Department of Medicine, Division of Endocrinology, Diabetes, and Metabolic Diseases, Jefferson Medical College of Thomas Jefferson University, Philadelphia, PA 19107, USA.
Postgrad Med. 2011 Jan;123(1):15-23. doi: 10.3810/pgm.2011.01.2241.
Metformin is a first-line pharmacological treatment for patients with type 2 diabetes mellitus because of its favorable overall profile, including its glucose-lowering ability, weight-neutral effects, and low risk of hypoglycemia; however, gastrointestinal (GI) intolerance may limit use in some patients. Extended-release metformin improves GI tolerability, allows once-daily dosing, and is currently available in multiple branded and generic formulations; however, it is more expensive than immediate-release metformin. Maximum plasma metformin concentrations are reached more slowly with the extended-release formulation compared with conventional immediate-release metformin, although both provide similar exposure at a given total daily dose. Extended-release metformin is as effective as immediate-release metformin in patients newly started on metformin and those switched from the immediate-release formulation, with similar weight-neutral effects. Tolerability is generally comparable, although patients switched from the immediate-release formulation--even those switched due to GI intolerance--are often better able to tolerate the extended-release formulation. Based on studies of extended-release formulations in other disease states, metformin extended-release formulation has the potential to improve patient adherence with a simpler dosing regimen and increased tolerability. Increased adherence may result in greater glycemic control, and in turn, improve outcomes and lower health care usage and costs. Extended-release metformin provides an appropriate option for patients with type 2 diabetes mellitus who require several medications to achieve glycemic control or manage comorbid conditions, and for those who have GI intolerance with the immediate-release formulation.
二甲双胍是治疗 2 型糖尿病患者的一线药物治疗选择，因为它具有全面的优势，包括降低血糖的能力、中性体重影响和低血糖风险低；然而，胃肠道（GI）不耐受可能会限制一些患者的使用。 缓释二甲双胍提高了 GI 耐受性，允许每日一次给药，并且目前有多种品牌和通用配方；然而，它比普通即时释放二甲双胍更昂贵。 与传统的即时释放二甲双胍相比，缓释制剂达到最大血浆二甲双胍浓度的速度较慢，尽管在给定的每日总剂量下，两者提供的暴露量相似。 对于新开始使用二甲双胍的患者和从即时释放制剂转换的患者，缓释二甲双胍与即时释放二甲双胍一样有效，并且具有相似的中性体重影响。 耐受性通常相当，尽管从即时释放制剂转换的患者 - 即使是由于 GI 不耐受而转换的患者 - 通常能够更好地耐受缓释制剂。 根据其他疾病状态下的缓释制剂研究，二甲双胍缓释制剂有可能通过更简单的给药方案和提高的耐受性来提高患者的依从性。 更高的依从性可能导致更好的血糖控制，从而改善结果并降低医疗保健使用和成本。 对于需要几种药物来控制血糖或治疗合并症的 2 型糖尿病患者，以及对即时释放制剂有 GI 不耐受的患者，缓释二甲双胍提供了一个合适的选择。
