Bupropion is used in smoking cessation and depression. Its mechanism that distinguishes it from SSRIs and SNRIs is:
- A MAO-A inhibition in the CNS increasing catecholamine and serotonin levels
- B Inhibition of neuronal reuptake of dopamine and norepinephrine (NDRI) without significant serotonin reuptake inhibition, and it also blocks nicotinic acetylcholine receptors ✓
- C Direct dopamine D2 receptor partial agonism reducing cravings
- D Blockade of the glutamate NMDA receptor, reducing withdrawal-associated neuroplastic changes
Correct answer: B. Inhibition of neuronal reuptake of dopamine and norepinephrine (NDRI) without significant serotonin reuptake inhibition, and it also blocks nicotinic acetylcholine receptors
Explanation
Bupropion is a norepinephrine-dopamine reuptake inhibitor (NDRI) — its primary antidepressant and pro-cessation mechanism involves blocking NET and DAT without significant SERT inhibition. Additionally, bupropion (and its active metabolite hydroxybupropion) non-competitively antagonises nicotinic acetylcholine receptors, reducing nicotine's rewarding effects and attenuating withdrawal symptoms. These dual properties make it effective in both depression and smoking cessation (Zyban). Varenicline works via D3/α4β2 nAChR partial agonism.
Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.
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