Hurren Kathryn M, Dunham Marissa W
a Department of Ambulatory Care , Veterans Affairs Ann Arbor Healthcare System , Ann Arbor , MI , USA.
Expert Opin Drug Metab Toxicol. 2017 Aug;13(8):891-896. doi: 10.1080/17425255.2017.1344214. Epub 2017 Jul 11.
Lorcaserin is a serotonin 2C receptor antagonist that was FDA approved in 2012. Lorcaserin is recently available as an extended-release (ER) formulation for the treatment of obesity as an adjunct to lifestyle modification. Areas covered: The pharmacokinetics, pharmacodynamics, efficacy, and safety of lorcaserin ER will be reviewed. Expert opinion: Lorcaserin ER 20mg daily provides drug exposure bioequivalent to lorcaserin immediate release (IR) 10mg twice daily. Lorcaserin IR is associated with 3.3 and 3.0% placebo-subtracted weight loss in patients without and with diabetes, respectively. A1C was reduced by 0.9% in patients with diabetes. Common side effects include headache, dry mouth, constipation, dizziness, fatigue, and nausea. Lorcaserin provides potential advantages over other antiobesity medications in regards to tolerability and simplicity of medication initiation, but may not be as effective as other options. Lorcaserin ER offers improved ease of administration and anticipated adherence compared to the IR formulation. The place in therapy for lorcaserin ER and other antiobesity medications will be further clarified by results of pending clinical trials addressing cardiovascular outcomes as well as the role pharmacogenomics and comorbid disease states may play in choosing patient-specific therapy.
氯卡色林是一种5-羟色胺2C受体拮抗剂，于2012年获得美国食品药品监督管理局（FDA）批准。氯卡色林最近有缓释（ER）制剂上市，可作为生活方式改变的辅助手段用于治疗肥胖症。涵盖领域：将对氯卡色林ER的药代动力学、药效学、疗效和安全性进行综述。专家意见：氯卡色林ER每日20mg的药物暴露量与氯卡色林速释（IR）制剂每日两次每次10mg相当。在未患糖尿病和患糖尿病的患者中，氯卡色林IR分别使体重较安慰剂组减轻3.3%和3.0%。糖尿病患者的糖化血红蛋白（A1C）降低了0.9%。常见副作用包括头痛、口干、便秘、头晕、疲劳和恶心。在耐受性和用药起始的简便性方面，氯卡色林相对于其他抗肥胖药物具有潜在优势，但可能不如其他药物有效。与IR制剂相比，氯卡色林ER的给药更简便，预计患者依从性更好。关于氯卡色林ER和其他抗肥胖药物在治疗中的地位，将通过正在进行的针对心血管结局的临床试验结果以及药物基因组学和合并疾病状态在选择针对特定患者的治疗中可能发挥的作用进一步阐明。
