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恩格列净/利拉利汀:用于 2 型糖尿病的治疗。

Empagliflozin/Linagliptin: A Review in Type 2 Diabetes.

机构信息

Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand,

出版信息

Drugs. 2015 Sep;75(13):1547-57. doi: 10.1007/s40265-015-0457-z.

DOI:10.1007/s40265-015-0457-z
PMID:26323340
Abstract

Empagliflozin/linagliptin (Glyxambi(®)) is a once-daily sodium glucose co-transporter type 2 (SGLT2) inhibitor and dipeptidyl peptidase (DPP)-4 inhibitor fixed-dose combination product that is approved in the USA as an adjunct to diet and exercise in adults with type 2 diabetes (T2D) when treatment with both empagliflozin and linagliptin is appropriate. This article reviews the clinical efficacy and tolerability of oral empagliflozin/linagliptin in patients with T2D and summarizes the pharmacological properties of the agents. Results of two randomized controlled trials of 52 weeks' duration in adults with T2D demonstrated that empagliflozin/linagliptin improved glycaemic control significantly more than linagliptin when administered as initial therapy (whereas results vs. empagliflozin were mixed in this setting) and significantly more than linagliptin or empagliflozin when administered as an add-on therapy to metformin. In addition to glycaemic control, empagliflozin/linagliptin provided significant weight loss compared with linagliptin in both trials. Empagliflozin/linagliptin was generally well tolerated in patients with T2D, with a low risk of hypoglycaemia and no reports of exacerbations of, or hospitalizations for, heart failure during the trials. As the first SGLT2 inhibitor/DPP-4 inhibitor fixed-dose combination available, empagliflozin/linagliptin is a useful new option for patients with T2D.

摘要

恩格列净/利拉利汀(甘精胰岛素/利拉利汀)是一种每日一次的钠-葡萄糖共转运蛋白 2(SGLT2)抑制剂和二肽基肽酶-4(DPP-4)抑制剂固定剂量复方制剂,在美国被批准作为饮食和运动的辅助治疗,用于 2 型糖尿病(T2D)成人患者,当恩格列净和利拉利汀的治疗都适用时。本文回顾了恩格列净/利拉利汀在 T2D 患者中的临床疗效和耐受性,并总结了这些药物的药理学特性。两项为期 52 周的成人 T2D 随机对照试验的结果表明,与利拉利汀相比,恩格列净/利拉利汀作为初始治疗时显著改善了血糖控制(而在这种情况下,与恩格列净相比结果则不一致),并且作为二甲双胍的附加治疗时也显著优于利拉利汀或恩格列净。除了血糖控制,与利拉利汀相比,恩格列净/利拉利汀在两项试验中均显著减轻了体重。在 T2D 患者中,恩格列净/利拉利汀总体耐受性良好,低血糖风险低,试验期间没有心力衰竭恶化或因心力衰竭住院的报告。作为首个 SGLT2 抑制剂/DPP-4 抑制剂固定剂量复方制剂,恩格列净/利拉利汀是 T2D 患者的一种有用的新选择。

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Empagliflozin/Linagliptin: A Review in Type 2 Diabetes.恩格列净/利拉利汀:用于 2 型糖尿病的治疗。
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Empagliflozin/Linagliptin: Combination therapy in patients with type 2 diabetes.恩格列净/利格列汀:2型糖尿病患者的联合治疗
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本文引用的文献

1
Empagliflozin (BI 10773), a Potent and Selective SGLT2 Inhibitor, Induces Dose-Dependent Glucosuria in Healthy Subjects.恩格列净(BI 10773),一种强效且选择性的 SGLT2 抑制剂,可在健康受试者中引起剂量依赖性的糖尿。
Clin Pharmacol Drug Dev. 2013 Apr;2(2):152-61. doi: 10.1002/cpdd.16. Epub 2013 Mar 27.
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SGLT2 Inhibitors May Predispose to Ketoacidosis.钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂可能易引发酮症酸中毒。
J Clin Endocrinol Metab. 2015 Aug;100(8):2849-52. doi: 10.1210/jc.2015-1884. Epub 2015 Jun 18.
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Euglycemic Diabetic Ketoacidosis: A Potential Complication of Treatment With Sodium-Glucose Cotransporter 2 Inhibition.
Exploring the recent molecular targets for diabetes and associated complications.
探讨糖尿病及其相关并发症的近期分子靶点。
Mol Biol Rep. 2021 Mar;48(3):2863-2879. doi: 10.1007/s11033-021-06294-0. Epub 2021 Mar 24.
4
Postoperative Euglycemic Diabetic Ketoacidosis and Encephalopathy Related to SGLT-2 Inhibitors: A Case Report and Discussion of Diabetes Treatment and "Sweet Pee Encephalopathy" in Perioperative Hospital Management.与SGLT-2抑制剂相关的术后血糖正常性糖尿病酮症酸中毒和脑病:1例病例报告及围手术期医院管理中糖尿病治疗与“甜尿脑病”的讨论
Neurohospitalist. 2020 Jan;10(1):51-54. doi: 10.1177/1941874419835035. Epub 2019 Mar 7.
5
The role of dipeptidylpeptidase-4 inhibitors in management of cardiovascular disease in diabetes; focus on linagliptin.二肽基肽酶-4 抑制剂在糖尿病心血管疾病管理中的作用;以利格列汀为例。
Cardiovasc Diabetol. 2018 Apr 18;17(1):59. doi: 10.1186/s12933-018-0704-1.
6
Pharmacokinetic Characteristics and Clinical Efficacy of an SGLT2 Inhibitor Plus DPP-4 Inhibitor Combination Therapy in Type 2 Diabetes.SGLT2抑制剂联合DPP-4抑制剂治疗2型糖尿病的药代动力学特征及临床疗效
Clin Pharmacokinet. 2017 Jul;56(7):703-718. doi: 10.1007/s40262-016-0498-9.
正常血糖性糖尿病酮症酸中毒:钠-葡萄糖协同转运蛋白2抑制剂治疗的一种潜在并发症。
Diabetes Care. 2015 Sep;38(9):1687-93. doi: 10.2337/dc15-0843. Epub 2015 Jun 15.
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Effect of Sitagliptin on Cardiovascular Outcomes in Type 2 Diabetes.西格列汀对 2 型糖尿病患者心血管结局的影响。
N Engl J Med. 2015 Jul 16;373(3):232-42. doi: 10.1056/NEJMoa1501352. Epub 2015 Jun 8.
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AACE/ACE comprehensive diabetes management algorithm 2015.美国临床内分泌医师协会/美国内分泌学会2015年糖尿病综合管理算法
Endocr Pract. 2015 Apr;21(4):438-47. doi: 10.4158/EP15693.CS. Epub 2015 Apr 15.
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American association of clinical endocrinologists and american college of endocrinology - clinical practice guidelines for developing a diabetes mellitus comprehensive care plan - 2015.美国临床内分泌医师协会和美国内分泌学会——糖尿病综合护理计划制定临床实践指南——2015年
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Heart failure and mortality outcomes in patients with type 2 diabetes taking alogliptin versus placebo in EXAMINE: a multicentre, randomised, double-blind trial.在 EXAMINE 研究中,比较阿格列汀与安慰剂治疗 2 型糖尿病患者的心力衰竭和死亡率结局:一项多中心、随机、双盲试验。
Lancet. 2015 May 23;385(9982):2067-76. doi: 10.1016/S0140-6736(14)62225-X. Epub 2015 Mar 10.
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Where does combination therapy with an SGLT2 inhibitor plus a DPP-4 inhibitor fit in the management of type 2 diabetes?钠-葡萄糖协同转运蛋白2(SGLT2)抑制剂联合二肽基肽酶-4(DPP-4)抑制剂的联合疗法在2型糖尿病管理中处于什么地位?
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Initial combination of empagliflozin and linagliptin in subjects with type 2 diabetes.恩格列净和利拉利汀联合治疗 2 型糖尿病患者。
Diabetes Care. 2015 Mar;38(3):394-402. doi: 10.2337/dc14-2365. Epub 2015 Jan 29.