Mecamylamine (Inversine): an old antihypertensive with new research directions.
Mecamylamine (Inversine), the first orally available antihypertensive agent, is now rarely used. Although celebrated in the 1950s, mecamylamine fell out of favour because of its widespread ganglionic side effects at antihypertensive doses (30-90 mg/day). However, recent studies suggest that mecamylamine is very effective at relatively low doses (2.5-5 mg b.i.d.) for blocking the physiological effects of nicotine and improving abstinence rates in smoking cessation studies, particularly for women. When these lower doses of mecamylamine are given, patients do not experience the severity of side effects that made the drug unpopular for the treatment of hypertension. Tobacco smoking is a strong risk factor for cardiovascular morbidity, including accelerated atherosclerosis and increased risk of heart attacks. Though currently untested, the available evidence suggests that low-dose mecamylamine therapy might reduce blood pressure variability and atherogenetic lipid profile in smokers. With this in mind, mecamylamine should be an important research tool in the field of hypertension research, particularly in recalcitrant smokers with mild to moderate hypertension.
Shytle
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RD
Center for Aging and Brain Repair, Department of Neurosurgery, University of South Florida College of Medicine, Tampa 33613, USA. dshytle@hsc.usf.edu
Penny
E
E
Silver
A A
AA
Goldman
J
J
Sanberg
P R
PR
D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D008464:Mecamylamine / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D018733:Nicotinic Antagonists / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D016540:Smoking Cessation
D000959:Antihypertensive Agents; D018733:Nicotinic Antagonists; D008464:Mecamylamine