Sibutramine<\/b>, formerly sold under the brand name\u00a0Meridia<\/b>\u00a0among others, is an\u00a0appetite suppressant\u00a0which has been discontinued in many countries. It works as a\u00a0serotonin\u2013norepinephrine reuptake inhibitor\u00a0(SNRI) similar to certain\u00a0antidepressants.<\/p>\n
Sibutramine has been used to produce appetite suppression for the purpose of attaining\u00a0weight loss\u00a0in the treatment of patients with obesity.<\/p>\n
Sibutramine is a\u00a0serotonin\u2013norepinephrine reuptake inhibitor\u00a0(SNRI) that, in humans, reduces the\u00a0reuptake\u00a0of\u00a0norepinephrine\u00a0(by ~73%),\u00a0serotonin\u00a0(by ~54%), and\u00a0dopamine\u00a0(by ~16%),<\/sup>\u00a0thereby increasing the levels of these substances in\u00a0synaptic clefts\u00a0and helping enhance\u00a0satiety; the serotonergic action, in particular, is thought to influence appetite. Older\u00a0anorectic\u00a0agents such as\u00a0amphetamine\u00a0and\u00a0fenfluramine\u00a0force the release of these neurotransmitters rather than affecting their reuptake.<\/sup><\/p>\n Sibutramine’s mechanism of action is similar to\u00a0tricyclic antidepressants, and it has demonstrated antidepressant effects in animal models of depression.<\/sup>\u00a0It was approved by the U.S.\u00a0Food and Drug Administration\u00a0(FDA) in November 1997<\/sup>\u00a0for the treatment of obesity.<\/p>\n Sibutramine is reported to be a\u00a0prodrug\u00a0to two\u00a0active metabolites,\u00a0desmethylsibutramine\u00a0(M1; BTS-54354) and\u00a0didesmethylsibutramine\u00a0(M2; BTS-54505), with much greater potency as monoamine reuptake inhibitors.<\/sup><\/sup>\u00a0Further studies have indicated that the (R<\/i>)-enantiomers of each metabolite exert significantly stronger anorectic effects than the (S<\/i>)-enantiomers.<\/sup><\/p>\n Unlike other serotonergic appetite suppressants like\u00a0fenfluramine, sibutramine and its metabolites have only low and likely inconsequential\u00a0affinity\u00a0for the\u00a05-HT2B<\/sub>\u00a0receptor.<\/sup><\/p>\n Sibutramine is well absorbed from the\u00a0gastrointestinal tract\u00a0(77%), but undergoes considerable\u00a0first-pass metabolism, reducing its bioavailability. The drug itself reaches its peak\u00a0plasma\u00a0level after 1 hour and has also a half-life of 1 hour. Sibutramine is metabolized by\u00a0cytochrome P450\u00a0isozyme\u00a0CYP3A4\u00a0into two pharmacologically active primary and secondary\u00a0amines\u00a0(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.<\/p>","protected":false},"excerpt":{"rendered":" Sibutramine, formerly sold under the brand name\u00a0Meridia\u00a0among others, is an\u00a0appetite suppressant\u00a0which has been discontinued in many countries. It works as<\/p>\n","protected":false},"featured_media":9903,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[],"product_cat":[73],"product_tag":[],"class_list":{"0":"post-9902","1":"product","2":"type-product","3":"status-publish","4":"has-post-thumbnail","6":"product_cat-ssteroides_orales","8":"first","9":"instock","10":"sale","11":"shipping-taxable","12":"purchasable","13":"product-type-simple"},"yoast_head":"\n