—新型失眠药物Belsomra(Suvorexant Tablets)获FDA批准上市 2014年8月13日，美国FDA批准默克的新型抗失眠药Belsomra(通用名suvorexant)，共有4个剂量（5，10，15，20毫克）被批准使用。Belsomra的主要副作用是第二天的嗜睡，所以用药7小时内应避免开车和其它复杂活动。 Belsomra是选择性促食素受体拮抗剂，在临床实验中有效地帮助患者更快入睡并延长睡眠时间，达到16个一级终点的15个。30和40毫克剂量的疗效最好，但由于次日嗜睡副作用被FDA拒绝。这次只批准4个20毫克以下剂量，并建议医生从最低剂量开始使用。由于潜在滥用风险，发放Belsomra需伴随FDA批准的患者用药指南。 BELSOMRA® (suvorexant)片为口服使用 美国初次批准：2014 作用机制 Suvorexant在失眠中发挥其治疗作用机制被假设是通过对食欲素受体的拮抗作用。The食欲素神经肽信号系统是一个觉醒中央启动子。阻断觉醒-促进神经肽食欲素A和食欲素B与受体OX1R和OX2R的结合被认为一致觉醒驱动。 食欲素手的拮抗作用可能也有潜在不良作用例如发作性睡病/猝倒的征象。Genetic mutations in the在动物中食欲素系统的遗传突变导致遗传性发作性睡病；曾报道在人有发作性睡病中食欲素神经元的丧失。 适应证和用途 BELSOMRA是一种食欲素受体拮抗剂适用为治疗特征为难以入睡和/或维持睡眠的失眠(1)。 剂量和给药方法 ⑴ 对患者使用最低有效剂量。 ⑵ 推荐剂量是10mg，每夜不超过1次睡前30分钟内服用，计划觉醒时间前至少有7小时剩余。如10mg剂量被良好耐受但无效，可增加剂量，剂量不超过每天1次20mg。 ⑶ 如与食物或进餐后立即服用至起效时间可能延迟。 剂型和规格 片，5mg，10mg，15mg，20mg. www.oneyao.net Belsomra(suvorexant,MK-4305) BELSOMRA CIV Pharmacological Class: Orexin receptor antagonist. Active Ingredient(s): Suvorexant 5mg, 10mg, 15mg, 20mg; tablets. Company Merck & Co., Inc. Indication(s): Treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance. Pharmacology: The mechanism by which suvorexant exerts its therapeutic effects in insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive. Clinical Trials: The efficacy of Belsomra was evaluated in 3 clinical trials in patients with insomnia characterized by difficulties with sleep onset and sleep maintenance. Two similarly designed, 3-month, randomized, double-blind, placebo-controlled, parallel-group studies were conducted (Study 1 and 2). In both studies, non-elderly adults (ages 18–64) were randomized to Belsomra 20mg (n=291) or placebo (n=449), and elderly adults (ages ≥65) were randomized to Belsomra 15mg (n=202) or placebo (n=318). In Study 1 and Study 2, Belsomra 15mg or 20mg was superior to placebo for sleep latency as assessed both objectively by polysomnography and subjectively by patient-estimated sleep latency. Belsomra 15mg or 20mg was also superior to placebo for sleep maintenance, as assessed both objectively and subjectively. In a 1-month crossover study (Study 3), non-elderly adults were randomized to placebo (n=249) or Belsomra 10mg (n=62), 20mg (n=61), or up to 80mg. Results showed Belsomra 10mg and 20mg were superior to placebo for sleep latency and sleep maintenance, as assessed by polysomnography. Belsomra was also evaluated at doses of 30mg and 40mg in the 3-month placebo-controlled trials. The higher doses were found to have similar efficacy to lower doses, but significantly more adverse effects were reported. For more clinical trials data, see full labeling. Legal Classification: CIV Adults: Use lowest effective dose. Take within 30 minutes of bedtime if able to get full night’s sleep (≥7 hours) before awakening. 10mg once per night; may increase if ineffective; max 20mg once daily. Concomitant moderate CYP3A inhibitors: 5mg once daily; max 10mg once daily. Effect may be delayed if taken with or soon after a meal. Children: Not established. Contraindication(s): Narcolepsy. Warnings/Precautions: Monitor for somnolence and CNS depression; discontinue or reduce dose if daytime somnolence develops. Risk of next-day impairment (including impaired driving). Monitor for worsening insomnia or abnormal thinking and behavioral changes. Consider discontinuing if any complex sleep behaviors develop. Depression. Monitor for suicidal ideation. Compromised respiratory function (eg, COPD, obstructive sleep apnea). Increased risk of exposure-related effects in obese women. Reevaluate if unresponsive after 7–10 days of treatment. Severe hepatic impairment: not recommended. Drug or alcohol abusers. Pregnancy (Category C). Nursing mothers. Interaction(s) Avoid alcohol. Potentiates CNS depression with other CNS depressants (eg, benzodiazepines, opioids, tricyclic antidepressants, alcohol); may need to adjust doses. Concomitant strong CYP3A inhibitors (eg, ketoconazole, itraconazole, posaconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, boceprevir, telaprevir, telithromycin, conivaptan): not recommended. Concomitant moderate CYP3A inhibitors (eg, amprenavir, aprepitant, atazanavir, ciprofloxacin, diltiazem, erythromycin, fluconazole, fosamprenavir, grapefruit juice, imatinib, verapamil); use reduced dose (see Adults). May be antagonized by strong CYP3A inducers (eg, rifampin, carbamazepine, phenytoin). Monitor digoxin. Adverse Reaction(s) Somnolence, headache, dizziness; CNS depression, daytime impairment, complex sleep-related behaviors (eg, sleep-driving), sleep paralysis, hallucinations, cataplexy-like symptoms. How Supplied: Blisters—30 LAST UPDATED: 3/27/2015