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首页 > 医学词汇大全 > Lorcaserin
Lorcaserin

内分泌

关键词内分泌 治疗药物 内分泌

词汇介绍

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解析

Lorcaserin

释    义   n. 氯卡色林

例    句   Wall Street analysts considered lorcaserin the most likely of three diet drugs before the FDA to succeed because it seemed to present fewer safety issues. 华尔街分析家认为氯卡色林很有可能在美国食品药品监督管理局批准之前三种减肥药中最成功的一个,因为该药物安全问题最少。

概述

概述


氯卡色林用于帮助肥胖或超重且患有与体重有关的医学问题的成年人减轻体重,并防止体重增加。氯卡色林必须与减少卡路里的饮食和运动计划一起使用,氯卡色林是一类称为5-羟色胺受体激动剂的药物,它通过增加饱腹感而起作用,从而减少了食物的摄入。氯卡色林可作为片剂和口服缓释(长效)片剂使用,缓释片剂通常每天与食物或不与食物一起服用,每天大约在同一时间服用氯卡色林。


不良反应


最常见的不良反应是恶心,呕吐,便秘,腹泻,疲劳,上呼吸道感染,尿路感染,背痛,头痛,头晕,和皮疹。如氯卡色林影响血清素受体,血清素综合征可以通过影响血清素神经递质(如选择性血清素再摄取抑制剂)的药物或草本产品沉淀。接受氯卡色林的患者有1.9%的注意力和记忆力下降,而安慰剂则为0.5%。患者应监测是否有抑郁症的迹象和症状或已经存在的抑郁症恶化,尤其是自杀倾向的发展。二尖瓣或主动脉瓣反流性瓣膜病患者的5-HT 2B受体表达增加,如在超治疗剂量下,氯卡色林可以激活5-HT 2B,这可能导致瓣膜病。还应监测患者的低血糖情况,尤其是糖尿病患者,因为体重减轻会加剧低血糖的趋势。临床前研究中已经报道了精神分裂症,但在临床试验中未见。白细胞和红血球减少与安慰剂的0.2%和1.2%相比,细胞的比例分别为0.4%和1.3%。氯卡西林还显示某些患者的催乳素水平适度增加。氯卡色林在怀孕期间是禁忌症,属于X类,因为在怀孕期间无法监测体重减轻,不知道它是否会从人乳中排出。18岁以下的患者尚未进行研究,因此儿科数据是不存在。对于轻度至中度的肾脏和肝病,无需调整剂量。


注意事项


在服用氯卡色林之前,告诉医生和药剂师是否对氯卡色林,任何其他药物或氯卡色林片剂或缓释片剂中的任何成分过敏。告诉医生是否有过血液细胞问题,例如镰状细胞性贫血(红细胞疾病),多发性骨髓瘤(浆细胞癌)或白血病(白细胞癌);影响阴茎形状的疾病,例如成角度,海绵体纤维化或佩罗尼氏病;糖尿病;心力衰竭,心律缓慢或不规则或其他心脏问题;或肝脏或肾脏疾病。服用氯卡色林时请勿母乳喂养。如果正在接受外科手术,包括牙科手术,请告诉医生或牙医正在服用氯卡色林。氯卡色林可能会导致嗜睡和难以集中注意力,因此,在知道这种药物如何影响您之前,请勿驾驶汽车或操作机械。

Improvements in albuminuria and chronic kidney disease progression with the appetite suppressant lorcaserin复制标题

通过食欲抑制剂lorcaserin改善蛋白尿和慢性肾脏疾病进展

发表时间:2019-05-01

影响指数:8.3

作者: Peter Rossing

期刊:Kidney Int

Obesity is an established risk factor for chronic kidney disease (CKD) and has been associated with both impaired kidney function and albuminuria, reflecting a broad spectrum of underlying pathology. Proposed mechanisms include hemodynamic effects, with increased glomerular pressure leading to hyperfiltration and albuminuria, with subsequent declines in kidney function, as well as possible adverse effects of adipokines on podocyte health. In contrast to the well-established relationship between obesity and CKD, whether intentional weight loss improves kidney disease outcomes has been debated. This possibility was recently evaluated in a secondary analysis of a large randomized placebo-controlled trial, CAMELLIATIMI 61 (Cardiovascular and Metabolic Effects of Lorcaserin in Overweight and Obese Patients). The CAMELLIA trial evaluated the cardiovascular safety of lorcaserin, a selective agonist of the 5-hydroxytryptamine (serotonin) 2C receptor that suppresses appetite through hypothalamic effects, in comparison with placebo, both in addition to behavioral counseling. Participants were overweight or obese adults either with or at high risk for cardiovascular disease. A prespecified secondary analysis assessed the impact of weight loss with lorcaserin versus placebo on development of a combined endpoint of new or worsening micro-or macro-albuminuria, new or worsening CKD, doubling of serum creatinine, end-stage renal disease, kidney transplant, or renal death. At baseline, the median estimated glomerular filtration rate (eGFR) was 76 ml/min per 1.73 m2 (interquartile range: 63–89 ml/min per 1.73 m2 ), approximately 20% of participants had a baseline eGFR. During a median of 3.3 years of follow up, a significant 13% reduction occurred in the combined CKD endpoint in the lorcaserin arm (hazard ratio 0.87; 95% confidence interval 0.79– 0.96). This change was driven by a significant reduction in the number of participants with new or worsening albuminuria (2.7% vs. 3.1%; HR 0.86, 95% CI 0.76–0.97) and new or worsening CKD stage (2.4% vs. 2.9%; HR 0.81, 95% CI 0.72–0.93). Other endpoints, including end-stage renal disease and 30% or 40% decline in eGFR, were rare, reflecting the relatively low CKD risk in the study population. The treatment effect was larger in the small subgroup without hypertension, but treatment effect had no interaction with baseline CKD stage, diabetes status, albuminuria level, or any other clinical characteristic. Modest effects on hemoglobin A1c and blood pressure did not fully explain the findings.

译文

肥胖是慢性肾脏病(CKD)的既定危险因素,与肾脏功能受损和蛋白尿有关,反映出广泛的潜在病理学。拟议的机制包括血液动力学效应,肾小球压力增高导致超滤和蛋白尿,随后肾功能下降,以及脂肪因子对足细胞健康的可能不利影响。与肥胖和CKD之间公认的关系相反,有意减肥是否可以改善肾脏疾病的结局一直存在争议。最近,在一项大型的随机安慰剂对照试验CAMELLIATIMI 61(洛卡斯汀对超重和肥胖患者的心血管和代谢作用)的二级分析中评估了这种可能性。 CAMELLIA试验评估了氯色林(lorcaserin)的心血管安全性,氯色林是5-羟色胺(5-羟色胺)2C受体的选择性激动剂,与安慰剂相比,它通过下丘脑作用抑制食欲。参与者是患有心血管疾病或处于心血管疾病高风险中的超重或肥胖成年人。预先进行的二级分析评估了氯卡色林与安慰剂相比,体重减轻对新的或恶化的微量或巨蛋白尿,新的或恶化的CKD,血清肌酐增加一倍,终末期肾脏疾病,肾脏移植,或肾脏死亡。在基线时,估计的肾小球滤过率中位数(eGFR)为每1.73平方米76毫升/分钟(四分位数范围:每1.73平方米为63-89毫升/分钟),约有20%的参与者具有基线eGFR。在平均3.3年的随访期间,洛卡塞林组的CKD联合终点显着降低了13%(危险比0.87; 95%置信区间0.79-0.96)。这种变化是由于新的或恶化的白蛋白尿参与者人数显着减少(2.7%比3.1%; HR 0.86,95%CI 0.76-0.97)和新的或恶化的CKD阶段(2.4%比2.9%)所致。 HR 0.81,95%CI 0.72-0.93)。其他终点(包括终末期肾脏疾病和eGFR下降30%或40%)很少见,这反映了研究人群中相对较低的CKD风险。在没有高血压的小亚组中,治疗效果较大,但治疗效果与基线CKD分期,糖尿病状态,蛋白尿水平或任何其他临床特征没有相互作用。对血红蛋白A1c和血压的适度影响不能完全解释这一发现。