Department of Medicine, Vanderbilt University, Nashville, TN, USA.
J Pain Res. 2010 Jun 22;3:81-8. doi: 10.2147/jpr.s7884.
This last article in a three-part series on approved medications for managing fibromyalgia syndrome (FMS) reviews pregabalin (Lyrica(®)). Pregabalin was the first drug approved for FMS management and, as an anticonvulsant, differs from the other approved agents that are antidepressants. Pregabalin inhibits presynaptic excitatory neurotransmitter release by blocking α(2)δ calcium channels. Five randomized, placebo-controlled trials have demonstrated pregabalin reduces pain and improves sleep and health-related quality of life in FMS patients. While indicated dosing is 300-450 mg divided twice daily, initial dosing of 25-50 mg at night is recommended owing to side effects including somnolence, dizziness, and cognitive dysfunction. Since side effects such as weight gain and peripheral edema are dose-related, uptitration in weekly increments based on tolerability and therapeutic response is recommended. Due to its lack of protein binding and negligible hepatic metabolism, pregabalin can be safely combined with other medications and used in patients with renal failure when the dose is appropriate. Pregabalin may worsen sedation when combined with central nervous system depressants. Pregabalin should be discontinued gradually. Pregabalin-treated patients should be monitored for the emergence or worsening of depression, suicidal thoughts or behavior. Pregabalin in combination with the other approved medications may be synergistic in treating FMS.
这是关于批准用于治疗纤维肌痛综合征 (FMS) 的药物的三篇系列文章中的最后一篇,介绍普瑞巴林(Lyrica(®))。普瑞巴林是第一种获得批准用于 FMS 管理的药物,作为一种抗惊厥药,它与其他获得批准的抗抑郁药不同。普瑞巴林通过阻断 α(2)δ 钙通道抑制突触前兴奋性神经递质的释放。五项随机、安慰剂对照试验表明,普瑞巴林可减轻 FMS 患者的疼痛,改善睡眠和健康相关生活质量。虽然推荐剂量为每日两次 300-450mg,但由于副作用包括嗜睡、头晕和认知功能障碍,建议初始剂量为每晚 25-50mg。由于体重增加和外周水肿等副作用与剂量有关,建议根据耐受性和治疗反应每周递增剂量。由于普瑞巴林与蛋白结合率低,肝脏代谢可忽略不计,因此可以安全地与其他药物联合使用,并且在适当剂量下可用于肾衰竭患者。普瑞巴林与中枢神经系统抑制剂合用时可能会加重镇静作用。普瑞巴林应逐渐停药。接受普瑞巴林治疗的患者应监测抑郁、自杀意念或行为的出现或恶化。普瑞巴林与其他获得批准的药物联合使用可能在治疗 FMS 方面具有协同作用。