Sparano N, Seaton T L
Department of Pharmacy Practice, Wilkes University, Wilkes-Barre, Pennsylvania 18766, USA.
Pharmacotherapy. 1998 May-Jun;18(3):539-48.
Troglitazone, a new antihyperglycemic agent, is approved for use alone, with oral sulfonylureas, or with insulin in the treatment of type II diabetes mellitus. Rather than stimulating insulin secretion, it enhances insulin sensitivity. Potential advantages of troglitazone over oral sulfonylureas include decreased endogenous insulin concentrations, decreased exogenous insulin requirements, reduced hypoglycemic risk, and convenient once/day administration. The effect on morbidity and mortality from lowering endogenous and exogenous insulin concentrations remains to be determined. Troglitazone also has potential disadvantages. It induces cytochrome P450 isoenzyme 3A4, although few drug interactions have been identified to date. Serum transaminases must be monitored routinely because of rarely reported cases of idiosyncratic hepatocellular injury. In addition, the cost of troglitazone is much higher than that of other oral antihyperglycemic agents or insulin. Given the available information, troglitazone has limited benefit over oral sulfonylureas or metformin as monotherapy or in combination with oral sulfonylureas. Until additional combination and comparative studies have been done, the agent should be reserved for patients with poor glycemic control receiving high daily doses of insulin.
曲格列酮是一种新型抗高血糖药物,已被批准可单独使用、与口服磺脲类药物联用或与胰岛素联合用于治疗II型糖尿病。它并非刺激胰岛素分泌,而是增强胰岛素敏感性。曲格列酮相对于口服磺脲类药物的潜在优势包括降低内源性胰岛素浓度、减少外源性胰岛素需求、降低低血糖风险以及每日一次给药方便。降低内源性和外源性胰岛素浓度对发病率和死亡率的影响仍有待确定。曲格列酮也有潜在的劣势。它可诱导细胞色素P450同工酶3A4,尽管迄今为止仅发现少数药物相互作用。由于有罕见的特异质性肝细胞损伤病例报告,必须常规监测血清转氨酶。此外,曲格列酮的费用远高于其他口服抗高血糖药物或胰岛素。鉴于现有信息,曲格列酮作为单一疗法或与口服磺脲类药物联合使用时,相对于口服磺脲类药物或二甲双胍的益处有限。在进行更多的联合和对比研究之前,该药物应仅保留用于血糖控制不佳且每日接受高剂量胰岛素治疗的患者。