Pharmacology · Antiepileptics and CNS Drugs (Antipsychotics, Antidepressants, Sedatives)

Buspirone is prescribed for generalised anxiety disorder. Unlike benzodiazepines, buspirone does not cause sedation, dependence, or enhance GABA-A function. Its primary mechanism of action is:

  • A Partial agonism at the 5-HT1A receptor with weak D2 antagonism
  • B Positive allosteric modulation at the benzodiazepine binding site of the GABA-A receptor
  • C Selective inhibition of serotonin reuptake transporter with alpha-2 adrenoceptor blockade
  • D Non-selective inhibition of phosphodiesterase, raising cAMP in limbic neurons
Correct answer: A. Partial agonism at the 5-HT1A receptor with weak D2 antagonism

Explanation

Buspirone is an azapirone that acts as a partial agonist at presynaptic and postsynaptic 5-HT1A receptors, reducing serotonergic neurotransmission in limbic areas, and also has modest D2 receptor antagonism. Its anxiolytic effect develops slowly over 1-2 weeks (unlike benzodiazepines) because it requires receptor desensitisation. It has no cross-tolerance with benzodiazepines, cannot prevent benzodiazepine withdrawal, and lacks abuse potential. It does not act on GABA-A receptors.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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