Zolpidem produces hypnosis with comparatively little anxiolytic, myorelaxant, or anticonvulsant activity compared with classical benzodiazepines. The pharmacological basis is:
- A Antagonism of orexin receptors in the lateral hypothalamus
- B Direct opening of the chloride channel independent of GABA
- C Non-selective binding to all benzodiazepine binding sites including spinal cord receptors
- D Selective affinity for GABA-A receptors containing the alpha-1 subunit ✓
Explanation
Zolpidem is a non-benzodiazepine hypnotic that binds selectively to GABA-D receptors containing the alpha-1 subunit, the subtype predominantly responsible for sedation. Anxiolytic, myorelaxant, and anticonvulsant effects are mediated largely by alpha-2, alpha-3, and alpha-5 containing receptors, so these actions are minimal at hypnotic doses. Orexin antagonists such as suvorexant represent a separate hypnotic class.
Reference: Katzung's Basic and Clinical Pharmacology, 15th ed.
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