Nicotinic antagonist

A nicotinic antagonist is a type of anticholinergic drug that inhibits the action of acetylcholine (ACh) at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery, the classical agent of this type being tubocurarine,[1] 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 drug addiction.

Comparison
Mechanism Antagonist Preferred receptor Clinical use
Ganglionic blocking agents Hexamethonium Ganglion type none[2]
Mecamylamine Ganglion type
Trimethaphan Ganglion type Rarely used for blood pressure decrease during surgery[2]
Nondepolarizing neuromuscular blocking agents Atracurium Muscle type muscle relaxant in anaesthesia[2]
Doxacurium Muscle type
Mivacurium Muscle type
Pancuronium Muscle type muscle relaxant in anaesthesia[2]
Tubocurarine Muscle type Discovered in arrow poison it was the first pheripheral muscle relaxant. Rarely used since 1980s. [2]
Vecuronium Muscle type muscle relaxant in anaesthesia[2]
Depolarizing neuromuscular blocking agents Succinylcholine* Muscle type
Centrally acting nicotinic antagonists 18-Methoxycoronaridine α3β4
Dextromethorphan α3β4. α4β2, α7 Common over the counter antitussive.
Dextrorphan α3β4. α4β2, α7 Metabolite of Dextromethorphan, no accepted medical uses.
3-Methoxymorphinan α3β4 Secondary metabolite of Dextromethorphan, not used in medical practice. Unknown medical efficacy.

See also

References

  1. ↑ P. Taylor (1990). In Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th Ed., (A. G. Gilman et al., Eds.), pp. 166-186, New York: Pergamon Press.
  2. 1 2 3 4 5 6 Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4. Page 149
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