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Medicinal Chemistry and Pharmacology Overview

The document outlines the syllabus for three subjects: Medicinal Chemistry I, Pharmacology I, and Pharmacognosy and Phytochemistry I, each with specific objectives and course content. Medicinal Chemistry focuses on drug structure, chemistry, and therapeutic value, while Pharmacology covers drug actions and effects on living organisms. Pharmacognosy emphasizes the identification and evaluation of crude drugs and their medicinal properties.

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6 views9 pages

Medicinal Chemistry and Pharmacology Overview

The document outlines the syllabus for three subjects: Medicinal Chemistry I, Pharmacology I, and Pharmacognosy and Phytochemistry I, each with specific objectives and course content. Medicinal Chemistry focuses on drug structure, chemistry, and therapeutic value, while Pharmacology covers drug actions and effects on living organisms. Pharmacognosy emphasizes the identification and evaluation of crude drugs and their medicinal properties.

Uploaded by

hekaf75079
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

SEMESTER IV

BP402T. MEDICINAL CHEMISTRY – I (Theory)


45 Hours
Scope: This subject is designed to impart fundamental knowledge on the structure,
chemistry and therapeutic value of drugs. The subject emphasizes on structure activity
relationships of drugs, importance of physicochemical properties and metabolism of
drugs. The syllabus also emphasizes on chemical synthesis of important drugs under each
class.
Objectives: Upon completion of the course the student shall be able to
1. understand the chemistry of drugs with respect to their pharmacological activity
2. understand the drug metabolic pathways, adverse effect and therapeutic value of
drugs
3. know the Structural Activity Relationship (SAR) of different class of drugs
4. write the chemical synthesis of some drugs
Course Content:

Study of the development of the following classes of drugs, Classification, mechanism of


action, uses of drugs mentioned in the course, Structure activity relationship of selective
class of drugs as specified in the course and synthesis of drugs superscripted (*)

UNIT- I 10 Hours

Introduction to Medicinal Chemistry


History and development of medicinal chemistry
Physicochemical properties in relation to biological action
Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein
binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.
Drug metabolism
Nonmicosomal
Drug metabolism principles- Phase I and Phase II.
Metabolism
Factors affecting drug metabolism including stereo chemical aspects.

UNIT- II 10 Hours

Drugs acting on Autonomic Nervous System

Adrenergic Neurotransmitters:
Biosynthesis and catabolism of catecholamine.
Adrenergic receptors (Alpha & Beta) and their distribution.

Sympathomimetic agents: SAR of Sympathomimetic agents


Direct acting: Nor-epinephrine, Epinephrine, Phenylephrine*, Dopamine,


Methyldopa, Clonidine, Dobutamine, Isoproterenol, Terbutaline,
Salbutamol*, Bitolterol, Naphazoline, Oxymetazoline and Xylometazoline.
• Indirect acting agents: Hydroxyamphetamine, Pseudoephedrine,
Propylhexedrine.
• Agents with mixed mechanism: Ephedrine, Metaraminol.

Adrenergic Antagonists:
Alpha adrenergic blockers: Tolazoline*, Phentolamine,
Phenoxybenzamine, Prazosin, Dihydroergotamine, Methysergide.
Beta adrenergic blockers: SAR of beta blockers, Propranolol*,
Metibranolol, Atenolol, Betazolol, Bisoprolol, Esmolol, Metoprolol,
Labetolol, Carvedilol.

UNIT-III 10 Hours

Cholinergic neurotransmitters:

Biosynthesis and catabolism of acetylcholine.


Cholinergic receptors (Muscarinic & Nicotinic) and their distribution.

Parasympathomimetic agents: SAR of Parasympathomimetic agents


Direct acting agents: Acetylcholine, Carbachol*, Bethanechol,
Methacholine, Pilocarpine.
Indirect acting/ Cholinesterase inhibitors (Reversible & Irreversible):
Physostigmine, Neostigmine*, Pyridostigmine, Edrophonium chloride,
Tacrine hydrochloride, Ambenonium chloride, Isofluorphate, Echothiophate
iodide, Parathione, Malathion.
Cholinesterase reactivator: Pralidoxime chloride.

Cholinergic Blocking agents: SAR of cholinolytic agents


Solanaceous alkaloids and analogues: Atropine sulphate, Hyoscyamine
sulphate, Scopolamine hydrobromide, Homatropine hydrobromide,
Ipratropium bromide*.
Synthetic cholinergic blocking agents: Tropicamide, Cyclopentolate
hydrochloride, Clidinium bromide, Dicyclomine hydrochloride*,
Glycopyrrolate, Methantheline bromide, Propantheline bromide,
Benztropine mesylate, Orphenadrine citrate, Biperidine hydrochloride,
Procyclidine hydrochloride*, Tridihexethyl chloride, Isopropamide iodide,
Ethopropazine hydrochloride.

UNIT- IV 08 Hours

Drugs acting on Central Nervous System


A. Sedatives and Hypnotics:
Benzodiazepines: SAR of Benzodiazepines, Chlordiazepoxide, Diazepam*,
Oxazepam, Chlorazepate, Lorazepam, Alprazolam, Zolpidem
Barbiturtes: SAR of barbiturates, Barbital*, Phenobarbital, Mephobarbital,
Amobarbital, Butabarbital, Pentobarbital, Secobarbital
Miscelleneous:
Amides & imides: Glutethmide.
Alcohol & their carbamate derivatives: Meprobomate, Ethchlorvynol.
Aldehyde & their derivatives: Triclofos sodium, Paraldehyde.

B. Antipsychotics
Phenothiazeines: SAR of Phenothiazeines - Promazine hydrochloride,
Chlorpromazine hydrochloride*, Triflupromazine, Thioridazine
hydrochloride, Piperacetazine hydrochloride, Prochlorperazine maleate,
Trifluoperazine hydrochloride.
Ring Analogues of Phenothiazeines: Chlorprothixene, Thiothixene,
Loxapine succinate, Clozapine.
Fluro buterophenones: Haloperidol, Droperidol, Risperidone.
Beta amino ketones: Molindone hydrochloride.
Benzamides: Sulpieride.

C. Anticonvulsants: SAR of Anticonvulsants, mechanism of anticonvulsant


action
Barbiturates: Phenobarbitone, Methabarbital. Hydantoins:
Phenytoin*, Mephenytoin, Ethotoin Oxazolidine diones:
Trimethadione, Paramethadione Succinimides:
Phensuximide, Methsuximide, Ethosuximide* Urea and epilepsy
monoacylureas: Phenacemide, Carbamazepine*
Benzodiazepines: Clonazepam
Miscellaneous: Primidone, Valproic acid , Gabapentin, Felbamate

UNIT – V 07 Hours

Drugs acting on Central Nervous System


General anesthetics:
Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane,
Sevoflurane, Isoflurane, Desflurane.
Ultra short acting barbitutrates: Methohexital sodium*, Thiamylal
sodium, Thiopental sodium.
Dissociative anesthetics: Ketamine hydrochloride.*

Narcotic and non-narcotic analgesics


Morphine and related drugs: SAR of Morphine analogues, Morphine
sulphate, Codeine, Meperidine hydrochloride, Anilerdine hydrochloride,
Diphenoxylate hydrochloride, Loperamide hydrochloride, Fentanyl citrate*,
Methadone hydrochloride*, Propoxyphene hydrochloride, Pentazocine,
Levorphanol tartarate.
Narcotic antagonists: Nalorphine hydrochloride, Levallorphan tartarate,
Naloxone hydrochloride.
Anti-inflammatory agents: Sodium salicylate, Aspirin, Mefenamic acid*,
Meclofenamate, Indomethacin, Sulindac, Tolmetin, Zomepriac, Diclofenac,
Ketorolac, Ibuprofen*, Naproxen, Piroxicam, Phenacetin, Acetaminophen,
Antipyrine, Phenylbutazone.


BP 404 T. PHARMACOLOGY-I (Theory)
45 Hrs
Scope: The main purpose of the subject is to understand what drugs do to the living
organisms and how their effects can be applied to therapeutics. The subject covers the
information about the drugs like, mechanism of action, physiological and biochemical
effects (pharmacodynamics) as well as absorption, distribution, metabolism and excretion
(pharmacokinetics) along with the adverse effects, clinical uses, interactions, doses,
contraindications and routes of administration of different classes of drugs.
Objectives: Upon completion of this course the student should be able to
1. Understand the pharmacological actions of different categories of drugs
2. Explain the mechanism of drug action at organ system/sub cellular/
macromolecular levels.
3. Apply the basic pharmacological knowledge in the prevention and treatment of
various diseases.
4. Observe the effect of drugs on animals by simulated experiments
5. Appreciate correlation of pharmacology with other bio medical sciences
Course Content:
UNIT-I 08 hours
1. General Pharmacology
a. Introduction to Pharmacology- Definition, historical landmarks and scope of
pharmacology, nature and source of drugs, essential drugs concept and routes of
drug administration, Agonists, antagonists( competitive and non competitive), spare
receptors, addiction, tolerance, dependence, tachyphylaxis, idiosyncrasy, allergy.
b. Pharmacokinetics- Membrane transport, absorption, distribution, metabolism and
excretion of drugs .Enzyme induction, enzyme inhibition, kinetics of elimination
UNIT-II 12 Hours

General Pharmacology
a. Pharmacodynamics- Principles and mechanisms of drug action. Receptor theories
and classification of receptors, regulation of receptors. drug receptors interactions
signal transduction mechanisms, G-protein–coupled receptors, ion channel receptor,
transmembrane enzyme linked receptors, transmembrane JAK-STAT binding
receptor and receptors that regulate transcription factors, dose response
relationship, therapeutic index, combined effects of drugs and factors modifying
drug action.
b. Adverse drug reactions.
c. Drug interactions (pharmacokinetic and pharmacodynamic)
d. Drug discovery and clinical evaluation of new drugs -Drug discovery phase,
preclinical evaluation phase, clinical trial phase, phases of clinical trials and
pharmacovigilance.


UNIT-III 10 Hours
2. Pharmacology of drugs acting on peripheral nervous system
a. Organization and function of ANS.
[Link] transmission,co-transmission and classification of neurotransmitters.
Atropine
c. Parasympathomimetics, Parasympatholytics, Sympathomimetics, sympatholytics.
Neostigmine
d. Neuromuscular blocking agents and skeletal muscle relaxants (peripheral).
e. Local anesthetic agents.
f. Drugs used in myasthenia gravis and glaucoma

UNIT-IV 08 Hours
3. Pharmacology of drugs acting on central nervous system
a. Neurohumoral transmission in the [Link] emphasis on importance of various
neurotransmitters like with GABA, Glutamate, Glycine, serotonin, dopamine.
b. General anesthetics and pre-anesthetics.
c. Sedatives, hypnotics and centrally acting muscle relaxants.
d. Anti-epileptics
e. Alcohols and disulfiram

UNIT-V 07 Hours
3. Pharmacology of drugs acting on central nervous system
a. Psychopharmacological agents: Antipsychotics, antidepressants, anti-anxiety agents,
anti-manics and hallucinogens.
b. Drugs used in Parkinsons disease and Alzheimer’s disease.
c. CNS stimulants and nootropics.
d. Opioid analgesics and antagonists
e. Drug addiction, drug abuse, tolerance and dependence.

Anticholinestrass


BP 405 [Link] AND PHYTOCHEMISTRY I (Theory)
45 Hours
Scope: The subject involves the fundamentals of Pharmacognosy like scope, classification of
crude drugs, their identification and evaluation, phytochemicals present in them and their
medicinal properties.

Objectives: Upon completion of the course, the student shall be able


1. to know the techniques in the cultivation and production of crude drugs
2. to know the crude drugs, their uses and chemical nature
3. know the evaluation techniques for the herbal drugs
4. to carry out the microscopic and morphological evaluation of crude drugs

Course Content:

UNIT-I 10 Hours
Introduction to Pharmacognosy:
(a) Definition, history, scope and development of Pharmacognosy
(b) Sources of Drugs – Plants, Animals, Marine & Tissue culture
(c) Organized drugs, unorganized drugs (dried latex, dried juices, dried extracts, gums and
mucilages, oleoresins and oleo- gum -resins).

Classification of drugs:
Alphabetical, morphological, taxonomical, chemical, pharmacological, chemo and sero
taxonomical classification of drugs

Quality control of Drugs of Natural Origin:


Adulteration of drugs of natural origin. Evaluation by organoleptic, microscopic, physical,
chemical and biological methods and properties.

Quantitative microscopy of crude drugs including lycopodium spore method, leafconstants,


camera lucida and diagrams of microscopic objects to scale with camera lucida.

UNIT-II 10 Hours
Cultivation, Collection, Processing and storage of drugs of natural origin:
Cultivation and Collection of drugs of natural origin
Factors influencing cultivation of medicinal plants.
Plant hormones and their applications.
Polyploidy, mutation and hybridization with reference to medicinal plants

Conservation of medicinal plants

UNIT-III
Plant tissue culture: calle 07 Hours

Historical development of plant tissue culture, types of cultures, Nutritional requirements,


growth and their maintenance.
Applications of plant tissue culture in pharmacognosy.
Edible vaccines


UNIT IV 10 Hours
Pharmacognosy in various systems of medicine:
Role of Pharmacognosy in allopathy and traditional systems of medicine namely, Ayurveda,
Unani, Siddha, Homeopathy and Chinese systems of medicine.

Introduction to secondary metabolites:


Definition, classification, properties and test for identification of Alkaloids, Glycosides,
Flavonoids, Tannins, Volatile oil and Resins

UNIT V 08 Hours
Study of biological source, chemical nature and uses of drugs of natural origin containing
following drugs
Plant Products:
Fibers - Cotton, Jute, Hemp
Hallucinogens, Teratogens, Natural allergens

Primary metabolites:
General introduction, detailed study with respect to chemistry, sources, preparation,
evaluation, preservation, storage, therapeutic used and commercial utility as Pharmaceutical
Aids and/or Medicines for the following Primary metabolites:
Carbohydrates: Acacia, Agar, Tragacanth, Honey
Proteins and Enzymes : Gelatin, casein, proteolytic enzymes (Papain, bromelain,
serratiopeptidase, urokinase, streptokinase, pepsin).
Lipids(Waxes, fats, fixed oils) : Castor oil, Chaulmoogra oil, Wool Fat, Bees Wax
Marine Drugs:
Novel medicinal agents from marine sources



Common questions

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Adrenergic and cholinergic neurotransmitter systems largely dictate the drug development strategies for targeting the autonomic nervous system. Adrenergic system modulates the sympathetic ‘fight or flight’ responses and is targeted in developing sympathomimetic and sympatholytic agents. Detailed understanding of receptor subtypes and their distribution led to development of selective agents, improving therapeutic outcomes and minimizing side effects. Similarly, cholinergic systems, influencing ‘rest and digest’ activities, serve as targets for drugs treating disorders like glaucoma, myasthenia gravis, and Alzheimer's disease. The nuanced understanding of receptor pharmacology guides the development of agents capable of modulating these pathways selectively and effectively .

Secondary metabolites, such as alkaloids, glycosides, flavonoids, tannins, volatile oils, and resins, are significant in therapeutic applications because of their diverse biological activities. These compounds often possess therapeutic properties including antimicrobial, anti-inflammatory, analgesic, and anticancer effects, among others. The understanding and classification of these metabolites contribute to the development of novel therapeutics and the optimization of extraction and formulation strategies for herbal medicines. Additionally, their qualitative and quantitative analysis is essential in standardizing herbal products, ensuring efficacy and safety .

The Structure Activity Relationship (SAR) for sympathomimetic agents involves modifications in their molecular structure that correspond to changes in their interaction with adrenergic receptors and, consequently, their pharmacological efficacy. Key aspects of SAR include the presence of hydroxyl groups on the aromatic ring which are critical for receptor binding and activity. The substitution pattern on the ring and nitrogen atom also greatly influences receptor selectivity and intrinsic activity. Modifications can either enhance binding affinity or modify the drug’s resistance to enzymatic degradation, affecting its duration and potency of action .

The therapeutic index (TI) of a drug is a critical parameter that represents the safety margin between the effective and toxic doses of the drug. A higher TI indicates a large safety margin, meaning the drug can be administered with less risk of adverse effects, while a low TI denotes a narrower safety range, requiring careful dose titration and monitoring. Clinically, the TI informs healthcare providers about the need for monitoring and the caution required in prescribing, especially in populations with variations in drug metabolism or those predisposed to adverse effects .

Enzyme induction accelerates the metabolism of drugs by increasing the synthesis of metabolic enzymes, leading to decreased drug concentrations and potential therapeutic failure. Conversely, enzyme inhibition slows down drug metabolism, resulting in increased drug concentrations and risk of toxicity. These interactions can significantly alter the pharmacokinetic profile of drugs co-administered, leading to clinically significant drug interactions that may require dosage adjustment or close therapeutic monitoring .

The cultivation of medicinal plants is influenced by environmental factors such as climate, soil type, and altitude, as well as horticultural practices like irrigation, fertilization, and pest control. These factors directly impact the growth and development of plants, subsequently affecting the quantity and quality of bioactive compounds produced. Furthermore, genetic factors including plant variety and the use of polyploidy or hybridization techniques can enhance the yield of specific metabolites. Effective cultivation practices are crucial for consistently obtaining high-quality raw materials for pharmaceutical use .

Plant tissue culture techniques enable the cultivation of plant cells, tissues, or organs in a controlled, sterile environment, which is vital in pharmacognosy for consistent production of plant-derived drugs. These techniques facilitate the production of bioactive compounds, mass propagation of plants with medicinal value, and allow for genetic manipulation such as polyploidy, mutation, and hybridization. Moreover, they offer a platform for producing edible vaccines and conserving endangered medicinal plants by providing an alternative to wholesale harvesting from the wild .

Drug metabolism is primarily divided into Phase I and Phase II reactions. Phase I, often involving oxidation, reduction, or hydrolysis, introduces or exposes functional groups through modifications. These reactions often convert lipophilic drugs to more polar metabolites. Phase II involves conjugation reactions where the drug or its phase I metabolites are linked with endogenous substances to increase solubility and facilitate excretion. These processes are crucial for drug elimination and significantly determine a drug's half-life, bioavailability, and dosage requirements .

Physicochemical properties, including ionization and solubility, significantly impact a drug’s biological action by altering how the drug interacts with biological membranes, proteins, and receptors. Ionization affects the drug's absorption and distribution by influencing its solubility in biological fluids and its ability to cross lipid membranes, thus impacting its bioavailability. Solubility determines the extent to which a drug dissolves in physiological conditions, affecting its concentration in systemic circulation and, consequently, its therapeutic efficacy .

Catecholamines biosynthesis starts with the amino acid tyrosine being converted to L-DOPA by tyrosine hydroxylase, followed by conversion to dopamine by aromatic L-amino acid decarboxylase. Dopamine is further converted into norepinephrine by dopamine β-hydroxylase, and norepinephrine can be converted to epinephrine by phenylethanolamine N-methyltransferase. Catecholamines are catabolized via monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT), producing final metabolites such as vanillylmandelic acid (VMA) which are excreted in urine .

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