name.

CNS Pharmacolgy:
01) Antidepressant drugs★★
02) Antipsychotic drugs★★★
03) Anticonvulsants ★★
04) Drugs for mania & bipolar disorder★
05) Sedative & hypnotics★★★

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06) Anticonvalsant★★
07) Anti PerkinsonDrugs★
08) Miotics★★
09) Mydriatics★★
10) Anti glaucoma drugs★★★
11) Drugs for acute migrane&migrane prophylaxis ★★★

Endocrinee pharmacology:
1) Anti diabetic agents & their property ★
2) Insulin preparation & side effect ★★
3) Side effect of OCP ★★
4) Ecbolics&tocolytics★
5) Induction of ovulation ★★★
6) Anti thyroid drug & their side effects★

Cardio, respiratory, renal, gastro Pharmacology:

1. Anti anginal agent★★
2. Drugs in heart failure★★★ ( including everything about digoxin)
3. Anti arrhythmic drugs & side effect of amiodarone★★
4. Hypertension (beta blocker, CCB, ACEI)★★★
5. Nitroglycerine★
6. Diuretics- side effects ★★
7. Nephrotoxic drug★★
8. Drugs in bronchial asthma★★
9. Anti histamine classification★★
10. Drugs for peptic ulcer★★★
11. Anti emitic drug ★★

Anti microbials and immune suppressive

1. Classification of antimicrobials according to mechanism of action★★★
2. Penicillin ★★
3. Cephalosporin★★
4. Protein synthesis inhibitor★★
5. Nucleic acid synthesis inhibitor★
6. Anti viral Drugs ★★
7. Anti fungal drugs ★★
8. Anti protozoal drugs. ★
9. Metronidazole indication & Side effects ★★
10. Anti ricketsial drug★
11. Amoebicidal drugs★
12. Drug resistance. ★★
13. Rational use of antibiotics ★
14. Anti tubercular drugs★★
15. Anti Cancer Drugs ★

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Drugs in Blood Disorder, Analgesic, Anaesthetics:

1. Anti platelet drugs ★★★
2. Anti coagulant drugs★★
3. Heparin★★
4. Warferin
5. Opioids★★★
6. NSAIDS. ★★
7. Anti Rheumatic Drugs ★★
8. Anaesthetic Classification ★
9. Lidocane ★★
10. General anaesthesia – preanaesthetic medication★
11. Induction & maintenance of GA ★★
12. Nitrous oxide★
13. Halothene★★
14. Ether★
15. Thiopental sodium★★
16. Ketamine ★★★
17. Propofol★★
18. Drugs avoided before OT★

43. Bibliography
1. Katzung 14th Edition
2. Vison 7th Edition Pharmacology
3. Goodman & Gilman Pharmacology
4. Davidson Principles & Practice of Medicine

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Previous Questions


Residency & Diploma Questions

01. Propranolol (Residency March 2024)

a) Enhances myocardial contraction
b) Decreases heart rate
c) Inhibits AV conduction
d) Promotes peripheral blood supply
c) Reduces stroke volume
Answer: F T T F T
Explanation:
Propranolol is non selective Beta blocker.

Mechanism of action:
Propranolol
↓
Inhibits Vasomotor conduction
↓
Decreases Sympathetic Discharge
↓
Vasodilation
↓
Decreased Blood Pressure

β Blocker / Propranolol:

Common use: Should not be used in /Contraindication:

-CVS: HTN, Angina, Arrhythmia, post MI, - Advanced heart failure, Acute/ Decompensated
HCM, SVT, HF heart failure
-Endocrine: hyper thyroid, -Heart block
phaeochromocytoma -Bronchial asthma
-CNS: Anxiety, Migraine, Essential tremor -Peripheral vascular disease
-Eye: Glaucoma -Diabetic patient receiving Insulin/ OHA
(masking S/S of hypoglycaemia)

Common Adverse effects: Withdrawal effect:

-Bradycardia, Hypotension, Heart block β blocker should not be withdrawn suddenly as
-Bronchospasm, Raynaud’s phenomenon It may cause Beta blocker withdrawal syndrome
Sexual interference/ Erectile Dysfunction -Rebound HTN
-↑Plasma lipoprotein (↑LDL, ↓HDL) -Precipitation of Angina
-Dangerous arrhythmia

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02. In a 30-year-old diabetic and hypertensive patient, the drug of choice is/ are
(Residency March 2024)
a) Atenolol
b) Amlodipinc
c) Labetalol
d) Losartan
e) Hydrochlorthiazide
Answer: F F F T F
Explanation:
The influence of comorbidity on choice of antihypertensive drug therapy
Class of drug Compelling indications Possible Caution Compelling
indications contraindications
α-blockers Benign prostatic hypertrophy -- Postural Urinary incontinence
hypotension,
heart failure1
ACE inhibitors Heart failure Chronic renal Renal Pregnancy
Left ventricular dysfunction, disease2 impairment2 Renovascular
post-MI or established CAD Type 2 diabetic PAD3 disease2
Type 1 diabetic nephropathy nephropathy
Secondary stroke
prevention4
Angiotensin II ACE inhibitor intolerance Left ventricular Renal Pregnancy
receptor Type 2 diabetic nephropathy dysfunction after impairment2
blockers Hypertension with left MI PAD3
ventricular hypertrophy Intolerance of
Heart failure in ACE- other
intolerant antihypertensive
patients, after MI drugs
Proteinuric or
chronic
renal disease2
Heart failure
β-blockers MI, angina --- Heart failure5 Asthma or chronic
Heart failure5 PAD obstructive
Diabetes (except pulmonary disease
with CAD) Heart block
Calcium channel Older patients, isolated Angina
blockers systolic
(dihydropyridine) hypertension
Calcium channel Angina Older patients Combination Atrioventricular
blockers with block, heart
(rate-limiting) β-blockade failure
Thiazides or Older patients, isolated --- Gout6
thiazide-like systolic
diuretics hypertension, heart failure,
secondary stroke prevention
1ln heart failure when used as monotherapy. 2ACE inhibitors or ARBs may be beneficial in chronic renal failure and

renovascular disease but should be used with caution, close supervision and specialist advice when there is established
and significant renal impairment. 3Caution with ACE inhibitors and ARBs in PAD because of association with
renovascular disease. 4In combination with a thiazide or thiazide-like diuretic. 5β-blockers are used increasingly to treat
stable heart failure but may worsen acute heart failure. 6Thiazides or thiazide-like diuretics may sometimes be necessary
to control BP in people with a history of gout, ideally used in combination with allopurinol.
(ACE = angiotensin-converting enzyme; ARBs = angiotensin II receptor blockers; CAD = coronary artery disease; MI =
myocardial infarction; PAD = peripheral arterial disease)

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03. Long term use of prednisolone may induce (Residency March 2024)
a) Diabetes mellitus
b) Bronchial asthma
c) Hypertension
d) Osteoarthritis
e) Peptic ulcer disease
Answer: T F T F T

Explanation:
Some of the common short-term side effects of prednisone include:
 Fluid retention causing swelling in the face, hands, ankles, and feet
 Increased appetite
 Insomnia (trouble sleeping)
 Restlessness
 Stomach pain and indigestion
 Mood changes
 Increased blood sugar
 Increased sweating and hot flash

long-term side effects of prednisone

 Weight gain
 Osteoporosis: Bone loss (decreased bone density and increased risk of bone fractures)
 Skin bruising
 Thinning of skin and hair
 Moon face: the face can swell and get rounder
 Muscle weakness
 High blood sugar
 Delayed or impaired wound healing
 Increased risk of bacterial, viral, and fungal infections
 Eye problems such as cataracts or glaucoma (increased eye pressure)
 Venous thromboembolism: Blood clots - there are findings that high doses of prednisone can
lead to blood clots. However, various confounding factors could account for blood clot
formation. Therefore, the risks for VTE are evaluated on a case-by-case basis.
 Decreased growth in children
 Psychotic symptoms

04. Dopamine (Residency March 2024)

a) Is a synthetic catecholamine
b) Deficiency in basal ganglia leads to Parkinson's disease
c) Is the immediate precursor of norepinephrine
d) Is used in anaphylactic shock
e) Is a central neurotransmitter
Answer: T T F F T
Explanation:
a) The catecholamines dopamine, norepinephrine, and epinephrine are synthesized from dietary
tyrosine in selected central and peripheral neurons and in the adrenal medulla by the
sequential action of enzymes in a synthetic pathway.
b) In perkinson disease dopamine is reduced, Ach concentration is increased, as dopamine has
regulatory effect on Acetylcholine,

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c) Dopamine itself is used as precursor in the synthesis of the neurotransmitters

norepinephrine and epinephrine. Dopamine is converted into norepinephrine by the
enzyme dopamine β-hydroxylase, with O2 and L-ascorbic acid as cofactors.
d) Adrenaline is used in anaphylactic shock
e) Dopamine is a neurotransmitter that is produced in the substantia nigra, ventral tegmental
area, and hypothalamus of the brain.

Features of Dopamine:
Dopamine
Mechanism:
Dopamine is a natural catecholamine formed by the decarboxylation of 3,4- dihydrroxyphenylalanine
(DOPA). It is a precursor to norepinephrine and is also a neurotransmitter in certain areas of the
central nervous system, especially in the nigrostriatal tract, and in a few peripheral sympathetic
nerves. Dopamine produces positive chronotropic and inotropic effects on the myocardium, resulting
in increased heart rate and cardiac contractility. This is accomplished directly by exerting an agonist
action on beta – adrenoceptors and indirectly by causing release of norepinephrine from storage sites
in sympathetic nerve endlings

Indication:
 Hypotension
 Shock
 Septicemia

Adverse Effect:
Techycardia, ectopic beats, anginal pain, vasoconstriction, Palpitation nausea, hypotension, vomiting,
headache, dyspnea, aberrant conduction, bradycardia, widened QRS complex, hypertension and
gangrene.

05. Warfarin (Residency March 2024)

a) Can be given by IV Route
b) Has high margin of safety
c) Is used in deep vein thrombosis
d) Overdose can be antagonized by giving vitamin K
e) Causes teratogcnesis
Answer: F F T T T
Explanation:
Warfarin:
• Warfarin is Coumarin derivative.
• Warfarin has the structural similarity of vit-K. It is vit-K antagonist.
• Warfarin competitively inhibits the enzyme vit-K epoxide reductase, thus inhibits the synthesis of
vit-K dependent clotting factor (II, VII, IX, X).
• Warfarin is rapidly absorbed after oral administration (100% bioavailability with little individual
patient variation). Although food may delay absorption.
• Warfarin is 99 percent bound to plasma albumin, which prevents its diffusion into the
cerebrospinal fluid, urine, and breast milk.
• However, drugs that have a greater affinity for the albumin binding site, such as sulfonamides,
can displace the anticoagulant and lead to a transient, elevated activity.
• Warfarin readily crosses the placental barrier. It is teratogenic.
• Its onset of action is delayed.

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• The mean half life of warfarin is approximately 40 hours, but this value is highly variable among
individuals.
• Prothrombin time, a measure of the extrinsic pathway, may be used to monitor warfarin therapy.
The result is reported as international normalized ratio (INR). Normal INR is 1. In warfarin therapy,
INR should increase to 2.5-3.5. INR <2.5: dose of warfarin should be increased INR >3.5: drugs
to be stopped.

Fate: The products of warfarin metabolism, catalyzed by the cytochrome P 450 system, are inactive. After
conjugation to glucuronic acid, they are excreted in the urine and stool.

Therapeutic uses:
Warfarin is used to prevent the progression or recurrence of acute deep vein thrombosis or pulmonary
embolism after initial heparin treatment. It is also used for the prevention of venous thromboembolism
during orthopaedic or gynecologic surgery. Prophylactically, it is used in patients with acute
myocardial infarction, prosthetic heart valves, or chronic atrial fibrillation.

Adverse effects:
• Bleeding disorders- treated by withdrawal of the drug and administration of oral vitamin K1; severe
bleeding requires that greater doses of the vitamin be given intravenously. Whole blood, frozen
plasma, or plasma concentrates of the blood factors may also be employed to arrest hemorrhaging.
• Skin lesions and necrosis are rare complications of warfarin therapy and are observed primarily in
women.
• Purple toe syndrome, a painful, blue-tinged discoloration of the toe caused by cholesterol emboli from
plaques, has also been observed with warfarin therapy.
Contraindications:
• Recent trauma, injury
• Active internal bleeding
• Severe hypertension
• Non-thromboembolic stroke
• Major surgery
• Pre-existing hemostatic defects
• Pregnancy as it is teratogenic
• Lactating mother
• Threatened abortion
• Severe liver and renal disease
• Hypoprothrombinemia.

06. Linagliptin (Residency March 2024)

a) Is an incretin mimetic
b) Releases insulin from beta 1-cell of pancreas
c) Can cause invariable hypoglycemia
d) Activates the enzyme dipeptidyl peptidase-4
e) Is an antagonist of GLP-1
Answer: T F F F F
Explanation:
Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like
peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).

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Effects of drugs used in Treatment of type 2 diabetes:

Insulin Sulphonylur Metformin Alpha- Thiazolidinedi DPP-4 GLP SGLT2
eas and glucosidase ones inhibitors receptor inhibitors
meglitinides inhibitors (glitazones (gliptins) agonists

Fasting blood ↓ ↓ ↓ ↓ ↓ ↓ ↓
glucose
Post-prandial ↓ ↓ ↓ ↓ ↓ ↓ ↓ ↓
blood glucose
Plasma insulin ↑ ↑ ↓ ↓ ↓ ↑ ↑ ↑
Body weight ↑ ↑ → → ↑ → ↓ ↓
Cardiovascular No No Possible No Probable No Yes Yes
benefit? (pioglitazone
)
Risk of ++ + - - - - - -
hypoglycaemia
Tolerability Good Good Moderate Moderate Moderate Good Moderate Limited
experience
( = Small reduction: DPP.4 = dipeptidyl peptidase 4; GLP-1 = Glucagon-like peptide 1; SGL T2 = sodium and glucose
transporter 2)

07. Spironolactone (Residency March 2024)

a) Is an aldosteronc antagonist
b) May produce g,ynaecomastia
c) Acts on loop of henle
d) Is contraindicated in nephrotic syndrome
e) May produce hypocalacmia
Answer: T T F F F (No effect on calcium concentration)
Explanation:
Classification of diuretics according to site of action:
Site-I: (PCT) Osmotic diuretics:
 Mannitol, lsosorbide, Urea
Carbonic anhydrase inhibitors:
 Acetazolamide
 Ethoxzolamide
Methozolamide
 Dorzolamide
 Topiramate
Site-II: ALLH High ceiling diuretics (Excrete 15-25% of filtered Na+)
 Frusemide
 Torsemide
 Bumetanide
 Piretanide
 Ethacrynic acid
Site-III: DCT Moderate efficacy diuretics (Excrete 5-10% of filtered Na+) Thiazides
and related diuretics:
 Chlorothiazide
 Hydrochlorothiazide
 Trichlomethiazide
 Chlorthalidone
 Quinethazone
 Metolazone
 Indapamide
Site-IV: CDs K+ sparing/low efficacy diuretics (Excrete <5% of filtered Na+)
 Aldosterone antagonists: Spironolactone, Eplerenone
 Epithelial Na-channel blocker: Amiloride, triamterene

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Renal side effects

• Hypovolaemia • Hyperuricaemia (gout)
• Hyponatraemia • Hypomagnesaemia
• Hypokalaemia • Hypercalciuria (loop)
• Metabolic alkalosis Hypocalciuria (thiazide)
Metabolic side effects
• Glucose intolerance/hyperglycaemia • Hyperlipidaemia
Miscellaneous
• Hypersensitivity reactions • Acute pancreatitis/cholecystits
• Erectile dysfunction
[Davidson/23rd/355]
Side effects of spironolactone:
• Gynaecomastia
• Impotence
• Benign prostatic hyperplasia
• Amenorrhea
• Metabolic acidosis in cirrhotic patient.
• Hyperkalaemia
• Endocrine abnormalities are:

08. Drug/s given in the treatment of MDR tuberculosis is/are (Residency March 2024)
a) Bedaquilone
b) Linezolid
c) Levolloxacin
d) Streptomycin
e) Rifampicin
Answer: T T T F F
Explanation: Multidrug-resistant TB (MDR TB) is caused by TB bacteria that are resistant to at least
isoniazid and rifampin, the two most potent TB drugs. These drugs are used to treat all persons with
TB disease.
09. Drugs metabolized by acetylation include (Residency March 2024)
a) Acetaminophen
b) Diazepam
c) Isoniazid
d) Morphine
e) Sulphonamide
Answer: F F T F T
Explanation:
Drugs metabol ized by acetylation
Types of conjugations Types of substrates Example of Drugs
Acetylation Amines Sulfonamides
Isoniazid, histamine
Clonazepam
Dapsone, Procainamide hydralazine,
sulphapyridine, sulphonamide, dapsone,

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10. Receptors have been paired correctly with their agonists are (Residency March
2024)
a) a2 receptor - clonidine
b) β1 receptor - terbutaline
c) β 2 receptor - salbutamol
d) D2 receptor - chlorpromazine
e) 5HT3 receptor - ondansetron
Answer: T F T F F
Explanation:
b) beta 2 agonist
d) D2 antagonist
e) 5HT3 antagonist

11. Pregabalin (Residency March 2024)

a) Acts by inhibiting presynaptic Ca2+ channel
b) Acts by activating GABA A ion channel
c) Acts rapidly
d) Increases weight
e) Is useful for focal seizures
Answer: T T F T T
Explanation:
Pregabalin:
They exhibit a high affinity for the α2δ-1 and α2δ-2 subunits of voltage-activated calcium channels,
wherein binding of gabapentinoids inhibits cellular calcium influx and attenuates
neurotransmission, mimic the action of GABA and to modulate GABA metabolism.

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Most common adverse effect:

 Drowsiness/lassitude
 Cutaneous
 Ulcers in mouth due to pancytopenia
 Easy bruising
 Fluid retention (leg)
 Weight gain
 Allergic eruptions
 Stevens-Johnsons syndrome
 Other side effects Cholestasis
 Cholestasis
 Hepatotoxicity
 Dyskinesia
 Reversible acute renal allografit dysfunction

12. The pharmacokinetic half-life of the following drugs resemble their

pharmacodynamic half-life (Residency March 2024)
a) Salbutumol
b) Phenelzine
c) Dobutamine
d) Omeprazolc
e) Cyclophosphamide
Answer: T (3 to 5 hours) T (11.6 hours) F (2 min) F (45 min) T (3 to 12 hours)
A pharmacodynamic parameter relating time-dependent changes of the effect with time-dependent changes of
concentrations has yet to be developed. In pharmacokinetics, half-lives (T1/2kin) are used to describe the
relation between concentration (C) and time (t). In pharmacodynamics, often the sigmoid Emax model and the
Hill equation are used (E = Emax CH/ (EC50H + CH)) to describe the relation between effect (E) and
concentration (C).

Pharmacokinetic and pharmacodynamic half life differs in drugs with very short half life. (Source: Hypothesis
from different researces)

13. Drug/s used in acute attack of migraine is/are (Residency March 2024)
a) Gabapentin
b) Ibuprofen
c) Sumatriptan
d) Propranolol
e) Ergotamine
Answer: F TT F T
Explanation :
Drugs used in acute attack of Migraine:
• NSAID
• Antiemitics
• 5 HT1 agonist- Sumatriptan, Rizatriptan, Zolmitriptan.
• Ergot alkaloids- Ergotamine
•
Drugs used in Migrane prophylaxis:
• Verapamil
• Valporic acid, Topiramate

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• Pizotifen (Antihistamine & 5 HT antagonist)

• Amitryptyline, Dosulepine
• Flunarizine (Both Ca2+ & Na + channel blocker)
• Methysergide
• Propranolol

SBA
14. Stem: A 25-year-old man has been diagnosed as a case of syphilis on the basis of
personal history and detection of Trepanoma pallidum on clinical and laboratory
investigation. Lead in: Which antibiotic will be the choice for shortest duration of
treatment?
a) Benzathine penicillin G
b) Aztreonam
c) Ceftriaxone
d) Vancomycin
e) Cefixime
Answer: C
Explanation:
a) 3 weeks.
b) 10 days
c) 7 days
d) 10 days
e) 14 days

15. Stem: A 59-year-old man with a history of type-2 diabetes mellitus and benign
prostatic hypertrophy presence of acute urinary retention. His serum creatinine level
is 2mg/dl. Lead in: Which one of the following drugs should be withheld? (Residency
March 2024)
a) c
b) Paroxetine
c) Gliclazide
d) Metformin
e) Atenolol
Answer: C
Explanation:
It should not be used in patients with severe renal impairment

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FCPS Questions

01. Drug used for cytoprotective in PUD? (FCPS January 2022)

a) Ranitidine
b) Piranzipine
c) Sucralfate
d) Sodium bicarbonate
e) Amoxicillin
Answer: C
Explanation:
Treatment of peptic ulcer
• Eradication of H. pylori infections
• Hyposecretory drugs.
 H2 receptor blockers
 Antimuscarinic drugs Proton pump inhibitors

• Mucosal cytoprotective agents.

 Prostaglandin analogues
 Sucralfate (CarafateR)
• Neutralizing agents (antacids).
02. Anti TB that causes optic neuritis? (FCPS July 2022)
a) Ethambutol
b) Pyrazinamide
c) Streptomycin
d) Rifampicin
e) Amikacin
Answer: A
Ethambutol cause retrobulbar optic neuritis and red green colour blindness

03. Non-sedative Anti histamine is- (FCPS January 2022)

a) Loratidine
b) Carbinoxamine
c) Diphenhydramine
d) Promethazine
e) Cyclizine
Answer: A
Explanation:
Second-generation (selective, non-sedating)
• 2-generation Hi-antihistamines are newer → more selective → significantly reducing of the
occurrence of ADR, such as sedation.
They are very polar → do not cross the blood-brain barrier and act mainly outside the CNS.
Loratadine
Cetirizine The most common ADR:
Ketotifen drowsiness, fatigue, headache, nausea and dry mouth
Acrivastine Prolongation QT interval -p polymorphic ventricular
Terfenadine tachyarrithmia (Torsades de pointes)!!!!
Quifenadine

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04. Drug acts by inhibition of 30 s ribosomal unit? (FCPS January 2021)

a) Chloramphenicol
b) Sulfonamide
c) Tetracycline
d) Cephalosporin
e) Trimethoprim
Answer: C
05. Antibiotics acts by cell wall synthesis? (FCPS January 2023)
a) Aminoglycoside
b) Tetracycline
c) Cycloserine
d) Sulfonamide
e) Metronidazole
Answer: C
06. Ethacrynic Acid acts through? (FCPS July 2023)
a) Inhibition of carbonic Anhydrase in PCT
b) Inhibition of Na+ k+ /2cl- co transporter in thick ascending limb of loop of henle
c) Inhibition of Na + cl- co transporter in DCT
d) Block Na + channel
e) Block Aldosterone receptor in collecting tubule.
Answer: B
Ethacrynic acid is a loop diuretic

07. Thiazide diuretics causes? (FCPS January 2020)

a) Hyperkalemia
b) Metabolic Alkalosis
c) Hypoglycemia
d) Hypocalciurea
e) Hypernatrimia
Answer: B
08. A child with Bronchial asthma which drug should be used for bronchodilator?
(FCPS July 2023)
a) Hydrocortisone
b) Necromil Sodium
c) Montelukast
d) Fruticasone
e) Theophyline
Answer: E
Explanation:
Classification of drugs for asthma
• Bronchodilators:
1. β-Sympathomimetics: Salbutamol. Terbutaline. Bambuterol. Salmeterol. Formoterol.
Ephedrine
2. Methyl Xanthines: Theophylline, Aminophylline, Choline theophyllinate. Hydroxyethyl
theophylline. Doxophylline.
3. Anticholinergics: Ipratropium bromide. Tiotropium bromide

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Leukotriene Antagonists: Montelukast. Zafirlukast

MAST CELL STABILIZERS: Sodium chromoglycate, Ketotifen

Corticosteroids
 Systemic: Hydrocortisone. Prednisolone
 Inhalational: Beclomethasone. Budesonide, Fluticasone. Flunisolide
 ANTI Ig-E ANTIBODY: Omalizumab

09. Bactericidal drug- (FCPS January 2022)

a) Sulfonamide
b) Tetracycline
c) Isoniazide
d) Erythromycin
e) Chloramphenicol
Answer: C

10. A 10-year-old child presented with status epilepticus how will u manage immediately?
(FCPS January 2023)
a) I/V Diazepum
b) I/M phenytoin
c) I/V pheno barbitone
d) Oral gabapentin
e) I/V Midazolam
Answer: A
11. Chloramphenicol does not cause? (FCPS July 2022)
a) Bacteriostatic drug
b) Gray baby syndrome
c) GI upset
d) Irreversible dose related bone marrow suppression
e) Neuritis
Answer: D
Explanation:
Chloramphenicol: Adverse Effects
• Hematologic
- Dose-related erythroid suppression is common, but in addition aplastic anemia occurs
• Gray baby syndrome
-The gray color is due to shock (hypotension and tissue hypoperfusion). Chloramphenicol
accumulates in neonates (especially if premature) due to reduced glucuronidation in the
immature liver
• Other effects
-Chloramphenicol can also cause sore mouth, diarrhea, encephalopathy and optic neuritis
12. What is the mechanism of action of methimazole? (FCPS January 2021)
a) Binds to the 30 s subunit of bacterial chromosome.
b) Inhibit cholesterol synthesis
c) Inhibit the addition of Iodide to thyroglobulin
d) Inhibit release of iodothyronines
e) Irridates and destroys the thyroid gland.
Answer: C

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13. Causes of gynecomastia does not include? (FCPS July 2022)

a) Digoxin
b) Cyclosporin
c) Cimetidine
d) Omeprazole
e) spironolactone
Answer: B
Explanation:
Discos
 Digoxin
 Isoniazid
 Spironolactone
 Cimetidine
 0estrogens
 Stilboestrol
14. Phase II reactions of a drug biotransformation: (FCPS January 2023)
a) Decreases its water solubility.
b) Includes activity of cytochrom P-450.
c) Usually leads to inactivation of the drug.
d) Does not include acetylation.
e) Occur at the same rate in adults and the new born.
Answer: C
15. A 3-year-old child has been admitted to emergency with suspicious of atropine
overdose as there are: (FCPS July 2021)
a) Abdominal cramps.
b) Increased gastric secretion.
c) Increased cardiac rate.
d) Papillary constriction.
e) Increased urinary frequency.
Answer: C
Explanation:
Excess doses of atropine sulfate may cause side effects such as palpitations, dilated pupils,
difficulty swallowing, hot dry skin, thirst, dizziness, restlessness, tremor, fatigue, and problems with
coordination.
16. Which of the following statements best describes the mechanism of action of
benzodiazepines? (FCPS July 2023)
a) Benzodiazepines activate GABAB-receptors in the spinal cord.
b) They inhibit GABA-transaminase leading to increased levels of GABA.
c) They block glutamate receptors in hierarchical neuronal pathways in the brain.
d) Benzodiazepines increase the frequency of Cl--channels opening which are coupled to GABAA
receptors.
e) They are direct-acting GABA receptor agonists in the CNS.
Answer: D

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17. Which of the following drugs when used for prolonged period in the maintenance treatment of
tonic-clonic seizures can lead to increased metabolism of warfarin like drugs? (FCPS July 2022)
a) Phenobarbital
b) Meprobamate
c) Chlordiazepoxide
d) Triazolam.
e) Zolpidum
Answer: A
Explanation:
Phenobarbital is an anticonvulsant and enzyme inducer.
18. Epinephrine added to a solution of lidocaine for local anesthesia will: (FCPS July 2020)
a) Cause cyanosis locally.
b) Increase the risk of convulsions.
c) Increase the duration of local anesthesia.
d) Increase the absorption of lidocaine.
e) Decrease the heart rate when absorbed.
Answer: C

Explanation:
Vasoconstrictors (epinephrine) are added to local anesthetics to counteract their vasodilatory action by
constricting blood vessels, thus decreasing blood flow to the injection area and prolonged action of anesthetics
19. Cephalosporins show their antimicrobial action by: (FCPS January 2023)
a) Binding to cytoplasmic receptor proteins.
b) Inhibition of beta-lactamases.
c) Inhibition of transpeptidation reactions.
d) Interference with the synthesis of ergosterol.
e) Inhibition of the synthesis of precursors of peptidoglycans.
Answer: C

20. The mechanism underlying the resistance of Gram +ve organisms to macrolides is (FCPS
July 2023)
a) Decreased drug permeability of the cytoplasmic membrane.
b) Methylation of binding sites on the 50-S ribosomal subunit.
c) Decreased activity of uptake mechanism.
d) Formation of estrases that hydrolyze the lactone ring.
e) Formation of acetyl transferase that inactivates macrolides.
Answer: B
Explanation:
Since macrolids work on 50 S subunit, mechanism of resistance involves Methylation of binding sites on the
50-S ribosomal subunit.

21. Doxycycline is: (FCPS January 2022)

a) Bactericidal.
b) Not excreted in the feces.
c) Having a short elimination half-life.
d) Not effective in lyme disease.
e) Not as effective as tetracycline against [Link].
Answer: E

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22. Which of the followings is useful topically for genital herpes infection? (FCPS July 2023)
a) Acyclovir.
b) Amantadine.
c) Ritonavir.
d) Trifluridine.
e) Foscarnet.
Answer: A
23. Acute hemorrhage cystitis is a common toxic effect seen with: (FCPS January 2020)
a)
Vincristine.
b)
Tamoxifen.
c)
Doxorubicin.
d)
Cyclophosphamide.
e)
Fluorouracil.
Answer: D
Explanation:
Hematuria can be caused by medications, such as blood thinners, including heparin, warfarin (Coumadin) or
aspirin-type medications, penicillins, sulfa-containing drugs and cyclophosphamide (Cytoxan).
24. A 30-year-old male suffering from cerebral edema will be best treated with: (FCPS July
2020)
a) Furosemide.
b) Amiloride.
c) Ethacrynic acid.
d) Mannitol.
e) Acetazolamide.
Answer: D
Explanation:
Mannitol caused osmotic diuresis, and decrease cerebral edema. Osmotic diuretics such as mannitol and
hyperosmotic saline increase blood osmolality acutely, thus reducing brain water content (mainly in healthy
brain tissue with an intact blood-brain barrier) and hence brain bulk and ICP.
25. Which of the following is a prophylactic anti-asthmetic agent that stabilizes mast cells:
(FCPS January 2023)
a) Ipratropium.
b) Prednisone.
c) Terbutaline.
d) Cromolyn.
e) Aminophyllin
Answer: D
Explanation:
Classification of drugs for asthma
• Bronchodilators:
 β-Sympathomimetics: Salbutamol. Terbutaline. Bambuterol. Salmeterol. Formoterol. Ephedrine
 Methyl Xanthines: Theophylline, Aminophylline, Choline theophyllinate. Hydroxyethyl theophylline.
Doxophylline.
 Anticholinergics: Ipratropium bromide. Tiotropium bromide
• LEUKOTRIENE ANTAGONISTS: Montelukast. Zafirlukast
• MAST CELL STABILIZERS: Sodium chromoglycate, Ketotifen
• Corticosteroids
1. Systemic: Hydrocortisone. Prednisolone
2. Inhalational: Beclomethasone. Budesonide, Fluticasone. Flunisolide
• ANTI Ig-E ANTIBODY: Omalizumab

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