近日，美国FDA已批准米那普伦盐酸盐(milnacipran Hcl，Savella)用于治疗纤维肌痛。纤维肌痛是一种以全身性疼痛与疲劳为主的疾病。根据美国风湿病学会估计大约有6百万美国人患有纤维肌痛。
虽然对于本品改善纤维肌痛症状的确切机制尚不明确，但一些研究者认为：某些脑部神经递质的异常可能是纤维肌痛的关键所在。本品可能是通过对5-羟色胺与去甲肾上腺素(NE)再摄取的双重抑制(在体外对NE再摄取抑制的选择性更强)来改善纤维肌痛症状。
在美国进行的2项关键性III期临床研究中，共纳入2084例患者，其中1460例患者接受本品治疗，624例患者则使用安慰剂。结果显示：与安慰剂相比，本品(剂量为100mg/天、200mg/天)能同时显著改善疼痛(视觉模拟评分)、患者整体评价(患者对变化的整体印象评分)与生理功能 (Short Form-36 总体生理健康)。预期，本品将于2009年3月上市。
本品的安全性与耐受性良好。最常见的不良反应为恶心。其他常见不良反应包括便秘、潮热、多汗、呕吐、心悸、心率上升、口干与高血压。本品所报道的大多数不良反应为轻微至中等程度。
批准日期：2009年2月2日 公司：actais pharma
Savella(米那普仑[milnacipran Hcl])片 供口服使用
作用机制
米那普仑的中枢疼痛抑制作用确切作用机制和在人中改善纤维肌痛症状的能力尚未知。临床前研究曾显示米那普仑是一种神经元去甲肾上腺素和5-羟色胺再摄取强抑制剂；在体外米那普仑抑制去甲肾上腺素摄取比5-羟色胺强度约更高3-倍，对多巴胺或其它神经递质的摄取无直接影响。米那普仑在体外对5-羟色胺能(5-HT1-7)，α-和β-肾上腺能，毒蕈硷(M1-5)，组胺(H1-4)，多巴胺(D1-5)，鸦片，苯二氮卓，和γ-氨基丁酸(GABA)受体无明显亲和力。在这些受体处的药理学活性被假设是伴随各种抗胆碱能，镇静，和心血管效应与其它精神病治疗药物所见。米那普仑对Ca++，K+，Na+和Cl– 通道无明显亲和力而且不抑制人单胺氧化酶(MAO-A和MAO-B)或胆碱酯酶活性。
适应证和用途
Savella是一种选择性5-羟色胺和去甲肾上腺素再摄取抑制剂(SNRI)适用于纤维肌痛的处理(1)未批准在儿童患者中使用Savella
剂量和给药方法
（1）每天分2次给予Savella
（2）根据疗效和耐受性，可按照以下方案调整给药：
第1天：12.5 mg1次
第2-3天：25 mg/day(12.5 mg每天2次)
第4-7天：50 mg/day (25 mg每天2次)
第7天后：100 mg/day (50 mg每天2次)
（3）推荐剂量是100 mg/day
（4）根据个体患者反应可增加至200 mg/day
（5）应调整剂量有严重肾损伤患者中
剂型和规格
片：12.5mg，25mg，50mg，100mg
禁忌证
（1）同时或时间密切接近使用单胺氧化酶抑制剂
（2）未控制窄角青光眼患者中使用
警告和注意事项
（1）自杀行为：监查抑郁症状和自杀风险的恶化
（2）5-羟色胺综合征或神经阻滞剂恶性综合征(NMS)-样反应：用再摄取抑制剂[SNRIs]和SSRIs曾报道5-羟色胺综合征或NMS-样反应。停止Savella和开始支持治疗
（3）血压和心率增加：用Savella曾报道情况。开始用Savella治疗前和治疗始终定期监查血压和心率
（4）癫痫发作：用Savella治疗曾报道情况，有癫痫疾患史患者中小心开Savella处方
（5）肝毒性：用Savella治疗患者比用安慰剂经受更多ALT和AST的轻度升高。罕见，用Savella治疗患者中曾报道暴发型肝炎。大量饮酒或慢性肝病患者避免同时使用Savella
（6）停药：患者停止使用Savella治疗时曾报道撤药症状。建议逐渐减低剂量
（7）异常出血：Savella可能增加出血事件的风险。患者谨慎同时使用Savella和伴随出血风险的NSAIDs，阿司匹林，或影响凝血的其它药物
（8）阻塞性泌尿疾病史男性患者可能经受更高发生率的泌尿生殖器的不良事件
不良反应
最频发生不良反应(≥ 5%和大于安慰剂)是恶心，头痛，便秘，眩晕，失眠，潮热，多汗，呕吐，心悸，心率增加，口干，和高血压
药物相互作用
（1）Savella是不可能涉及临床上有意义的药代动力学药物相互作用
（2）Savella与其它药物可能发生药效学相互作用
在特殊人群中的使用
（1）妊娠和哺乳母亲：只有如潜在获益合理大于对胚胎或儿童的潜在风险才使用。
（2）为纳入Savella妊娠注册电话1-877-6433010(免费)或从注册网站下载数据表：www.savellaPregnancyregistry.com .
Savella
Brand Names:Savella
Generic name:milnacipran
Pregnancy Category:C
What is Savella?
Savella (milnacipran HCI) is a prescription drug that is in a class of medications known as selective serotonin and norepinephrine reuptake inhibitors, or SNRIs. Savella is used to increase the amount and effectiveness of neurotransmitters such as serotonin and norepinephrine, which are used to communicate between brain cells. Savella (milnacipran) prescribed by your doctor is a laboratory-synthesized form of these neurotransmitters.
Savella comes in a tablet form that is taken orally, usually twice per day. Milnacipran medications may be taken with or without food; taking the drug with food may reduce the occurrence of common Savella side effects, such as nausea. For best results, always take Savella exactly as directed by your doctor and at the same time each day.
Savella Uses
The Food and Drug Administration approved Savella (milnacipran) for the treatment of fibromyalgia in 2009. Savella works best for fibromyalgia patients age 18 and older; it is not usually recommended for children or young teenagers. In clinical trials completed before the drug received FDA approval, a large number of patients using Savella reported a 30 percent or greater reduction in the severity or occurrence of fibromyalgia-related conditions such as chronic pain, fatigue, muscle stiffness and tiredness, and difficulty falling or staying asleep.
Although the Food and Drug Administration has not approved Savella for the treatment of major depressive disorders, milnacipran has been used to treat depression in French patients since 1996. In fact, milnacipran is used as an antidepressant in more than 45 countries around the world, including Finland, Japan, France, Austria, Bulgaria, Mexico, Portugal and Russia. Only time, and further clinical trials, will tell whether the FDA will approve milnacipran as a treatment for depression and other mood disorders in American patients.
What to Expect
Patients are started on a low dose of Savella, and based on their reactions to the medication, the dose can be increased during the first week of treatment.
Some patients have reported pain reduction in as little as the first week of stable doses; however, it can take several weeks to feel the beneficial effects of Savella. Patients should continue taking the prescribed dose even if they do not experience immediate improvement.
Risk Information
Savella also carries the same risks as antidepressant medications. Savella is not approved for individuals under the age of 18 because of the increased risk of suicidal thoughts or actions in children, teenagers, and young adults.
Patients on Savella should alert their doctor if they experience unusual changes in behavior, suicidal thoughts, anxiety, agitation, panic attacks, difficulty sleeping, irritability, hostility, aggressiveness, impulsivity, restlessness, or extreme hyperactivity.
Before Taking Savella
You should not take Savella if you are currently taking or have recently taken a monoamine oxidase inhibitor (MAOI) or have uncontrolled narrow-angle glaucoma.
Before taking Savella, you should tell your healthcare provider if you have hypertension, heart rhythm problems, any heart diseases, liver problems, substantial alcohol use, kidney problems, manic episodes, seizure disorders, bleeding disorders, or glaucoma. Also tell your doctor if you are taking medication for a psychiatric or neurological condition, NSAID pain relievers, aspirin, warfarin, blood thinners, or diuretics.
Savella is a viable option for any individuals suffering from Fibromyalgia. If you feel that Savella could help relieve your chronic pain, talk to your doctor to see if Savella is right for you.