Boden Institute of Obesity, Nutrition and Exercise, University of Sydney, Sydney, NSW, Australia.
Oxford Centre for Diabetes, Endocrinology and Metabolism, and Harris Manchester College, University of Oxford, Oxford, UK.
Diabetes Res Clin Pract. 2018 Sep;143:1-14. doi: 10.1016/j.diabres.2018.05.028. Epub 2018 May 24.
The sulfonylureas are effective oral glucose-lowering agents with a long history of clinical use. While all have the same general mechanism of action, their pharmacokinetic properties are influenced by factors such as dosage, rate of absorption, duration of action, route of elimination, tissue specificity, and binding affinity for pancreatic β-cell receptor. The result is a class of agents with similar HbA1c-lowering efficacy, but well-documented differences in terms of effects on hypoglycemia, and cardiovascular and renal safety. This review examines the differences between currently available sulfonylureas with a focus on how gliclazide modified release (MR) differs from other members of this class and from newer oral antihyperglycemic agents in the form of dipeptidyl peptidase-4 (DPP4) and sodium- glucose cotransporter 2 (SGLT2) inhibitors. The first part focuses on major outcome trials that have been conducted with the sulfonylureas and new oral agents. Consideration is then given to factors important for day-to-day prescribing including efficacy and durability, weight changes, hypoglycemia, renal effects and cost. Based on current evidence, third-generation sulfonylureas such as gliclazide MR possess many of the properties desired of a type 2 diabetes drug including high glucose-lowering efficacy, once-daily oral administration, few side effects other than mild hypoglycemia, and cardiovascular safety.
磺酰脲类药物是一种有效的口服降血糖药物，具有悠久的临床应用历史。虽然它们具有相同的一般作用机制，但它们的药代动力学特性受到剂量、吸收速度、作用持续时间、消除途径、组织特异性和与胰腺β细胞受体的结合亲和力等因素的影响。结果是一类具有相似的糖化血红蛋白降低效果的药物，但在低血糖、心血管和肾脏安全性方面存在明显差异。本综述考察了目前可用的磺酰脲类药物之间的差异，重点介绍了格列齐特缓释（MR）与该类药物其他成员以及新型口服抗高血糖药物（二肽基肽酶-4 [DPP4] 和钠-葡萄糖共转运蛋白 2 [SGLT2] 抑制剂）之间的差异。第一部分重点介绍了已进行的磺酰脲类药物和新型口服药物的主要结局试验。然后考虑了包括疗效和持久性、体重变化、低血糖、肾脏影响和成本在内的日常处方的重要因素。基于目前的证据，第三代磺酰脲类药物，如格列齐特 MR，具有许多理想的 2 型糖尿病药物的特性，包括高效降低血糖、每日口服一次、除轻度低血糖外几乎没有其他副作用，以及心血管安全性。
