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2
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[Pharmacological therapy of obesity].[肥胖症的药物治疗]
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本文引用的文献

1
Effect of lorcaserin on prevention and remission of type 2 diabetes in overweight and obese patients (CAMELLIA-TIMI 61): a randomised, placebo-controlled trial.盐酸氯卡色林对超重和肥胖 2 型糖尿病患者预防和缓解作用的研究(CAMELLIA-TIMI 61):一项随机、安慰剂对照试验。
Lancet. 2018 Nov 24;392(10161):2269-2279. doi: 10.1016/S0140-6736(18)32328-6. Epub 2018 Oct 4.
2
Cardiovascular Safety of Lorcaserin in Overweight or Obese Patients.盐酸氯卡色林在超重或肥胖患者中的心血管安全性。
N Engl J Med. 2018 Sep 20;379(12):1107-1117. doi: 10.1056/NEJMoa1808721. Epub 2018 Aug 26.
3
Effect of lorcaserin on glycemic parameters in patients with type 2 diabetes mellitus.氯卡色林对2型糖尿病患者血糖参数的影响。
Obesity (Silver Spring). 2017 May;25(5):842-849. doi: 10.1002/oby.21798. Epub 2017 Mar 27.
4
Lorcaserin Administration Decreases Activation of Brain Centers in Response to Food Cues and These Emotion- and Salience-Related Changes Correlate With Weight Loss Effects: A 4-Week-Long Randomized, Placebo-Controlled, Double-Blind Clinical Trial.洛卡塞林给药可降低大脑中枢对食物线索的反应性激活,且这些与情绪和显著性相关的变化与体重减轻效果相关:一项为期4周的随机、安慰剂对照、双盲临床试验。
Diabetes. 2016 Oct;65(10):2943-53. doi: 10.2337/db16-0635. Epub 2016 Jul 6.
5
5-HT2C receptor agonist anorectic efficacy potentiated by 5-HT1B receptor agonist coapplication: an effect mediated via increased proportion of pro-opiomelanocortin neurons activated.5-HT2C 受体激动剂与 5-HT1B 受体激动剂联合应用增强了食欲抑制作用:这种作用是通过增加被激活的 pro-opiomelanocortin 神经元的比例来介导的。
J Neurosci. 2013 Jun 5;33(23):9800-4. doi: 10.1523/JNEUROSCI.4326-12.2013.
6
Randomized placebo-controlled clinical trial of lorcaserin for weight loss in type 2 diabetes mellitus: the BLOOM-DM study.BLOOM-DM 研究:用于治疗 2 型糖尿病患者体重的乐卡司汀随机安慰剂对照临床试验。
Obesity (Silver Spring). 2012 Jul;20(7):1426-36. doi: 10.1038/oby.2012.66. Epub 2012 Mar 16.
7
A one-year randomized trial of lorcaserin for weight loss in obese and overweight adults: the BLOSSOM trial.一项为期一年的用于肥胖和超重成年人减肥的lorcaserin 随机试验:BLOSSOM 试验。
J Clin Endocrinol Metab. 2011 Oct;96(10):3067-77. doi: 10.1210/jc.2011-1256. Epub 2011 Jul 27.
8
Multicenter, placebo-controlled trial of lorcaserin for weight management.多中心、安慰剂对照的氯卡色林用于体重管理的试验。
N Engl J Med. 2010 Jul 15;363(3):245-56. doi: 10.1056/NEJMoa0909809.
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HDL particle size and the risk of coronary heart disease in apparently healthy men and women: the EPIC-Norfolk prospective population study.高密度脂蛋白颗粒大小与健康男性和女性患冠心病的风险:欧洲癌症与营养前瞻性调查诺福克队列前瞻性人群研究
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Low-density lipoprotein and high-density lipoprotein particle subclasses predict coronary events and are favorably changed by gemfibrozil therapy in the Veterans Affairs High-Density Lipoprotein Intervention Trial.在退伍军人事务部高密度脂蛋白干预试验中,低密度脂蛋白和高密度脂蛋白颗粒亚类可预测冠状动脉事件,并且吉非贝齐治疗可使其发生有利变化。
Circulation. 2006 Mar 28;113(12):1556-63. doi: 10.1161/CIRCULATIONAHA.105.565135. Epub 2006 Mar 13.

盐酸氯卡色林治疗肥胖症成人,可降低体重和心血管代谢风险因素:一项为期 6 个月、随机、安慰剂对照、双盲临床试验。

Lorcaserin treatment decreases body weight and reduces cardiometabolic risk factors in obese adults: A six-month, randomized, placebo-controlled, double-blind clinical trial.

机构信息

Division of Endocrinology, Diabetes and Metabolism, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.

Department of Medicine, Division of Infectious Diseases, UCLA David Geffen School of Medicine, Los Angels, California.

出版信息

Diabetes Obes Metab. 2019 Jun;21(6):1487-1492. doi: 10.1111/dom.13655. Epub 2019 Mar 18.

DOI:10.1111/dom.13655
PMID:30724455
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6504613/
Abstract

Lorcaserin is a serotonin 2c receptor agonist that promotes weight loss while contributing to the prevention and improvement of type 2 diabetes and improvement of atherogenic lipid profiles, without higher rates of major cardiovascular events. The full spectrum of possible lorcaserin-induced improvements in cardiometabolic health remains to be clarified. Thus, we investigated the way in which lorcaserin treatment may alter cardiovascular disease risk, either independently or through changes in body weight. We measured, for the first time, lipid particle quantification, lipid peroxidation, appetite-regulating hormones and mRNA expression of the 5-hydroxytryptamine 2c receptor (5-HT2c receptor). A total of 48 obese participants were enrolled in this six-month, randomized (1:1), placebo-controlled, double-blinded clinical trial. Lorcaserin treatment reduced fat mass (P < 0.001), the fatty liver index (P < 0.0001) and energy intake (P < 0.03) without affecting energy expenditure or lean mass. Total low-density lipoprotein (LDL) (P < 0.04) and small LDL particles (P < 0.03) decreased, while total high-density lipoprotein (HDL) P < 0.02) increased and heart rate significantly decreased with lorcaserin treatment. No mRNA expression of the 5-HT2c receptor was observed in peripheral organs. These data suggest that lorcaserin treatment for six months improves cardiometabolic health in obese individuals, acting mainly through the brain.

摘要

盐酸氯卡色林是一种血清素 2C 受体激动剂,可在预防和改善 2 型糖尿病和改善动脉粥样硬化脂质谱的同时促进体重减轻,而不会增加主要心血管事件的发生率。盐酸氯卡色林可能改善心血代谢健康的全部范围仍有待阐明。因此,我们研究了盐酸氯卡色林治疗可能通过改变体重或通过其他方式改变心血管疾病风险的方式。我们首次测量了脂质颗粒定量、脂质过氧化、调节食欲的激素和 5-羟色胺 2C 受体(5-HT2c 受体)的 mRNA 表达。共有 48 名肥胖参与者参与了这项为期 6 个月的、随机(1:1)、安慰剂对照、双盲临床试验。盐酸氯卡色林治疗可降低脂肪量(P<0.001)、脂肪肝指数(P<0.0001)和能量摄入(P<0.03),而不影响能量消耗或瘦体重。总低密度脂蛋白(LDL)(P<0.04)和小 LDL 颗粒(P<0.03)减少,而总高密度脂蛋白(HDL)(P<0.02)增加,心率明显下降。外周器官中未观察到 5-HT2c 受体的 mRNA 表达。这些数据表明,盐酸氯卡色林治疗 6 个月可改善肥胖个体的心血代谢健康,主要通过大脑发挥作用。