Nicotinic antagonist


A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine at nicotinic acetylcholine receptors. 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 typenone
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 pheripheral muscle relaxant. Rarely used since 1980s.
Nondepolarizing neuromuscular blocking agentsVecuroniumMuscle typemuscle relaxant in anaesthesia
Depolarizing neuromuscular blocking agentsSuccinylcholine*Muscle type
Centrally acting nicotinic antagonists18-Methoxycoronaridineα3β4
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.