全球首款“女性版伟哥”氟班色林片flibanserin(商品名 ADDYI) 被FDA批准用于妇女性欲低的苦恼提供一种治疗选择 注：本品在美国咨询委员会有争议，在美国只能在受限制程序下才允许使用。本品不适合我国国情、社会和文化。使用说明书是为了解。 FDA批准对于性欲障碍第一个治疗。FDA的药品评价和研究中心(CDER)主任Janet Woodcock，M.D.说：“今天的批准为被她们低性欲苦恼妇女提供一种被批准的治疗选择，” “FDA努力保护和促进妇女健康，而我们承诺支持对女性性功能障碍安全和有效治疗的发展。”“因为与酒精潜在地严重相互作用，将只能通过认证卫生保健专业人员和认证的药房得到用Addyi治疗，” “考虑使用Addyi治疗前患者和开处方者应充分了解伴随使用的风险。” 批准日期：2015年5月18日；公司：Sprout Pharmaceuticals，Inc. ADDYI(氟班色林[flibanserin]) 片，为口服使用 美国初次批准：2015 一般描述 ADDYI(氟班色林[flibanserin])是一片为口服给药。氟班色林的化学名是2H-Benzimidazol-2-one，1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]。其经验式是C20H21F3N4O和分子量是390.41。 其结构式是： 氟班色林是一种白色至蛋白色粉，不溶于水，微溶于甲醇，乙醇，乙腈和甲苯，溶于丙酮，自由溶于氯仿，和非常溶于二氯甲烷。 每片ADDYI含100mg的氟班色林。无活性成分由一水乳糖，微晶纤维素，羟丙甲纤维素，羧甲基纤维素钠，硬脂酸镁，滑石，聚乙二醇，和着色剂，二氧化钛和氧化铁组成。 作用机制 不知道ADDYI治疗活力减低性性欲障碍绝经前妇女治疗中的作用机制。 适应症和用途 ADDYI是适用为有获得性，普遍性活力减低性性欲障碍(HSDD)当特征为低性欲致明显苦恼或人际交往困难和不是由于以下的绝经前妇女治疗： ⑴ 一种共存医疗或精神条件， ⑵ 相互关系内问题，或 ⑶ 一种药物或其他药物物质的影响。 使用限制： ADDYI是不适用为绝经后妇女或在男性中HSDD的治疗. 剂量和给药方法 ⑴ 推荐剂量是100 mg每天1次在睡前时服用。 ⑵ ADDYI是在睡前给药因为清醒小时期间给药增加低血压，昏厥，意外损伤，和中枢神经系统(CNS)抑郁的风险。 ⑶ 如治疗8周后无改善终止治疗。 剂型和规格 片：100mg 禁忌证 ⑴ 酒精。 ⑵ 中度或强细胞色素P450 3A4(CYP3A4)抑制剂。 ⑶ 肝受损。 警告和注意事项 ⑴ 单独用ADDYI低血压和昏厥：有预晕厥[pre-syncope ]患者应立即仰卧和及时寻求医疗帮助如症状没有解决。 ⑵ 中枢神经系统(CNS)抑郁(如，嗜睡，镇静)：单独使用ADDYI可能发生。被其它抑制剂和氟班色林浓度增加情况中加重。患者应避免需求全面警觉活动(如，操作机械或驾驶)直至每次给药后至少6小时和直至她们知道ADDYI如何影响她们。 不良反应 最常见不良反应(发生率 ≥2%)是眩晕，嗜睡，恶心，疲乏，失眠，和口干. 药物相互作用 ⑴ 口服避孕药和其他弱CYP3A4抑制剂：增加氟班色林暴露和不良反应发生率。 ⑵ 强CYP2C19抑制剂：增加氟班色林暴露可能增加低血压，昏厥，和CNS抑郁风险。 ⑶ CYP3A4诱导剂：建议不使用ADDYI；氟班色林浓度实质上减低。 ⑷ 地高辛：增加地高辛[digoxin]浓度，可能导致地高辛毒性。增加地高辛浓度监视。 特殊人群中使用 ⑴ 哺乳母亲：建议不用ADDYI。 ⑵ CYP2C19慢代谢型者：增加氟班色林暴露可能增加低血压，昏厥，和CNS抑郁风险。 包装规格/贮存和处置 可得到ADDYI是100 mg椭圆，粉色，膜包衣片在一侧凹陷有“f100”和另一侧空白。可得到30片瓶.(NDC 58604-214-30) 贮存 贮存在25°C(77°F)；外出允许至15°-30°C(59°-86°F)[见USP控制室温]。 http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3819daf3-e935-2c53-c527-e1d57922f394 The first and only FDA-approved treatment for acquired, generalized Hypoactive Sexual Desire Disorder (HSDD) in premenopausal women The U.S. Food and Drug Administration (FDA) has approved Addyi (flibanserin, Sprout Pharmaceuticals) to boost sexual desire in premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), according to an agency press release. Addyi is now the first FDA-approved treatment for HSDD, which is characterized by low sexual desire that causes significant distress or interpersonal difficulty and is not related to a co-existing medical or psychiatric condition, problems within a relationship or the effects of a medication or other drug substance. The disorder is acquired when a patient who previously had no problems begins to develop issues with sexual desire. HSDD is considered generalized when it occurs regardless of the type of sexual activity, the situation or the sexual partner. Addyi is a serotonin 1A receptor agonist and a serotonin 2A receptor antagonist, although it remains unclear through which mechanism the drug improves sexual desire and related distress. The drug is a once-daily treatment that is to be taken at bedtime to reduce the risk for adverse events due to possible hypotension, syncope and central nervous system depression like sleepiness and sedation. If no improvement in sexual desire or related distress is experienced after 8 weeks, women should discontinue treatment, according to the release. Researchers assessed the efficacy of the 100-mg bedtime dose of Addyi in three 24-week randomized, double-blind, placebo-controlled trials that involved about 2,400 premenopausal women (mean age, 36 years) with acquired, generalized HSDD. Duration of the disorder was approximately 5 years. In the trials, women tracked the number of satisfying sexual events (scored on a range of 1.2 to 6.0), reported sexual desire during the preceding 4 weeks and distress due to low sexual desire (range of 0 to 4). Treatment with Addyi appeared to increase the number of satisfying sexual events by 0.5 to one additional event per month, increased sexual desire score by 0.3 to 0.4 and decreased related distress by 0.3 to 0.4, as compared with placebo, according to information in the release. Results from additional analyses in women who felt much or very much improved overall with treatment showed that 10% more patients who took Addyi vs. placebo experienced meaningful improvements in satisfying sexual events, sexual desire or distress. The drug, however, is not linked to enhanced sexual performance. Dizziness, sleepiness, nausea, fatigue, insomnia and dry mouth were the most commonly reported adverse reactions associated with use of Addyi. In clinical trials of women with acquired, generalized HSDD, about 3,000 women have received the 100-mg bedtime dose of Addyi, with about 1,700 receiving treatment for at least 6 months and 850 receiving treatment for at least 1 year. The release warns that Addyi can cause hypotension and syncope, and drinking alcohol or taking Addyi with certain medicines, including moderate or strong CYP3A4 inhibitors, can exacerbate the risk for these severe adverse events. The drug is also being approved with a risk evaluation and mitigation strategy (REMS) that includes elements to assure safe use (ETASU). The REMS is required by the FDA due to the increased risk for severe hypotension and syncope due to the interaction between Addyi and alcohol. Addyi also carries a Boxed Warning emphasizing the severe hypotension and syncope risks in those who drink alcohol during treatment or those who use moderate or strong CYP3A4 inhibitors as well as those who have liver impairment. The FDA is requiring the manufacturer to conduct three studies to better understand these risks. “Today's approval provides women distressed by their low sexual desire with an approved treatment option. The FDA strives to protect and advance the health of women, and we are committed to supporting the development of safe and effective treatments for female sexual dysfunction,” Janet Woodcock, MD, director of the FDA's Center for Drug Evaluation and Research (CDER), said in the release. “Because of a potentially serious interaction with alcohol, treatment with Addyi will only be available through certified health care professionals and certified pharmacies. Patients and prescribers should fully understand the risks associated with the use of Addyi before considering treatment.”