Forest Research Institute, Harborside Financial Center, Plaza V, Jersey City, NJ 07311, USA.
Ther Adv Musculoskelet Dis. 2010 Aug;2(4):201-20. doi: 10.1177/1759720X10372551.
Milnacipran, a serotonin and norepinephrfrine reuptake inhibitor with preferential inhibition of norepinephrine reuptake over serotonin, is approved in the United States for the management of fibromyalgia. Owing to its effects on norepinephrine and serotonin, as well as its lack of activity at other receptor systems, it was hypothesized that milnacipran would provide improvements in pain and other fibromyalgia symptoms without some of the unpleasant side effects associated with other medications historically used for treating fibromyalgia. The clinical safety and efficacy of milnacipran 100 and 200 mg/day in individuals with fibromyalgia has been investigated in four large, randomized, double-blind, placebo-controlled studies and three long-term extension studies. The clinical studies used composite responder analyses to identify the proportion of individual patients reporting simultaneous and clinically significant improvements in pain, global status, and physical function, in addition to assessing improvement in various symptom domains such as fatigue and dyscognition. In the clinical studies, patients receiving milnacipran reported significant improvements in pain and other symptoms for up to 15 months of treatment. Most adverse events were mild to moderate in severity and were related to the intrinsic pharmacologic properties of the drug. Long-term exposure to milnacipran did not result in any new safety concerns. As with other serotonin and norepinephrine reuptake inhibitors, increases in heart rate and blood pressure have been observed in some patients with milnacipran treatment.
米那普仑是一种 5-羟色胺和去甲肾上腺素再摄取抑制剂,对去甲肾上腺素再摄取的抑制作用强于 5-羟色胺,已获美国批准用于纤维肌痛的治疗。由于其对去甲肾上腺素和 5-羟色胺的作用,以及对其他受体系统无活性,人们推测米那普仑将改善疼痛和其他纤维肌痛症状,而不会产生与历史上用于治疗纤维肌痛的其他药物相关的一些不良副作用。米那普仑 100mg 和 200mg/天在纤维肌痛患者中的临床安全性和疗效已在四项大型、随机、双盲、安慰剂对照研究和三项长期扩展研究中进行了研究。这些临床研究采用综合应答分析来确定报告疼痛、整体状况和身体功能同时显著改善以及疲劳和认知障碍等各种症状域改善的个体患者的比例。在临床研究中,接受米那普仑治疗的患者报告疼痛和其他症状在长达 15 个月的治疗中得到显著改善。大多数不良事件的严重程度为轻度至中度,与药物的固有药理特性有关。米那普仑的长期暴露并未导致任何新的安全问题。与其他 5-羟色胺和去甲肾上腺素再摄取抑制剂一样,一些接受米那普仑治疗的患者的心率和血压有所升高。