Alruwaili Heshma, Dehestani Babak, le Roux Carel W
Diabetes Complications Research Centre, Conway Institute, University College Dublin, Dublin, Ireland.
Diabetes Research Group, School of Biomedical Sciences, Ulster University, Belfast, UK.
Clin Pharmacol. 2021 Mar 11;13:53-60. doi: 10.2147/CPAA.S276085. eCollection 2021.
Obesity is defined as a chronic, complex, relapsing disease characterized by excessive adipose tissue. Obesity impacts an individual's health by increasing complications such as prediabetes, type 2 diabetes mellitus (T2DM), hypertension, dyslipidemia, metabolic syndrome, cardiovascular disease, nonalcoholic fatty liver disease (NAFLD), cancers (eg endometrial), and obstructive sleep apnea (OSA). With the increase of obesity prevalence and its negative influences on individuals' quality of life, there is a great need for therapy with a purpose to produce sustainable weight loss of more than 10% in order to improve or even reverse the progress of obesity related complications. The GLP-1 analogue, liraglutide reduce food consumption, promote weight reduction and improve metabolic functions. The primary mechanism of GLP-1 effect on food intake, metabolism, and weight reduction is mainly due to its actions on peripheral (vagal) and central pathways and activation of hindbrain and hypothalamus. The average weight reduction induced by liraglutide was significant and the weight loss was maintained as long as the patients on therapy. Liraglutide has advantages on weight loss maintenance and promoting cardiovascular disease (CVD) risk reduction, by decreasing systolic blood pressure and glycemic index. In this review, we aim to explain the mechanism of action of Liraglutide, its pharmacokinetic properties, its clinical impact on obesity and its safety and tolerability.
肥胖被定义为一种以脂肪组织过多为特征的慢性、复杂、复发性疾病。肥胖通过增加诸如糖尿病前期、2型糖尿病(T2DM)、高血压、血脂异常、代谢综合征、心血管疾病、非酒精性脂肪性肝病(NAFLD)、癌症(如子宫内膜癌)和阻塞性睡眠呼吸暂停(OSA)等并发症来影响个体健康。随着肥胖患病率的上升及其对个体生活质量的负面影响,迫切需要一种能够实现超过10%的可持续体重减轻的治疗方法,以改善甚至逆转肥胖相关并发症的进展。胰高血糖素样肽-1(GLP-1)类似物利拉鲁肽可减少食物摄入、促进体重减轻并改善代谢功能。GLP-1对食物摄入、代谢和体重减轻产生作用的主要机制主要归因于其对外周(迷走神经)和中枢途径的作用以及对后脑和下丘脑的激活。利拉鲁肽诱导的平均体重减轻显著,并且只要患者接受治疗,体重减轻就能维持。利拉鲁肽在维持体重减轻和促进降低心血管疾病(CVD)风险方面具有优势,可降低收缩压和血糖指数。在本综述中,我们旨在解释利拉鲁肽的作用机制、其药代动力学特性、其对肥胖的临床影响以及其安全性和耐受性。