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继日本中央社会保险医疗委员会批准了Victoza®（利拉鲁肽）的定价之后，诺和诺德制药公司计划将尽快在当地市场推出这种产品。诺和诺德表示，Victoza®是首个在日本获准上市的GLP-1类药物，既可以单独用药，也可以作为辅助药物与磺脲类降糖药(SU)联用。
综述：各种GLP-1受体激动剂及DPP-4抑制剂的结构、作用机制及药理学
GLP-1受体激动剂及DPP-4抑制剂对于空腹及餐后血糖控制都有益处，使得达标更为简单；它们还能改善B细胞功能，甚至能降低血压，与其他传统药物相结合，能延缓2型糖尿病进程。
Objective: To review the pharmacology (absorption, metabolism, distribution,elimination, and contraindications) of incretin-based agents currently available and in regulatory review for the treatment of patients with type 2 diabetes.
Data sources: Medline search of all relevant clinical and review articles.
Study selection: English-language articles pertinent to the pharmacology, pharmacodynamics,pharmacokinetics, efficacy, and safety of glucagon-like peptide-1 (GLP-1) agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors were reviewed for relevance.
Data extraction: Data pertinent to the pharmacology, pharmacodynamics, pharmacokinetics,efficacy, and safety of GLP-1 agonists and DPP-4 inhibitors were extracted and used.
Data synthesis: Incretin hormones are secreted from the gastrointestinal tract following meal ingestion, the two most important of which are glucose-dependent insulinotropic polypeptide (GIP) and GLP-1. Patients with type 2 diabetes have an impaired response to GIP, while intravenous GLP-1 has been shown to increase insulin secretion in response to elevated glucose levels. Incretin-based agents include GLP-1 receptor agonists, which mimic endogenous GLP-1, and DPP-4 inhibitors (e.g., sitagliptin,vildagliptin, saxagliptin, alogliptin), which inhibit the breakdown of endogenous incretin hormones. GLP-1 receptor agonists stimulate insulin secretion in a glucose-dependent manner and suppress glucagon secretion with a low risk of hypoglycemia.The GLP-1 receptor agonists are further differentiated as either human analogues (e.g., liraglutide) or synthetic exendin-based mimetics (e.g., exenatide). These agents delay gastric emptying and may beneficially affect satiety and are thus associated with weight reduction.
Conclusion: GLP-1 receptor agonists and DPP-4 inhibitors facilitate therapy intensification and achievement of established glycemic goals. They enhance postprandial and fasting glycemic control, and use may improve beta-cell function and possibly preserve beta-cell mass. GLP-1 receptor agonists may also have favorable effects on blood pressure. They may be introduced as adjuncts to ongoing therapy with conventional agents with a potential benefit of slowing the progression of type 2 diabetes.
Keywords: Type 2 diabetes, incretins, exenatide, liraglutide, taspoglutide, sitagliptin,vildagliptin, saxagliptin, albiglutide, alogliptin.
编辑: helen
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