Saturday, June 12, 2021

Competitive and non-competitive antagonism

 

Feature

Competitive antagonism

Non-competitive antagonism (equilibrium type)

Non-competitive antagonism (Non-equilibrium)

Site of receptor binding

Same as that of agonist (orthosteric)

Different from that of agonist (Allosteric)

Same as that of agonist (orthosteric)

Reversibility of binding

Reversible

Reversible

Irreversible (strong covalent bonds)

Dose response curve at increasing concentration of antagonist

Rightward shift

Flattening

Flattening

Maximal response

Reached with increase in concentration of agonist (surmountable)

Not reached with increase in concentration of agonist (Unsurmountable)

Not reached with increase in concentration of agonist (Unsurmountable)

Duration of action

As long as antagonist is above the threshold concentration

As long as antagonist is above the threshold concentration

Action persists even if plasma is cleared of the antagonist. Action returns after fresh receptors are synthesized which bind the agonist

 

No comments:

Post a Comment

Lidocaine and phenytoin- both are sodium channel blockers. Lidocaine is a local anaesthetic and an anti-arrhythmic. Phenytoin is an anticonvulsant. What explains their differential action? Is it because of their difference in pharmacokinetics.

 Drugs, more than often, have multiple actions. The ability of drugs to interact with different targets and sometimes same target in differe...