中华内分泌代谢杂志
中華內分泌代謝雜誌
중화내분비대사잡지
CHINESE JOURNAL OF ENDOCRINOLOGY AND METABOLISM
2012年
9期
后插1-后插7
,共1页
肠促胰素%糖尿病,2型%胰升糖素样肽1受体激动剂%二肽基肽酶4抑制剂
腸促胰素%糖尿病,2型%胰升糖素樣肽1受體激動劑%二肽基肽酶4抑製劑
장촉이소%당뇨병,2형%이승당소양태1수체격동제%이태기태매4억제제
Incretins%Diabetes mellitus,type 2%Glucagon-like peptide 1 receptor agonist%Dipeptidylpeptidase 4 inhibitor
随着对肠促胰素在维持葡萄糖稳定作用认识的日益增多,促进了针对2型糖尿病患者肠促胰素活性缺乏治疗药物的研发.根据肠促胰素治疗药物不同的作用机制,可分为以下2类:(1)胰升糖素样肽1(GLP-1)受体激动剂,包括利拉鲁肽(liraglutide)、艾塞那肽每日2次制剂和艾塞那肽每周1次制剂；(2)二肽基肽酶4(DPP-4)抑制剂,包括西格列汀(sitagliptin)、利拉利汀(linagliptin)、沙格列汀(saxagliptin)和维格列汀(vildagliptin),DPP-4抑制剂可限制内源性GLP-1的降解.这2类药物具有某些共性,如葡萄糖依赖性刺激胰岛素分泌,低血糖发生率低.然而这2类药物在疗效方面的表现却有所不同.本文综述了这2类基于肠促胰素治疗药物的药代动力学及其临床方面的疗效和安全性,阐明了此类药物在2型糖尿病治疗中的地位.
隨著對腸促胰素在維持葡萄糖穩定作用認識的日益增多,促進瞭針對2型糖尿病患者腸促胰素活性缺乏治療藥物的研髮.根據腸促胰素治療藥物不同的作用機製,可分為以下2類:(1)胰升糖素樣肽1(GLP-1)受體激動劑,包括利拉魯肽(liraglutide)、艾塞那肽每日2次製劑和艾塞那肽每週1次製劑；(2)二肽基肽酶4(DPP-4)抑製劑,包括西格列汀(sitagliptin)、利拉利汀(linagliptin)、沙格列汀(saxagliptin)和維格列汀(vildagliptin),DPP-4抑製劑可限製內源性GLP-1的降解.這2類藥物具有某些共性,如葡萄糖依賴性刺激胰島素分泌,低血糖髮生率低.然而這2類藥物在療效方麵的錶現卻有所不同.本文綜述瞭這2類基于腸促胰素治療藥物的藥代動力學及其臨床方麵的療效和安全性,闡明瞭此類藥物在2型糖尿病治療中的地位.
수착대장촉이소재유지포도당은정작용인식적일익증다,촉진료침대2형당뇨병환자장촉이소활성결핍치료약물적연발.근거장촉이소치료약물불동적작용궤제,가분위이하2류:(1)이승당소양태1(GLP-1)수체격동제,포괄리랍로태(liraglutide)、애새나태매일2차제제화애새나태매주1차제제；(2)이태기태매4(DPP-4)억제제,포괄서격렬정(sitagliptin)、리랍리정(linagliptin)、사격렬정(saxagliptin)화유격렬정(vildagliptin),DPP-4억제제가한제내원성GLP-1적강해.저2류약물구유모사공성,여포도당의뢰성자격이도소분비,저혈당발생솔저.연이저2류약물재료효방면적표현각유소불동.본문종술료저2류기우장촉이소치료약물적약대동역학급기림상방면적료효화안전성,천명료차류약물재2형당뇨병치료중적지위.
Increased understanding of the role of incretin hormones in maintaining glucose homeostasis has enabled the development of pharmacotherapies that target deficient incretin activity in type 2 diabetes mellitus.lncretin-based therapies could be classified into 2 categories with different mechanisms of action:glucagon-like peptide 1 ( GLP-1 ) receptor agonists ( e.g.liraglutide,exenatide twice daily,and exenatide once weekly),and the dipeptidyl peptidase 4 ( DPP-4 ) inhibitors ( e.g.sitagliptin,linagliptin,saxagliptin,and vildagliptin),which inhibit the breakdown of endogenous GLP-1.Both categories share some specific characteristics,such as glucose-dependent insulin stimulation and low incidence of hypoglycemia.But there are also different profiles in efficacy between these 2 classes.This article reviews the pharmacokinetics and clinical aspects of efficacy and safety of these 2 classes of incretin-based therapies and elucidates their roles in treating type 2 diabetes mellitus.
