Division of Reproductive Endocrinology and Infertility, Department of Obstetrics and Gynecology, University of California Davis, 4869 Y Street, Suite 2550 ACC, Sacramento, CA 95817, USA.
Steroids. 2012 Mar 10;77(4):306-11. doi: 10.1016/j.steroids.2011.11.014. Epub 2011 Dec 13.
Polycystic ovary syndrome (PCOS) is associated with metabolic derangements including insulin resistance, dyslipidemia, systemic inflammation and endothelial dysfunction. There is a growing need to develop pharmacologic interventions to improve metabolic function in women with PCOS. Medications that have been tested in patients with PCOS include metformin, thiazolidinediones, acarbose, naltrexone, orlistat, vitamin D and statins. Metformin decreases hepatic gluconeogenesis and free fatty acid oxidation while increasing peripheral glucose uptake. Early studies in PCOS suggested that metformin indirectly reduces insulin level, dyslipidemia and systemic inflammation; however, recent placebo-controlled trials failed to demonstrate significant metabolic benefit. Thiazolidinediones act primarily by increasing peripheral glucose uptake. Most studies in PCOS have demonstrated that thiazolidinediones reduce insulin resistance; however, effects on dyslipidemia were disappointing. Use of thiazolidinediones is associated with weight gain and major complications. Acarbose reduces digestion of polysaccharides. Studies in PCOS yielded inconsistent effects of acarbose on insulin sensitivity and no significant improvement of dyslipidemia. Naltrexone reduces appetite and modulates insulin release; its use in PCOS may reduce hyperinsulinemia. Orlistat decreases absorption of dietary fats; studies in PCOS suggest beneficial effects on insulin sensitivity. Vitamin D may improve insulin sensitivity but mixed results on lipid profile in PCOS have been reported. Statins are competitive inhibitors of the key enzyme regulating the mevalonate pathway; their effects are related to reduced cholesterol production as well as anti-inflammatory and anti-oxidant properties. In women with PCOS, statins reduce hyperandrogenism, improve lipid profile and reduce systemic inflammation while the effects on insulin sensitivity are variable. Use of statins is contraindicated in pregnancy.
多囊卵巢综合征（PCOS）与代谢紊乱有关，包括胰岛素抵抗、血脂异常、全身炎症和内皮功能障碍。因此，迫切需要开发药物干预措施来改善 PCOS 患者的代谢功能。已经在 PCOS 患者中进行了测试的药物包括二甲双胍、噻唑烷二酮类、阿卡波糖、纳曲酮、奥利司他、维生素 D 和他汀类药物。二甲双胍可减少肝糖异生和游离脂肪酸氧化，同时增加外周葡萄糖摄取。早期的 PCOS 研究表明，二甲双胍间接降低胰岛素水平、血脂异常和全身炎症；然而，最近的安慰剂对照试验未能证明其具有显著的代谢益处。噻唑烷二酮类主要通过增加外周葡萄糖摄取起作用。大多数 PCOS 研究表明，噻唑烷二酮类可降低胰岛素抵抗；然而，对血脂异常的影响却令人失望。噻唑烷二酮类的使用与体重增加和主要并发症有关。阿卡波糖可减少多糖的消化。PCOS 的研究结果显示阿卡波糖对胰岛素敏感性的影响不一致，且对血脂异常没有明显改善。纳曲酮可降低食欲并调节胰岛素释放；它在 PCOS 中的应用可能会降低高胰岛素血症。奥利司他可减少膳食脂肪的吸收；PCOS 的研究表明其对胰岛素敏感性有益。维生素 D 可能改善胰岛素敏感性，但 PCOS 中的血脂谱结果喜忧参半。他汀类药物是调节甲羟戊酸途径的关键酶的竞争性抑制剂；它们的作用与降低胆固醇生成以及抗炎和抗氧化特性有关。在 PCOS 女性中，他汀类药物可降低高雄激素血症、改善血脂谱并降低全身炎症，而对胰岛素敏感性的影响则各不相同。他汀类药物在怀孕期间禁用。
