bupropion history

bupropion history - Bupropion was synthesized in 1966 by...

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Bupropion was synthesized in 1966 by Burroughs Research' group of scientists seeking "an agent that would be active in antidepressant screening models, but differ chemically and pharmacologically from the tricyclics, and not be sympathomimetic, cholinolytic, nor an inhibitor of monoamine oxidase" (Soroko et al. 1977). The bupropion research endeavour led to the discovery of a molecule with a novel mechanism of action and a favorable side-effect profile that minimized the anticholinergic, sympathomimetic, and cardiac effects of many of the antidepressants that were currently in use. Bupropion was patented by Burroughs-Wellcome (later Glaxo-Wellcome, and, as of 2000, GlaxoSmithKline) in 1974. There is evidence that bupropion's development was inspired by the structure of amphetamine, which had been used, with limited success, as an antidepressant in the 1930s. Bupropion is similar in structure to the stimulant cathinone (a monoamine alkaloid found in the shrub Catha edulis - Khat), and to phenethylamines in general. It is a chemical derivative of diethylpropion, an amphetamine-like substance used as an anorectic. It was originally approved by the FDA in 1985 and marketed under the name Wellbutrin (IR formulation) as an antidepressant. However, a significant incidence of seizures at the originally recommended dosage (400-600 mg) caused the removal of the drug from the market in 1986. It was subsequently discovered that reducing the dose by about half greatly reduced the risk of seizures. Bupropion was re-introduced to the market in 1989 with the maximum dose of 450 mg/day. Glaxo then developed a sustained-release (SR) version which releases bupropion hydrochloride at a slower rate. It was approved by the FDA in 1996. In 1997, bupropion was approved as a smoking cessation aid under the brand name Zyban. Extended release bupropion, Wellbutrin XL, is the most recent formulation (approved in 2003) and is taken orally once a day 2 . Because of this altered mechanism of delivery and reduced dosing, incidence of seizures is comparable to, and in some cases, lower than that of other antidepressants. Bupropion was licensed as a pharmacotherapy for smoking cessation in the United Kingdom in 2000,
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This note was uploaded on 04/27/2011 for the course SCIENCE 02 taught by Professor Apfd during the Spring '10 term at Alabama.

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bupropion history - Bupropion was synthesized in 1966 by...

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