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Lecture 3
dr. Taher
N. Ali
Pharmacodynamics
Pharmacodynamics are the action of drugs on the
body and include the following :
1) Pharmacological action
2) Mechanism of action
3) Drugs adverse effects
4) Therapeutic uses
5) Drugs interactions
6) Contraindications
7) Precautions
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Pharmacological action
Types of pharmacological action :-
a)local action :-
the drug acts at site of application . e.g. skin -
ointment .
b)systemic action:-
the drug acts on various tissues
c)remote (reflex)actions :-
the drug produce an effect away from it is site of
action.
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Mechanism of action :-
Drugs may act through one or more of the following
mechanism:-
1- physically :-
. by adsorption e.g. kaolin in diarrhea
. by osmosis e.g. diuretics .
2- chemically :-
By neutralization e.g. sodium bicarbonate as
antacid .
3- action on enzymes :-
Some drugs act by inhibiting some enzymes .
e.g. neostigmine acts by inhibiting acetyl
cholinesterase enzyme .
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Mechanism of action :-
4- action on receptors :-
This is the common way by which drugs act .
e.g. adrenaline acts on adrenergic receptors .
The theory of receptors:-
the ability of drugs to fit onto a receptors to form drug-
receptor complex is called affinity.
the ability of drug – receptor complex to produced a
response is called efficacy .
drug + receptor drug receptor complex
response
affinity efficacy
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Mechanism of
action :-
Agonist :-
Agonist is the drug that has both affinity and
efficacy e.g. adrenaline .
Antagonist :-
Antagonist is the drug that has affinity and not
has efficacy e.g. Propranolol.
5- action on ion channel :-
Some drugs act by blocking ion
channels .
e.g. local anesthetics act by
blocking sodium channel.
6- interference with cell division :-
e.g. anticancer drugs .
7- interference with normal metabolic
pathway:-
e.g. sulphonamides.
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Adverse effects of drug
Adverse effects of drug
These are undesired effects of drugs and include the
following
1- predictable adverse effects .
2- unpredictable adverse effects .
predictable adverse effects
These are the adverse effects that not related from the
pharmacological action of drugs but its from the patient
himself and classified into :-
1- allergy (hypersensitivity)
e.g. hypersensitivity that caused by penicillin in some
patients .
2- Idiosyncrasy :-
Its an abnormal response due to genetic abnormalities .
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e.g. hemolytic anemia that caused by aspirin in patient
Adverse effects of drug
unPredictable adverse effects
These are related to pharmacological action of the drug and they are
1- THE SECONDARY EFFECTS :-
These are indirect consequences to the primary action of the
drug
e.g. prolonged used of antibiotics may lead to deficiency of
vitamin K.
2- OVER DOSE
These are effects that result from administration of large dose
of drug .
e.g. hypoglycemic shock due to over dose of insulin .
3- TOLERANCE
Tolerance means decrease the response to normal drug dose .
To overcome tolerance either increase the dose or stop the drug
for some time .
Tolerance are two type :-
Congenital and acquired
4- INTOLERANCE
Means increase the response
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to normal dose of drug .
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Drugs intolerance is usually observed in infants .
Adverse effects of drug
5- DRUG DEPENDENCE :-
Drug dependence is caused by repeated
administration of substances
A- HABITUATION :-
habituation is a psychic dependence
sudden stop of drug result in psychic
effects
e.g. cocaine addiction .
B- ADDICTION :-
addiction is a psychic and physical
dependence , sudden stop the drug result in
9 withdrawal syndrome which may be fatal .
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Adverse effects of drug
6- DRUG INTERACTION :-
Drug interaction may result in increase or decrease in the
activity of drugs .
7- CELL TOXICITY :-
e.g. gentamycin may cause nephrotoxicity (which means
kidney damage
8- TERATOGENICITY :-
Some drugs cause fetal malformation when given to
pregnant women
e.g. thalidomide .
9- PRODUCTION OF DISEASE :-
Some drugs may sometimes produce disease .
e.g. chlorpromazine may lead to parkinsonism .
10- CARCINOGENESIS :-
e.g. tobacco smoking may lead to lung cancer .
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Drug interactions
Drug interactions:
When two or more drugs are used in the
same patient they may act independently
and in this case there is no interaction,
but if one drug affects the activity of the
other drug interaction occur.
Types of drug interaction
Pharmacokinetic inter action
Pharmacodynamic interaction
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Drug interactions
Pharmacodynamic Pharmacokinetic
interaction interaction
pote anta Abso Distri meta
Additi Syner Excre
ntiati gonis rptio butio bolis
on gism tion
ng m n n m
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Pharmacokinetic interaction :-
1- Absorption :-
A- Motility :-
Atropine decrease the motility lead to decrease the
absorption of drugs
Metaclopromide increase the motility lead to
increase the absorption of drugs.
B- PH :-
Acidic ph enhance absorption of acidic drugs.
Alkaline ph enhance absorption of basic drugs.
So aspirin is better absorption in stomach (acidic ph)
Ephedrine is better absorption in intestine (alkaline
ph)
C- Contents :-
Food contents affect absorption
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of some drugs:-
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e.g. calcium (milk )interact with absorption of
Drug interactions
2- Distribution:-
Some drugs displace other drugs from its plasma
protein binding site.
e.g. aspirin displace oral hypoglycemic drugs.
3- metabolism:-
Drugs that affecting on enzyme that metabolism
of other drugs.
E.g. Phenobarbital is enzyme inducer. It increase
the metabolism of other drugs (as oral
hypoglycemic drugs) Lead to decrease their
activity.
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Drug interactions
4- Excretion:-
Alkalinization of urine leads to increase the
excretion of acidic drugs.
Acidification of urine leads to increase the
excretion of basic drugs.
Note:-
NaHCO3 (I.V) can be used for Alkalinization of
urine.
Ascorbic acid (Vit. C) Can be used for
acidification of urine.
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-:Pharmacodynamic interaction
Pharmacodynamic interaction:-
In this type the drug interacts with the
action of other drug. The interaction may
be:-
1- Addition:-
Two active drugs produce a similar action.
The total activity of both drugs is the sum
of individual activity for each drug.
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Additive Effects
Hi
A+B
Response
A B
Lo
Time
The effect of two chemicals is equal to the sum of the effect of the two chemicals
.taken separately, eg., aspirin and oxaprozin
2- Synergism:-
Two active drugs have a similar action. Each
drug increase the activity of the other drug.
E.g. ethanol and barbiturate (CNS
depressants).
3- potentiating:-
A certain activity of drug is increase by other
drug that does not have the activity.
e.g. barbiturate increase the analgesic activity
of aspirin. (While barbiturate alone has not
any analgesic activity)
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Synergistic Effects
A+B
Hi
Response
A B
Lo
Time
The effect of two chemicals taken together is greater than the sum of their separate
effect at the same doses, e.g., alcohol and other drugs
4- antagonism:-
The antagonism results in decrease the activity of
drugs.
Type of antagonism:-
A- Chemical antagonism:-
Each drug antagonizes the other chemically.
e.g. heparin (acidic drug ) and ergotamine (basic
drug ).
b - physiological antagonism:-
Each drug produces an opposite action to other drug.
e.g. adrenalin produces bronco dilation.
Histamine produces bronco constriction.
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Antagonistic Effects
Hi
A+B
Response
A B
Lo
Time
The effect of two chemicals taken together is less than the sum of their separate effect
at the same doses
C- Pharmacological antagonism:-
Both drugs act on the same receptor, one of them
is agonist and the other is antagonist.
There are two types of pharmacological
antagonism:-
A- Competitive antagonist:-
Excessive agonist can displace antagonist.
E.g. acetylcholine and atropine (on muscarinic
receptors).
b- Non competitive antagonist:-
Excessive agonist cannot displace antagonist.
E.g. organic phosphorous compounds cannot
displace by agonist.
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شكرا لحسن
المتابعة ,,,,,,,,
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