ลอร์คาเซริน ยาลดน้ำหนักที่ออกฤทธิ์กระตุ้นอย่างจำเพาะที่ 5-HT2c receptor Lorcaserin, A Novel Selective 5-HT2c Receptor Agonist for Weight Reduction

Abstract

AbstractLorcaserin, a novel selective 5-HT2C receptor agonist for appetite control,acts on central nervous system through specifically stimulating 5-HT2Creceptors. With 100-fold specificity on 5-HT2C than 5-HT2B and 15-foldspecificity on 5-HT2C than 5-HT2A, less adverse events of heart valve(through 5-HT2B) and depression and psychotic symptoms (through 5-HT2A)could be reasonably expected. It is cautious to use lorcaserin in patientswith mild-moderate impairment where a 1.7 to 6-fold increase in bloodconcentration was reported. It is also suggested to avoid use in patientswith severe renal impairment and severe hepatic impairment. Clinicalstudies demonstrated that lorcaserin 10 mg once or twice daily with dietcontrol and regular exercise resulted in at least 5% weight reduction inobese or overweight patients with no type II diabetes. However, oncediscontinued, obesity was highly likely to rebound if diet control and regularexercise could not be maintained.Keywords: lorcaserin, appetite, weight reduction, 5-HT2C receptor