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

Which antiepileptic drug produces its effect by inhibiting the neuronal and glial GABA transporter GAT-1, thereby blocking reuptake of synaptically released GABA?

  • A Vigabatrin
  • B Tiagabine
  • C Gabapentin
  • D Valproate
Correct answer: B. Tiagabine

Explanation

Tiagabine selectively inhibits the GAT-1 GABA transporter, prolonging the synaptic action of GABA. Vigabatrin raises GABA by inhibiting its degradation (GABA-transaminase), gabapentin binds the alpha-2-delta subunit of voltage-gated calcium channels, and valproate acts through sodium channel blockade and enhanced GABA effects. Distinguishing enhancement of GABA release versus prevention of GABA breakdown versus blockade of GABA reuptake is a frequently tested discriminator.

Reference: Goodman and Gilman's The Pharmacological Basis of Therapeutics, 14th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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