FDA十三年来首次批准Arena公司减肥药Belviq上市
药理类别：
5 - 羟色胺2C受体激动剂。
活性成分（S）：
lorcaserin的盐酸10mg的标签。
公司
卫材制药公司
指示（S）：
作为一个辅助低热量饮食和增加体力活动成年人慢性体重管理的初始BMI≥30kg/m2或≥27kg/m2的存在至少一个与体重相关的合并症（如高血压[HTN ]，血脂异常，2型糖尿病2型糖尿病）。
使用限制：其他减肥产品（例如，芬特明，OTC药品，草药PREPS）合用的安全性和有效性尚未确立。心血管疾病的发病率和死亡率的影响尚未建立。
药理作用：
lorcaserin的被认为是减少食品消费，促进饱足感，由位于下丘脑食欲亲阿黑皮素原神经元选择性5-HT2C受体激活。的确切作用机制是未知的。
临床试验：
Belviq慢性体重管理相结合，减少热量的摄入，增加体力活动的安全性和有效性进行了评估，三个随机，双盲，安慰剂对照的trials.The主要疗效参数是在1年内减肥，这是评估％的患者达到≥5％的重量损失，≥10％的重量损失，平均体重变化。
研究1是一个2年的研究，招收谁是肥胖（BMI 30-45kg/m2）或超重（BMI 27-29.9kg/m2）的有3,182例患者≥1与体重相关的合并症（如高血压或血脂异常）。在2年，继续服用安慰剂的患者和安慰剂Belviq患者重新随机2:1继续Belviq或切换到安慰剂。研究2是一项1年的研究中，4,008名谁是肥胖或超重，≥1与体重相关的合并症（如高血压或血脂异常）的患者。研究是为期1年的研究，招收604名患者与BMI≥27kg/m2，控制不佳的2型糖尿病的（糖化血红蛋白7-10％）与二甲双胍和/或磺脲类药物治疗。
在没有糖尿病的患者中，有统计学显着Belviq与安慰剂相比，在52周的减肥。 1年实现在Belviq治疗的患者是安慰剂调整减肥3.3千克（95％CI，-3.6，-2.9，P <0.001）。 ，47％的患者在Belviq治疗组失去≥5％的体重，22.4％，失去了≥10％的体重。在糖尿病患者中，有统计学显着更大的减肥Belviq比安慰剂。在的Belviq治疗组中，37.5％的患者失去体重≥5％，和16.3％≥10％体重丢失。
法律分类：
CIV
成人：
10毫克，每天两次。减肥12周后评估。停止如果没有达到≥5％的重量损失。
儿童：
<18岁：不推荐。
禁忌（S）：
怀孕（X类）。
警告/注意事项：
监测的5 - 羟色胺综合征或抗精神病药物恶性综合征样症状/体征;停止治疗如果发生。瑞士法郎。心脏瓣膜病的风险评估和考虑停止如果出现症状/体征。心动过缓或> 1度心脏传导阻滞。监测抑郁症，自杀的念头，和/或不寻常的行为改变，停止发展。增加低血糖的风险，与糖尿病患者降糖治疗开始前和治疗期间测量血糖。阴茎异常勃起的易感性。阴茎解剖变形。 CBCS治疗期间定期监控。如果怀疑高程测量催乳素水平。中度肾功能损害。严重肾功能不全或终末期肾病（ESRD）：不建议。严重肝功能损害。哺乳母亲：不推荐。
互动（补）
注意伴随曲普坦类药物，单胺氧化酶抑制剂，利奈唑胺，SNRIs的SSRIs类药物，三环类抗抑郁药，安非他酮，锂，曲马多，色氨酸，圣约翰草，抗精神病药物，或PDE-5抑制剂。增强效应右美沙芬和其他CYP2D6基板。心脏心瓣膜病伴药物，是有效的5-HT 2B受体激动剂（例如，卡麦角林）的风险增加。伴随胰岛素：没有研究过。
不良反应（S）
头痛，头晕，乏力，恶心，口干，便秘，低血糖，背部疼痛，咳嗽，认知障碍，心动过缓，精神紊乱，血液的变化，催乳素升高。
如何提供：
标签-60
最后更新：
2013年6月25日
FDA批准Belviq用于体重控制
2012年7月12日，FDA批准Belviq(lorcaserin HCl)用于肥胖成年人的慢性体重控制。Belviq作为针对在肥胖成年患者当中低卡热量饮食和较多的增加运动的一种补充品，这些患者的最初的身体质量指数（BMI）为30kg/㎡或更高（肥胖），或者至少伴随一种与体重相关的疾病（如，高血压、血脂异常、2型糖尿病）时BMI值为27kg/㎡或更高（超重）。指示包括以下使用限制：服用Belviq 的同时还服用别的药物时会不会达到减肥目的的安全性和疗效还有待进一步验证，并且使用Belviq 对心血管疾病的发病率和死亡率会不会产生影响也还不确定。
Belviq的使用对于那些和肥胖做斗争的还有伴有并发症的体重超重的需要通过慢性体重管理来代替饮食和锻炼的患者来说是件很重要的一种举措。
Belviq的双盲试验，随机对照试验和安慰剂对照试验这三项试验证实了Belviq在饮食和锻炼中服用在帮助患者病人减轻体重方面所产生的效应，比起只有饮食和锻炼更加有效，经过一年他们的体重减轻了5%或更多，并且管理减肥治疗长达两年。
临床试验中，那些使用了Belviq的非糖尿病患者最常见的不良反应是头痛，头晕，乏力，口干和便秘。而那些糖尿病患者当中，最常见的不良反应是：低糖血症，头痛，背痛，咳嗽和乏力。
提示：使用时请仔细阅读完整资料[附件]：http://www.drugs.com/pro/belviq.html
Pharmacological Class:
Serotonin 2C receptor agonist.
Active Ingredient(s):
Lorcaserin HCl 10mg; tabs.
Company
Eisai Pharmaceuticals
Indication(s):
As an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with an initial BMI of ≥30kg/m2 or ≥27kg/m2 in the presence of at least one weight-related comorbidity (eg, hypertension [HTN], dyslipidemia, type 2 diabetes mellitus [T2DM]).
Limitations of use: safety and efficacy of coadministration with other weight loss products (eg, phentermine, OTC drugs, herbal preps) have not been established. Effect on cardiovascular morbidity and mortality has not been established.
Pharmacology:
Lorcaserin is believed to decrease food consumption and promote satiety by selectively activating 5-HT2C receptors on anorexigenic pro-opiomelanocortin neurons located in the hypothalamus. The exact mechanism of action is unknown.
Clinical Trials:
The safety and efficacy of Belviq for chronic weight management in conjunction with reduced caloric intake and increased physical activity were evaluated in three randomized, double-blind, placebo-controlled trials.The primary efficacy parameter was weight loss at 1 year, which was assessed by percent of patients achieving ≥5% weight loss, ≥10% weight loss, and mean weight change.
Study 1 was a 2-year study that enrolled 3,182 patients who were obese (BMI 30–45kg/m2) or overweight (BMI 27–29.9kg/m2) and had ≥1 weight-related comorbidity (eg, HTN or dyslipidemia). In Year 2, placebo patients were continued on placebo and Belviq patients were re-randomized 2:1 to continue Belviq or switch to placebo. Study 2 was a 1-year study that enrolled 4,008 patients who were obese or overweight and had ≥1 weight-related comorbidity (eg, HTN or dyslipidemia). Study 3 was a 1-year study that enrolled 604 patients with BMI ≥27kg/m2 and inadequately controlled T2DM (HbA1c 7–10%) being treated with metformin and/or a sulfonylurea.
In patients without diabetes, there was statistically significant greater weight loss with Belviq vs. placebo at Week 52. The Year 1 placebo-adjusted weight loss achieved in patients treated with Belviq was 3.3kg (95% CI, -3.6, -2.9; P<0.001). In the Belviq treatment group, 47% of patients lost ≥5% body weight, and 22.4% lost ≥10% body weight. In patients with diabetes, there was statistically significantly greater weight loss with Belviq than with placebo. In the Belviq treatment group, 37.5% of patients lost ≥5% body weight, and 16.3% lost ≥10% body weight.
Legal Classification:
CIV
Adults:
10mg twice daily. Evaluate weight loss after 12 weeks. Discontinue if ≥5% weight loss is not achieved.
Children:
<18 years: not recommended.
Contraindication(s):
Pregnancy (Category X).
Warnings/Precautions:
Monitor for serotonin syndrome or neuroleptic malignant syndrome-like signs/symptoms; discontinue and treat if occur. CHF. Risk of valvular heart disease; evaluate and consider discontinuing if signs/symptoms occur. Bradycardia or >1st degree heart block. Monitor for depression, suicidal thoughts, and/or unusual behavioral changes; discontinue if develop. Increase risk of hypoglycemia in patients with diabetes on antidiabetic therapy; measure blood glucose prior to starting and during treatment. Predisposition to priapism. Anatomical penile deformation. Monitor CBCs periodically during therapy. Measure prolactin levels if elevation is suspected. Moderate renal impairment. Severe renal impairment or ESRD: not recommended. Severe hepatic impairment. Nursing mothers: not recommended.
Interaction(s)
Caution with concomitant triptans, MAOIs, linezolid, SSRIs, SNRIs, TCAs, bupropion, lithium, tramadol, tryptophan, St. John’s wort, antipsychotics, or PDE-5 inhibitors. Potentiates dextromethorphan and other CYP2D6 substrates. Increased risk of cardiac valvulopathy with concomitant drugs that are potent 5-HT2B receptor agonists (eg, cabergoline). Concomitant insulin: not studied.
Adverse Reaction(s)
Headache, dizziness, fatigue, nausea, dry mouth, constipation, hypoglycemia, back pain, cough; cognitive impairment, bradycardia, psychiatric disorders, hematological changes, prolactin elevation.
How Supplied:
Tabs—60