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二甲双胍:一种新型口服双胍类药物。

Metformin: a new oral biguanide.

作者信息

Campbell R K, White J R, Saulie B A

机构信息

College of Pharmacy, Washington State University, Pullman, USA.

出版信息

Clin Ther. 1996 May-Jun;18(3):360-71; discussion 359. doi: 10.1016/s0149-2918(96)80017-8.

Abstract

The biguanide metformin is an oral anti-hyperglycemic agent used in the treatment of patients with non-insulin-dependent diabetes mellitus (NIDDM). Metformin is an important addition to the drug therapy options available for those patients because it reduces blood glucose levels predominantly by decreasing hepatic glucose production and release and also by increasing peripheral tissue sensitivity to insulin; it does not stimulate insulin secretion from the beta cells in the pancreas. Metformin also has a potentially beneficial effect by reducing serum lipid levels. Its glycemic control is similar to that of the sulfonylureas and is effective as monotherapy or in combination with sulfonylureas or insulin. Unlike sulfonylureas and insulin, it does not cause a gain in body weight, and when used as monotherapy, it does not cause hypoglycemia. The most common side effects associated with metformin are mild, transient, gastrointestinal symptoms, which are usually self-limiting. These side effects can be minimized by initiating metformin therapy at a low dose and gradually titrating upward, and by taking metformin with meals. Lactic acidosis caused by metformin is rare, and the risk of this complication may be diminished by the observance of prescribing precautions and contraindications that avoid accumulation of metformin or lactate in the body. In patients who are not getting the desired effect with sulfonylureas, it is useful to combine sulfonylureas with metformin therapy. Metformin should be considered a first-line agent, particularly in obese and/or hyperlipidemic NIDDM patients.

摘要

双胍类药物二甲双胍是一种口服抗高血糖药物,用于治疗非胰岛素依赖型糖尿病(NIDDM)患者。二甲双胍是这些患者可用药物治疗选择中的重要补充,因为它主要通过减少肝脏葡萄糖生成和释放以及增加外周组织对胰岛素的敏感性来降低血糖水平;它不会刺激胰腺β细胞分泌胰岛素。二甲双胍还通过降低血脂水平具有潜在的有益作用。其血糖控制与磺脲类药物相似,作为单一疗法或与磺脲类药物或胰岛素联合使用均有效。与磺脲类药物和胰岛素不同,它不会导致体重增加,并且作为单一疗法使用时不会引起低血糖。与二甲双胍相关的最常见副作用是轻度、短暂的胃肠道症状,通常为自限性。通过低剂量开始二甲双胍治疗并逐渐向上滴定剂量,以及与餐同服二甲双胍,这些副作用可以最小化。二甲双胍引起的乳酸性酸中毒很少见,遵守避免二甲双胍或乳酸在体内蓄积的处方预防措施和禁忌证,可能会降低这种并发症的风险。在使用磺脲类药物未获得理想效果的患者中,将磺脲类药物与二甲双胍联合治疗是有用的。二甲双胍应被视为一线药物,特别是在肥胖和/或高脂血症的NIDDM患者中。

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