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Sibutramine, formerly sold under the brand name Meridia among others, is an appetite suppressant which has been discontinued in many countries. It works as a serotonin–norepinephrine reuptake inhibitor (SNRI) similar to certain antidepressants .
Orlistat (Xenical), the most commonly used medication to treat obesity and sibutramine (Meridia), a medication that was withdrawn due to cardiovascular side effects. Anti-obesity medication or weight loss medications are pharmacological agents that reduce or control excess body fat.
Sibutramine is the name of an SNRI based appetite suppressant with use in the treatment of obesity. This was explored in the treatment of depression, but was shown not to be effective. Both sibutramine and venlafaxine are phenethylamine-based. At high doses, both venlafaxine and sibutramine will start producing dopaminergic effects.
Medifoxamine (Cledial, Gerdaxyl) is an antidepressant that appears to act as an SDRI as well as a 5-HT 2 receptor antagonist. [3] Sibutramine (Reductil, Meridia, Siredia, Sibutrex) is a withdrawn anorectic that itself as a molecule in vitro is an SNDRI but preferentially an SDRI, with 18.3- and 5.8-fold preference for inhibiting the reuptake of serotonin and dopamine over norepinephrine ...
Following sibutramine administration in humans, didesmethylsibutramine (M2) is formed through the N-demethylation of desmethylsibutramine (M1) by CYP2B6. [7] Elevated plasma levels of sibutramine are observed with concomitant use of CYP2B6 inhibitors (e.g. clopidogrel) and in individuals with certain CYP2B6 genotypes due to the reduced conversion of sibutramine into desmethylsibutramine.
Sibutramine was the first drug for the treatment of obesity to be approved in 30 years. [17] It has been associated with increased cardiovascular events and strokes and has been withdrawn from the market in several countries and regions including the United States in 2010.
Desmethylsibutramine (also known as norsibutramine and BTS-54354) is an active metabolite of the anorectic drug sibutramine.It is a more potent monoamine reuptake inhibitor than sibutramine and has been sold as an ingredient in weight loss products sold as dietary supplements, along with related compounds such as the N-ethyl and 3,4-dichloro derivatives.
Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS) and are implicated in many neurological processes, including motivational and incentive salience, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling.