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Pharmacology · single question

Clonazepam works as a GABA agonist. What does this mean pharmacologically?

  1. It enhances the effect of GABA at GABA-A receptors, increasing chloride ion influx → hyperpolarization → CNS depression/anxiolysis
  2. It inhibits GABA reuptake
  3. It is a direct GABA receptor agonist replacing GABA
  4. It blocks GABA receptors causing excitation
Show answer and explanation

Correct answer: A. It enhances the effect of GABA at GABA-A receptors, increasing chloride ion influx → hyperpolarization → CNS depression/anxiolysis

  • A. Correct. Benzodiazepines (including clonazepam) are positive allosteric modulators of GABA-A receptors — they ENHANCE (not replace) GABA's inhibitory effect by increasing the frequency of chloride channel opening. This causes hyperpolarization of neurons → CNS depression → anxiolysis, anticonvulsant effect, and muscle relaxation.
  • B. GABA reuptake inhibition is not the mechanism of benzodiazepines.
  • C. Benzodiazepines are modulators (allosteric), not direct agonists — they require GABA to be present and simply amplify its effect.
  • D. Blocking GABA receptors would cause excitation/convulsions (the opposite of benzodiazepine action).

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