Evaluation of Bupropion Hydrochloride: The First of a New Class of Atypical Antidepressants

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Abstract
Bupropion hydrochloride is a new antidepressant that differs clinically and pharmacologically from the tricyclic antidepressants and the monoamine oxidase inhibitors. Pharmacokinetically, bupropion is an intermediate-lived drug with a half-life of about 12 hours. Its antidepressant activity in man has been demonstrated in double-blind, placebo and active drug-controlled studies. Onset of antidepressant action occurs in one to three weeks. Bupropion has a greater effect on the neuronal reuptake of dopamine than of other biogenic amines. At a recommended dose of 450–600 mg/day, the side effect profile of bupropion also distinguishes it from other antidepressants. It does not bind to cholinergic receptors in vitro at clinically relevant concentrations and does not produce appreciable autonomic side effects. The exception is dry mouth, which is reported in 13% of patients. The mechanism underlying this effect is unclear. Bupropion is devoid of cardiovascular effects (e.g., impaired intracardiac conduction, reduced myocardial contractility, decreased peripheral resistance, orthostatic hypotension) in both human and animal studies. The drug is nonsedating and antagonizes the effects of commonly used sedatives, such as alcohol and diazepam. It does not produce weight gain. In susceptible patients, activating effects can occur. Given this profile, bupropion should be less toxic than conventional antidepressants when taken in overdoses; however overdose experience with the drug is limited.