DRUG ANTAGONISM

Dr. Munish Kumar

JR-2
Pharmacology Dept.
 DEFINITION
When one drug decreases or abolishes the
action of another drug.

Effect of drug A + B < effect of drug A + effect of

drug B.
 TYPES OF ANTAGONISM

1. PHYSICAL ANTAGONISM
2. CHEMICAL ANTAGONISM
3. PHYSIOLOGICAL ANTAGONISM
4. RECEPTOR / PHARMACOLOGICAL ANTAGONISM
a) COMPETITIVE ANTAGONISM
i. REVERSIBLE COMPETITIVE OR EQUILIBRIUM TYPE
ii. IRREVERSIBLE COMPETITIVE OR NON-EQUILIBRIUM TYPE
b) NON-COMPETITIVE ANTAGONISM
 PHYSICAL ANTAGONISM
It is based on physical property of drugs

Eg. Charcoal adsorbs alkaloids and can prevent

their absorption – used in alkaloidal poisonings.

Pectin adsorbs enterotoxins.

Resins (K+ binding resins) adsorbs K+ .

 CHEMICAL ANTAGONISM
The two drugs react chemically and form an
inactive product.

Eg. Heparin is antagonized by protamine.

Excess gastric acid is neutralized by antacids.
Chelating agents like BAL or calcium sodium
edetate, forms inactive complexes with heavy
metals ( As,Pb).
KMnO4 oxidizes alkaloids – used for gastric lavage
in poisoning.
PHYSIOLOGICAL ANTAGONISM

When two drugs acts on different receptors or

by different mechanisms, but have opposite
effects on same physiological system.

Eg. Histamine and adrenaline on bronchial

muscles and B.P.
Glucagon and insulin on blood sugar level.
Atropine and ACh on heart rate.
 RECEPTOR ANTAGONISM

Reversible
(equilibrium)
antagonism
Competitive
antagonism
Receptor Irreversible
antagonism (nonequilibrium)
antagonism
Non-competitive
antagonism
Receptor antagonism – one drug (antagonist)
blocks the receptor action of the other
(agonist).

Receptor antagonism can be competitive or

non-competitive.
Competitive antagonism (equilibrium
type) Non-competitive antagonism
1) Antagonist is chemically 1) Does not resemble.
similar to agonist.
2) Antagonist binds with the 2) Binds to another site of
same receptor as the action.
agonist.
3) Intensity of response 3) Maximal response depends
depends on the only on the concentration
concentration of both of antagonist.
agonist and antagonist.
4) Examples –
4) Examples –
ACh – Atropine
Diazepam - Bicuculline
Morphine - Naloxone
Competitive antagonism Non-competitive antagonism

 Parallel rightward shift of  Flattening of agonist DRC

agonist DRC
NON-EQUILIBRIUM ANTAGONISM

Also known as irreversible competitive

antagonism.
Antagonists bind to the receptor with strong
(covalent) bonds.
DRC is shifted to right and the maximal
response is lowered.
Examples – phenoxybenzamine is a non-
equilibrium antagonist of adrenaline at α
receptor.
NON-EQUILIBRIUM ANTAGONISM