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LEARNING OBJECTIVES
At the end of this lecture, every student should be able to
understand following:
Different types of antagonist Competitive & Non- competitve antagonism with the help
of graphs.
Differences between Competitive & Non- competitve
antagonism
INTRODUCTION
The phenomenon in which one drug decreases or inhibits
ANTAGONIST:
A drug that decreases or inhibits the action of another drug or an endogenous substance.
PHYSICAL ANTAGONISM
When one drug decreases action of another drug by physical
means.
EXAMPLES:
1. ADSORPTION: Charcoal adsorbs alkaloids & prevents their absorption Used in poisoning.
2. CHELATION:
CHEMICAL ANTAGONISM
This is when one drug reacts chemically in the body to decrease effect of another drug or an endogenous substance. EXAMPLES: 1. Antacid like Sodium Bicarbonate Neutralizes Hcl in the stomach by a chemical reaction.
2. Protamine, which is positively charged at physiological pH, is used to counter the effects of negatively charged Heparin, an anti-coagulant, by biniding to it.
inflammatory action due to its ability to sequester the inflammatory cytokine, tumour necrosis factor.
PHYSIOLOGICAL ANTAGONISM
This is when two drugs OR one drug & one endogenous
substance act upon two different receptors to produce opposite physiological actions.
EXAMPLE: Histamine & Adrenaline (1)Histamine acts on its receptors to cause
histamine
_ Severe vasodilation & bronchoconstriction. _ Patient faints immediately due to severe vasodilation. _ Circulatory Shock. _ Treatment of Choice: Adrenaline
EXAMPLE:
(2) Histamine acts on receptors of the parietal cells of the gastric mucosa to stimulate acid secretion, while omeprazole blocks this effect by inhibiting the proton pump; the two drugs can be said to act as physiological antagonists.
PHARMACOLOGICAL ANTAGONISM
This is antagonism produced by blockage of receptors. Antagonist interferes with binding of agonist to its receptor
& itself binds with receptor but doesnt produce response. RECEPTOR ANTAGONIST:
Drugs that occupy the receptor but do not bring about
any response.
Have Affinity but no Intrinsic activity/ Efficacy
EXAMPLE
(1) An agonist causes increased heart rate by binding to beta 1 receptors in the heart.
_ Beta antagonist cause decrease in heart rate by blocking these receptors.
antagonist can be increased by exercise as exercise will release enough of nor-adrenaline (agonist) to overcome effects of antagonist.
EXAMPLE
(2) The antihypertensive drug prazosin competes with the
endogenous ligand, norepinephrine, at 1-adrenoceptors, decreasing vascular smooth muscle tone and reducing blood pressure.
change in maximal response of agonist, but log doseresponse curve is shifted towards higher concentration of drug. ( RIGHT)
Irreversible antagonism
If the antagonist binds to a site other than where the
Phenoxybenzamine (Antagoinst) at alpha adrenergic receptors Adrenaline (Agonist) at alpha adrenergic receptors
DECREASE in maximal response & the log dose response curve is shifted towards Higher concentrations of drug. ( RIGHT)
of spare receptors).
As more and more receptors are bound ( and essentially
PHARMACOKINETIC ANTAGONISM
This is when one drug decreases the concentration &
The reduction of the anticoagulant effect of warfarin when an agent that accelerates its hepatic metabolism, such as phenobarbital.
REVERSIBLE
Yes
No ( Irreversible)
Weak
SHIFT OF CURVE
EC50
POTENCY EXAMPLE
Increased
Decreased Prazosin
Learning resources
Katzung text book of pharmacology Good man & Gilman book of pharmacology Rang & Dale Lippincotts text book of pharmacology Naumans text book of pharmacology