Drug intelligence / Profile preview

mecamylamine

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Mecamylamine is a small molecule, non-selective, non-competitive antagonist of nicotinic acetylcholine receptors (nAChRs). It was originally introduced in the 1950s as an orally active ganglionic blocker for the management of moderate to severe essential hypertension and uncomplicated malignant hypertension. Mecamylamine acts by inhibiting acetylcholine at autonomic ganglia, leading to reduced sympathetic tone, vasodilation, and decreased cardiac output. Its antihypertensive effect is predominantly orthostatic but also reduces supine blood pressure. The drug crosses the blood-brain barrier and has been investigated for other uses such as autonomic dysreflexia and as an antiaddictive agent in smoking cessation research[1][4][5][6][8].

Brand names
VecamylInversine
Other names
mecamylamine hydrochloridemecamylamine HCl
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)

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