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阿必鲁肽:一种用于2型糖尿病的每周一次胰高血糖素样肽-1受体激动剂。

Albiglutide: A once-weekly glucagon-like peptide-1 receptor agonist for type 2 diabetes mellitus.

作者信息

Davis Portia N, Ndefo Uche Anadu, Oliver Ashley, Payton Enryka

机构信息

Portia N. Davis, Pharm.D., is Assistant Professor of Pharmacy Practice, Texas Southern University (TSU) College of Pharmacy and Health Sciences, and Clinical Pharmacy Specialist, Ambulatory Care, San José Clinic, Houston. Uche Anadu Ndefo, Pharm.D., BCPS, is Associate Professor of Pharmacy Practice; Ashley Oliver is a Pharm.D. student; and Enryka Payton is a Pharm.D. student, TSU College of Pharmacy and Health Sciences.

出版信息

Am J Health Syst Pharm. 2015 Jul 1;72(13):1097-103. doi: 10.2146/ajhp140260.

Abstract

PURPOSE

The pharmacology, pharmacokinetics, efficacy, safety, dosage and administration, and place in therapy of the glucagon-like peptide-1 (GLP-1) receptor agonist albiglutide are reviewed.

SUMMARY

Albiglutide (Tanzeum, GlaxoSmithKline) is an injectable GLP-1 agonist approved in 2014 for use as an adjunct to diet modification and exercise to improve glycemic control in adults with type 2 diabetes. Albiglutide augments glucose-dependent insulin secretion and slows gastric emptying; it has an elimination half-life of approximately five days, allowing for once-weekly administration. Clinical trials demonstrated mean absolute reductions in glycosylated hemoglobin (HbA1c) values of 0.78-1.55% after 16 weeks of adjunctive therapy with albiglutide. Specific recommendations on albiglutide use have been issued by the American Association of Clinical Endocrinologists (AACE) and the American Diabetes Association (ADA). Studies show that the potential for hypoglycemic episodes with albiglutide use is low. In clinical trials, the most frequently reported adverse events were nausea and diarrhea. The use of albiglutide is contraindicated in patients with a history of pancreatitis and patients with a personal or family history of thyroid cancer.

CONCLUSION

Albiglutide has been shown to be effective for the management of type 2 diabetes in adults and is recommended (by ADA) as second-line therapy when used in combination with metformin and (by AACE) as first-line monotherapy in patients with an HbA1c concentration of ≤7.5% at treatment initiation. In clinical trials, albiglutide was generally well tolerated by patients, with adverse effects comparable to those seen with other GLP-1 agonists.

摘要

目的

对胰高血糖素样肽-1(GLP-1)受体激动剂阿必鲁泰的药理学、药代动力学、疗效、安全性、剂量与用法及其在治疗中的地位进行综述。

总结

阿必鲁泰(Tanzeum,葛兰素史克公司)是一种注射用GLP-1激动剂,于2014年获批,作为饮食调整和运动的辅助手段,用于改善2型糖尿病成人患者的血糖控制。阿必鲁泰可增强葡萄糖依赖性胰岛素分泌并延缓胃排空;其消除半衰期约为5天,允许每周给药一次。临床试验表明,在接受阿必鲁泰辅助治疗16周后,糖化血红蛋白(HbA1c)值平均绝对降低0.78 - 1.55%。美国临床内分泌医师协会(AACE)和美国糖尿病协会(ADA)已发布了关于使用阿必鲁泰的具体建议。研究表明,使用阿必鲁泰发生低血糖事件的可能性较低。在临床试验中,最常报告的不良事件是恶心和腹泻。有胰腺炎病史的患者以及有甲状腺癌个人或家族病史的患者禁用阿必鲁泰。

结论

已证明阿必鲁泰对成人2型糖尿病的管理有效,(美国糖尿病协会)推荐其与二甲双胍联合使用时作为二线治疗药物,(美国临床内分泌医师协会)推荐在治疗起始时HbA1c浓度≤7.5%的患者中作为一线单药治疗药物。在临床试验中,患者对阿必鲁泰总体耐受性良好,其不良反应与其他GLP-1激动剂相当。

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