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Although the exact mechanism is unknown, it is believed to involve the selective activation of 5-HT2C receptors in the anorexigenic pro-opiomelanocortin neurons in the arcuate nucleus of the hypothalamus. This results in decreased food intake and satiety by promoting the release of alpha-melanocortin stimulating hormone, which acts on melanocortin-4 receptors.
Lorcaserin produced a dose-dependent weight loss over a 12-week period by promoting satiety and decreasing food consumption.
Lorcaserin has extensive hepatic metabolism producing inactive compounds. Lorcaserin sulfamate (M1) is the major metabolite circulating in the plasma, and N-carbamoyl glucuronide lorcaserin (M5) is the major metabolite in urine. Other minor metabolites that are both excreted in urine are glucuronide or sulfate conjugates.
Most common adverse reactions include hypoglycemia (diabetic patients), headache, back pain, fatigue, decrease in lymphocytes, upper respiratory tract infection, and nasopharyngitis. Moreover, the safety and efficacy of coadministration with other weight loss products has not been established, and cardiovascular effects on mortality and morbidity have not been established.
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