University of Connecticut, School of Pharmacy, Storrs, CT, USA.
Curr Med Res Opin. 2013 Jul;29(7):839-48. doi: 10.1185/03007995.2013.794776. Epub 2013 May 10.
Obesity has become an epidemic in the United States and its prevalence continues to increase. Adjunctive treatment with pharmacotherapy is often reserved for individuals who fail to achieve their intended weight goals with diet and exercise alone. Current approved therapies for weight loss include phentermine, diethylpropion, orlistat, and phentermine/topiramate. The objective of this paper was to review the place of lorcaserin, a novel serotonin 2C agonist, which was FDA approved in July 2012. Unlike contemporary lipase inhibitors and sympathomimetic amines, lorcaserin is purported to reduce food consumption and increase satiety.
A systematic review of the literature for all relevant articles was performed through January 2013 using MEDLINE, Web of Science, and International Pharmaceutical Abstracts using key words related to lorcaserin.
Three phase III clinical studies have been published evaluating the efficacy and safety of lorcaserin in various obese populations. A higher proportion of patients receiving lorcaserin (∼47%) lost more than 5% body weight from baseline in comparison with the placebo group (∼25%; p < 0.05 in all studies). Those receiving the recommended dose of lorcaserin 10 mg twice daily lost on average ∼6 kg of body weight from baseline versus ∼3 kg with placebo. Patients with diabetes mellitus also saw significant reductions in their HbA1c with lorcaserin (∼0.9%) versus placebo (∼0.4%; p < 0.001). Lorcaserin is generally well tolerated with the most commonly experienced adverse events being nausea, dizziness, headache, upper respiratory tract infections, and nasopharyngitis. Cardiovascular evaluations showed no appreciable increase in valvulopathy with lorcaserin use versus placebo.
For now, pharmacists should continue to recommend the use of lorcaserin as a complement to, not in lieu of, ongoing lifestyle and behavioral modification.
肥胖已成为美国的一种流行病，其流行率持续上升。对于那些仅通过饮食和运动无法达到预期体重目标的患者，常辅助使用药物治疗。目前批准用于减肥的疗法包括苯丁胺、右苯丙胺、奥利司他和苯丁胺/托吡酯。本文旨在回顾洛卡塞林的地位，洛卡塞林是一种新型的 5-羟色胺 2C 激动剂，于 2012 年 7 月获得 FDA 批准。与当代的脂肪酶抑制剂和拟交感胺不同，洛卡塞林据称可减少食物摄入并增加饱腹感。
通过 MEDLINE、Web of Science 和 International Pharmaceutical Abstracts 使用与洛卡塞林相关的关键词，对截至 2013 年 1 月的所有相关文章进行了系统的文献回顾。
已发表了三项评估洛卡塞林在各种肥胖人群中的疗效和安全性的 III 期临床试验。与安慰剂组（25%）相比，接受洛卡塞林治疗的患者（47%）有更多的患者体重减轻超过基线的 5%（所有研究中均为 p<0.05）。接受推荐剂量的洛卡塞林 10mg 每日两次治疗的患者体重平均减轻约 6kg，而安慰剂组为3kg。患有糖尿病的患者接受洛卡塞林治疗后 HbA1c 也显著降低（0.9%比安慰剂组~0.4%；p<0.001）。洛卡塞林总体上耐受性良好，最常见的不良反应是恶心、头晕、头痛、上呼吸道感染和鼻咽炎。心血管评估显示，与安慰剂相比，洛卡塞林的使用并没有明显增加瓣膜病。
目前，药剂师应继续建议将洛卡塞林作为生活方式和行为改变的补充，而不是替代物。
