Pharmacology · Pharmacokinetics and Pharmacodynamics

A competitive antagonist shifts the agonist dose-response curve. Which statement CORRECTLY describes this shift?

  • A The curve shifts to the right with a reduced maximum effect (increased EC50, decreased Emax)
  • B The curve shifts upward with no change in EC50 (unchanged EC50, increased Emax)
  • C The curve shifts to the left with unchanged Emax (decreased EC50, unchanged Emax)
  • D The curve shifts to the right in parallel (increased EC50, unchanged Emax)
Correct answer: D. The curve shifts to the right in parallel (increased EC50, unchanged Emax)

Explanation

A competitive (reversible) antagonist competes with the agonist for the same receptor binding site. Increasing agonist concentration can overcome the competitive block—thus maximal efficacy (Emax) is preserved. The dose-response curve shifts to the right in a parallel manner: more agonist is needed to achieve 50% of the maximal effect, increasing the EC50 (or ED50). This rightward parallel shift with preserved Emax is the defining characteristic of competitive antagonism. Non-competitive (irreversible or allosteric) antagonism reduces Emax with variable EC50 changes because no amount of agonist can fully overcome blockade when receptors are permanently occupied.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

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