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mecamylamine + bupropion + nicotine
- Development stage
- Unknown
- Lead developer
- United States Department of Veterans Affairs
- Modality
- Small Molecules
- Administration
- Oral, Transdermal
01
Overview
mecamylamine + bupropion + nicotine is a combination pharmacotherapy regimen investigated by the US Department of Veterans Affairs for smoking cessation. This "agonist-antagonist" approach combines mecamylamine, a non-competitive nicotinic acetylcholine receptor antagonist, with bupropion (a dopamine and norepinephrine reuptake inhibitor that also acts as a nicotinic antagonist) and a nicotine transdermal patch (a nicotinic agonist). The rationale behind this triple therapy is to block the reinforcing effects of nicotine via mecamylamine while simultaneously alleviating withdrawal symptoms and cravings through the nicotine patch and bupropion. Earlier studies of the dual combination (mecamylamine and nicotine patch) showed significant improvements in abstinence rates compared to the patch alone. The VA-sponsored research has further evaluated the triple combination in heavy smokers to determine its effectiveness in achieving long-term smoking cessation.
- Other names
- mecamylamine/bupropion/nicotine combinationVA smoking cessation combination therapymecamylamine + bupropion + nicotine patch
02
Targets
DAT (Dopamine plasma membrane transport protein)Nicotinic Acetylcholine ReceptorNET (Norepinephrine Transporter)
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