Nicotinic antagonist


A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine at nicotinic [acetylcholine receptor]s. These compounds are mainly used for peripheral muscle paralysis in surgery, the classical agent of this type being tubocurarine, but some centrally acting compounds such as bupropion, mecamylamine, and 18-methoxycoronaridine block nicotinic acetylcholine receptors in the brain and have been proposed for treating nicotine addiction.
MechanismAntagonistPreferred receptorClinical use-
Ganglionic blocking agentsHexamethoniumGanglion type--
Ganglionic blocking agentsMecamylamineGanglion type-
Ganglionic blocking agentsTrimethaphanGanglion typeRarely used for blood pressure decrease during surgery-
Nondepolarizing neuromuscular blocking agentsAtracuriumMuscle typeMuscle relaxant in anaesthesia-
Nondepolarizing neuromuscular blocking agentsDoxacuriumMuscle type-
Nondepolarizing neuromuscular blocking agentsMivacuriumMuscle type-
Nondepolarizing neuromuscular blocking agentsPancuroniumMuscle typeMuscle relaxant in anaesthesia-
Nondepolarizing neuromuscular blocking agentsTubocurarineMuscle typeDiscovered in arrow poison; it was the first peripheral muscle relaxant. Rarely used since the 1980s.-
Nondepolarizing neuromuscular blocking agentsVecuroniumMuscle typeMuscle relaxant in anaesthesia-
Depolarizing neuromuscular blocking agentsSuccinylcholine*Muscle type-
Centrally acting nicotinic antagonists18-Methoxycoronaridineα3β4-
Centrally acting nicotinic antagonistsBupropionα3β4. α4β2, α1β1γδAntidepressant
Centrally acting nicotinic antagonistsHydroxybupropionα3β4. α4β2, α1β1γδAntidepressant. Metabolite of bupropion.
Centrally acting nicotinic antagonistsThreohydrobupropionα3β4.Antidepressant. Metabolite of bupropion.
Centrally acting nicotinic antagonistsDextromethorphanα3β4. α4β2, α7Common over the counter antitussive.-
Centrally acting nicotinic antagonistsDextrorphanα3β4. α4β2, α7Metabolite of dextromethorphan; no accepted medical uses.-
Centrally acting nicotinic antagonists3-Methoxymorphinanα3β4Secondary metabolite of dextromethorphan; not used in medical practice. Unknown medical efficacy.-