英文药名: Atripla(Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate Tablets) 中文药名: 依法韦恩茨+恩曲他滨+替诺福韦富马酸片 生产厂家: Gilead Sciences, LLC. 药品介绍 本品为复方制剂，由百时美施贵宝公司和加州生物技术公司（Gilead Sciences Inc.）共同研制 2006 年7月12日，由FDA批准上市。每片含Sustuva（efa-virenz,依发韦仑）600mg/Emt-riva（emtricitabine,恩曲他滨）200mg/Viread（tenofovir disoproxil fumar-ate，替诺福韦酯）300 mg。 FDA批准首个治疗1型人类免疫缺陷病毒(HIV-1)感染的复方片剂Atripla(含固定剂量依法韦仑、恩曲他滨和替诺福韦3种广泛使用的抗逆转录病毒药),可单独应用或与其他抗逆转录病毒药合用治疗HIV-1感染成年患者。Atripla也是第一种每次1片、每日只需服用1次治疗HIV/AIDS的药物,它符合推荐的HIV感染治疗原则开始治疗时至少使用3种高效抗逆转录病毒药。 Atripla简化了HIV-1感染的治疗方法,患者更易坚持治疗,而且有助于减少耐药性的产生,以达到长期控制HIV-1感染的目的。一项纳入244例HIV-1感染患者的为期48周的临床研究证明,联合应用依法韦仑、恩曲他滨和替诺福韦这3种药物安全、有效,80%的患者HIV显著减少,CD4细胞数显著增多。 Atripla的标签包括一个警告框,即该药可导致乳酸酸中毒。慢性乙型肝炎患者在停用Atripla(FDA没有批准这个适应证)后可加剧乙肝感染。其他可能导致的严重不良事件包括严重肝毒性、肾损伤和重症抑郁。最常见的不良反应有头痛、头晕、腹痛、恶心、呕吐和皮疹。 任何疑问，请遵医嘱！ ATRIPLA Rx Generic Name and Formulations: Efavirenz 600mg, emtricitabine 200mg, tenofovir disoproxil fumarate 300mg; tabs. Company: Bristol-Myers Squibb and Gilead Indications for ATRIPLA: HIV-1 infection, use alone or in combination with other antiretroviral agents. Adult: Take on empty stomach. ≥12yrs and ≥40kg: 1 tab once daily (preferably at bedtime). Concomitant rifampin (≥50kg): give additional 200mg/day of efavirenz. Children: <12yrs: not recommended. Pharmacological Class: Non-nucleoside reverse transcriptase inhibitor + reverse transcriptase inhibitors (nucleoside + nucleotide analogue). Contraindications: Concomitant voriconazole. Warnings/Precautions: Risk of lactic acidosis or severe hepatomegaly with steatosis; suspend if occur. Assess CrCl prior to initiating therapy in all patients. Monitor CrCl, serum phosphorus, urine glucose and proteins prior to initiation and then periodically in patients at risk for renal impairment. Not for treating chronic hepatitis B virus; test for HBV before starting therapy and closely monitor patients co-infected with HBV and HIV during and for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection). Women, obesity, prolonged nucleoside exposure, other risk factors for hepatic dysfunction: increased risk of toxicity. Hepatic or renal impairment (CrCl<50mL/min): not recommended. Monitor liver enzymes before and during treatment (esp. with underlying hepatic disease). History or risk of fractures, osteoporosis or bone loss: consider bone mineral density (BMD) assessment; Vit. D and calcium supplementation may be beneficial. History of seizures. Elderly. Women of childbearing potential should undergo pregnancy testing prior to initiation. Use effective methods of contraception (barrier and hormonal) during and for 12 weeks after discontinuing treatment. Pregnancy (Cat.D); avoid. Nursing mothers: not recommended. Interactions: See Contraindications. Avoid concomitant drugs that contain emtricitabine, efavirenz, tenofovir, or lamivudine. Avoid alcohol, atazanavir, posaconazole, boceprevir, adefovir dipivoxil or other NNRTIs, psychoactive, and/or hepatotoxic drugs. Potentiates didanosine toxicity (>60kg; reduce dose of didanosine); discontinue didanosine if toxicity develops. Potentiates, and is potentiated by ritonavir (monitor liver function and for adverse events). Tenofovir levels increased by lopinavir/ritonavir; discontinue if toxicity occurs. Efavirenz levels decreased by phenobarbital, carbamazepine, phenytoin, rifampin, rifabutin. May decrease levels of indinavir (may be ineffective, even with increased dose), amprenavir, atazanavir, bupropion, carbamazepine, phenytoin, phenobarbital, clarithromycin, calcium channel blockers (eg, diltiazem, felodipine, nicardipine, nifedipine, verapamil), itraconazole, ketoconazole, lopinavir (adjust dose), maraviroc, methadone, rifabutin (increase dose), raltegravir, sertraline, statins, progestins (eg, norelgestromin, levonorgestrel), immunosuppressants (eg, cyclosporine, sirolimus, tacrolimus). Efavirenz increases nelfinavir plasma levels. Antagonizes, and is antagonized by, saquinavir (do not use as sole protease inhibitor), telaprevir. Caution with drugs metabolized by, or that affect activity of, CYP2C9, CYP2C19, CYP3A4. Closely monitor warfarin, anticonvulsants (esp. phenytoin, phenobarbital, carbamazepine), rifabutin, immunosuppressants, methadone, others. Monitor drugs that decrease renal function or compete for renal tubular secretion (eg, acyclovir, adefovir dipivoxil, cidofovir, ganciclovir, valacyclovir, valganciclovir, aminoglycosides, high-dose or multiple NSAIDs). Efavirenz may cause false (+) cannabis screening test (CEDIA DAU multi-level THC assay). Adverse Reactions: Diarrhea, nausea, fatigue, headache, dizziness, depression, insomnia, abnormal dreams, rash (may be severe, eg, Stevens-Johnson; discontinue if occurs), hallucinations, other CNS and psychiatric effects, skin discoloration; fat redistribution, immune reconstitution syndrome, lactic acidosis, severe hepatomegaly with steatosis, hepatotoxicity, others. Note: Register pregnant patients exposed to Atripla by calling (800) 258-4263. How Supplied: Tabs—30 本品美国上市： 本品德国上市： 艾滋病即获得性免疫缺陷综合征(AIDS),是由艾滋病病毒(HIV)引起的一种传染病,其特征是HIV特异性攻击辅助性T淋巴细胞,造成免疫系统功能进行性破坏,导致各种机会性感染和相关肿瘤的发生。艾滋病已成为威胁全人类的重大传染病,从1981年美国报道第1例艾滋病到至今的25年间,艾滋病病毒在全世界迅速蔓延。联合国艾滋病规划署(UNAIDS)2006年12月的最新流行报告显示,目前全球现存HIV/AIDS患者3950万例,仅2006年1年间,就有430万新感染病例,290万人死于艾滋病。 艾滋病药Atripla含3种药物：依法韦恩茨(efavirenz)、恩曲他滨(emtricitabine)和富马酸替诺福韦酯（tenofovir disoproxil fumarate），服用剂量为每日一片。