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Sibutramine (usually in the form of the hydrochloride monohydrate salt) is an oral anorexiant. Until 2010 it was marketed and prescribed as an adjunct in the treatment of exogenous obesity along with diet and exercise. It has been associated with increased cardiovascular events and strokes and has been withdrawn from the market in several countries and regions including Australia, Canada,〔(Health Canada Endorsed Important Safety Information on MERIDIA (Sibutramine Hydrochloride Monohydrate) ): Subject: Voluntary withdrawal of Meridia (sibutramine) capsules from the Canadian market.〕 China, the European Union (EU),〔 Sibutramin-Vertrieb in der Europäischen Union ausgesetzt (). Abbott Laboratories in Germany. Press Release 2010-01-21. Retrieved 2010-01-27〕 Hong Kong, India, Mexico, New Zealand, the Philippines, Thailand, the United Kingdom, and the United States. Sibutramine is a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines,〔 (PDF )〕 although its mechanism of action is distinct. Sibutramine was originally developed and marketed by Knoll Pharmaceuticals and was most recently manufactured and marketed by Abbott Laboratories before its withdrawal from the market. It was sold under a variety of brand names including Reductil, Meridia, Siredia, and Sibutrex. It is classified as a Schedule IV controlled substance in the United States. ==Pharmacokinetics== Sibutramine is well absorbed from the GI tract (77%), but undergoes considerable first-pass metabolism, reducing its bioavailability. The drug itself reaches its peak plasma level after 1 hour and has also a half-life of 1 hour. Sibutramine is metabolized by cytochrome P450 isozyme CYP3A4 into two pharmacologically-active primary and secondary amines (called active metabolites 1 and 2) with half-lives of 14 and 16 hours, respectively. Peak plasma concentrations of active metabolites 1 and 2 are reached after three to four hours. The following metabolic pathway mainly results in two inactive conjugated and hydroxylated metabolites (called metabolites 5 and 6). Metabolites 5 and 6 are mainly excreted in the urine. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「sibutramine」の詳細全文を読む スポンサード リンク
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