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How does sibutramine work?

M E Lean
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Abstract

Sibutramine offers three types of benefit in weight management: by enhancing weight loss, by improving weight maintenance and by reducing the comorbidities of obesity. The clinical effects of sibutramine are explained through its known mode of action as a serotonin (5-HT) and noradrenaline reuptake inhibitor (SNRI). This dual mechanism of action results in two synergistic physiological effects--a reduction in energy intake and an increase in energy expenditure, which combine to promote and maintain weight loss.

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Appetite DepressantsCyclobutanesDose-Response Relationship, DrugEnergy IntakeEnergy MetabolismHumansObesitySelective Serotonin Reuptake InhibitorsJournal ArticleReview

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BibTeXRIS

M E Lean. 2001. How does sibutramine work?. https://doi.org/10.1038/sj.ijo.0801931

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PubMed2003

Determination of the active metabolite of sibutramine by liquid chromatography-electrospray ionization tandem mass spectrometry.

A sensitive and specific method for the determination of the active primary amine metabolite of sibutramine, N-di-desmethylsibutramine (BTS 54,505), in human plasma was developed, based on high-performance liquid chromatography (HPLC)-electrospray ionization tandem mass spectrometry (MS-MS). The samples were extracted from plasma with methyl tert.-butyl ether, followed by separation and evaporation after addition of the internal standard, propranolol, and basification with sodium hydroxide. The residue was reconstituted in mobile phase and injected into the HPLC-MS-MS system. Chromatography was performed on an ODS MS column with a mobile phase consisting of acetonitrile (containing 0.1% trifluoroacetic acid, v/v)-0.1% trifluoroacetic acid (55:45, v/v) at a flow-rate of 0.3 ml/min. Multiple reaction monitoring using precursor-->product ion combinations at m/z 252.00-->125.00 and 260.00-->115.70 was applied to determine BTS 54,505 and propranolol, respectively. Linearity was confirmed in the concentration range 0.328-32.8 ng/ml in human plasma and the imprecision of this assay was less than 19.90% over the entire concentration range. The method is sufficiently sensitive and repeatable to be used in pharmacokinetic studies.

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