Bupropion: pharmacological and clinical profile
in smoking cessation

by
Haustein KO.
Institute for Nicotine Research and Smoking Cessation,
Erfurt, Germany.
haustein@inr-online.de
Int J Clin Pharmacol Ther 2003 Feb;41(2):56-66


ABSTRACT

Chemistry, pharmacokinetics, pharmacology, clinical efficacy, adverse effects and dosage of bupropion hydrochloride (BP), an aminoketone antidepressant used in smoking cessation, are reviewed. The nicotinergic acetylcholine receptors are inhibited at clinically relevant concentrations of BP. BP does not inhibit monoamine oxidase, and it has minimal inhibitory effects on presynaptic noradrenaline and dopamine uptake. BP is rapidly absorbed after oral administration and demonstrates biphasic elimination with an elimination half-life of 11 - 14 hours. BP is extensively metabolized by oxidation and reduction to at least 6 metabolites, 2 of which may be active. The plasma levels of the erythro-amino alcohol of BP correlate with several side effects such as insomnia and dry mouth. Efficacy of BP(SR) in smoking cessation has been examined in several double-blind, randomized trials in which daily doses of 150 or 300 mg have been administered for 7 or 9 weeks. In addition, 1 study examined the combination of BP(SR) plus nicotine patch. The point prevalences of stopping smoking reached values between 21.2 and 38%, but they did not exceed those after nicotine replacement therapy alone. Long-term administration (52 weeks) of BP did not improve abstinence compared with placebo after a 2-year follow-up period. Thus, the efficacy of BP in smoking cessation is comparable to that of nicotine replacement therapy. However, BP possesses a broad spectrum of infrequent adverse effects and interferes with the degradation of several drugs such as tricyclic antidepressants, beta-recpetor blocking agents, class Ic-antiarrhythmics etc. As the risk-benefit ratio of BP is smaller than that of nicotine replacement, BP should be considered as a second-line treatment in smoking cessation.
'Zyban'
Bupropion
Free-base nicotine
Bupropion and REM
Bupropion and mania
Bupropion and seizures
Bupropion and smoking
Bupropion and depression
Bupropion versus trazodone
Bupropion and its metabolites
Bupropion versus methylphenidate
Non-nicotinic drugs for tobacco addicts
Bupropion, amphetamine and cigarettes
Bupropion (Zyban): prescribing information (PDF)
Bupropion enhances pleasure for smokers who quit
Zyban/bupropion SR for tobacco smokers in remission
Varenicline (Chantix) vs bupropion SR for tobacco addicts


Refs
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Critique of Huxley's Brave New World

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