近日，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。
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。
批准日期：2006年7月15日  公司：Bristol-Myers Squibb and Gilead Sciences, LLC
ATRIPLA（依法韦仑，恩曲他滨和替诺福韦地索普西富马酸盐[efavirenz/emtricitabine/tenofovir disoproxil fumarate]）片剂，用于口服
美国最初批准：2006年
警告：对于完整的盒装警告，后处理急性乙型肝炎的检查请参见完整的预定信息。
已经报道了合并HBV和HIV-1的患者严重急性恶化乙型肝炎病毒（HBV），这些患者停用了含有恩曲他滨（FTC）和/或替诺福韦地索普西富马酸盐（TDF）的产品，并且可能在停用ATRIPLA时发生。在HIV-1和HBV合并感染并停用ATRIPLA的患者中，通过临床和实验室随访密切监测肝功能至少数月。如果合适，可能需要开始抗乙型肝炎治疗。
最近的重大变化
适应症和用法：07/2018
剂量和给药
在启动ATRIPLA之前进行测试：07/2018
成人和儿童患者的推荐剂量至少40公斤：07/2018
禁忌症：07/2018
警告和注意事项
HBV感染患者乙型肝炎严重急性发作期：07/2018
肝毒性（5.3）07/2018
与相关产品的共同管理：已删除：07/2018
精神症状：07/2018
新发作或恶化的肾功能损害：07/2018
作用机制
ATRIPLA是抗病毒药物依法韦仑，恩曲他滨和依诺福韦地索普西富马酸盐的固定剂量组合[见微生物学]。
适应症和用法
ATRIPLA是efavirenz（EFV），非核苷类逆转录酶抑制剂和恩曲他滨（FTC）和替诺福韦地索普西富马酸盐（TDF）的三种药物组合，两者均为HIV-1核苷类似物逆转录酶抑制剂，并表示为完整方案或与其他抗逆转录病毒药物联合用于治疗成人和体重至少40公斤的儿科患者的HIV-1感染。
剂量和给药
测试：在开始之前和ATRIPLA治疗期间，咨询完整的处方信息以获得重要的测试建议。
成人和儿童患者体重至少40公斤的推荐剂量：每天一片，空腹口服，最好在睡前服用。
肾功能损害：不建议估计肌酐清除率低于50mL/min的患者。
肝功能损害：不推荐用于中度至重度肝功能损害的患者。
利福平合用剂量调整：对于体重50公斤或以上的患者，建议额外服用200毫克/天的依法韦仑。
剂量形式和强度
片剂：600mg依法韦仑，200mg恩曲他滨和300mg替诺福韦地索普西富马酸盐。
禁忌症
先前已经证明了对efavirenz（ATRIPLA的组分）的超敏反应（例如，Stevens-Johnson综合征，多形性红斑或中毒性皮疹）。
与伏立康唑共同给药。
与elbasvir/grazoprevir共同管理。
警告和注意事项
皮疹：如果出现严重的皮疹，则停止使用。
肝毒性：监测患有潜在肝病的患者在治疗前和治疗期间的肝功能检查，包括乙型肝炎或丙型肝炎合并感染，转氨酶升高或正在服用与肝毒性相关的药物。在报告的肝衰竭病例中，少数发生在没有预先存在肝病的患者中。
药物相互作用引起的不良反应或病毒学应答损失的风险：在治疗前和治疗期间查阅完整的处方信息，以了解重要的潜在药物相互作用。考虑使用已知Torsade de Pointes风险的其他药物或Torsade de Pointes风险较高的患者的ATRIPLA替代品。
严重的精神症状：建议立即进行医学评估。
神经系统症状（NSS）：NSS常见，通常在开始治疗后1-2天开始，并在2-4周内消退。就寝时间给药可以改善耐受性。 NSS不能预测精神症状的发作。
新发病或恶化的肾功能损害：可包括急性肾功能衰竭和范可尼综合征。在开始和使用ATRIPLA之前，评估所有患者的血清肌酸酐，估计的肌酐清除率，尿糖和尿蛋白。在慢性肾病患者中，还要评估血清磷。避免给予ATRIPLA同时或最近使用肾毒性药物。
胚胎胎儿毒性：在妊娠头三个月给孕妇服用可能会发生胎儿伤害。在接受ATRIPLA时避免怀孕，在停药后12周避免怀孕。
骨密度（BMD）下降：考虑有病史骨折史或骨质疏松症或骨丢失的其他危险因素患者的BMD评估。
惊厥：对有癫痫病史的患者慎用。
乳酸性酸中毒/严重肝肿大伴脂肪变性：对出现症状或实验室检查发现乳酸性酸中毒或明显肝毒性的患者，停止治疗。
免疫重建综合症：可能需要进一步评估和治疗。
体脂肪的再分配/积累：在接受抗逆转录病毒治疗的患者中观察到。
不良反应
在EFV，FTC和TDF的主动对照临床试验中观察到的最常见的不良反应（发生率大于或等于10％）是腹泻，恶心，疲劳，头痛，头晕，抑郁，失眠，异常梦和皮疹。
要报告疑似不良反应，请致电1-800-GILEAD-5或FDA 1-800-FDA-1088或www.fda.gov/medwatch与Gilead Sciences，Inc。联系。
药物相互作用
在治疗前和治疗期间咨询完整的处方信息，以了解重要的潜在药物相互作用。
HIV-1蛋白酶抑制剂：ATRIPLA与洛匹那韦/利托那韦或地瑞纳韦和利托那韦共同给药可增加替诺福韦浓度。监测替诺福韦毒性的证据。不建议将ATRIPLA与阿扎那韦或阿扎那韦和利托那韦共同给药。
用于特定人群
怀孕：接受ATRIPLA时避免怀孕，停药后12周。
哺乳期：不推荐母乳喂养。
女性和生殖潜力的男性：建议进行妊娠试验和避孕。
儿科：皮疹的发病率高于成人。
包装提供/存储和处理
ATRIPLA片剂呈粉红色，胶囊状，薄膜包衣，一面凹陷，“123”，另一面平面。 每瓶含有30片（NDC 15584-0101-1）和硅胶干燥剂，并用儿童防护罩封闭。
储存在25°C（77°F）; 允许偏移15-30°C（59-86°F）[见USP受控室温]。
保持容器密闭。
仅在原始容器中分配。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2e97aa6d-09f7-46df-9499-63db7e9bac35 。

AIDS, Acquired Immunodeficiency Syndrome (AIDS), is an infectious disease caused by HIV (HIV), which is characterized by HIV-specific attack on helper T lymphocytes, causing progressive destruction of immune system functions, leading to various diseases. Opportunistic infections and the occurrence of related tumors.
AIDS has become a major infectious disease that threatens all mankind. From the 1981 report of the first case of AIDS in the United States to the present, the HIV epidemic has spread rapidly around the world. The latest epidemic report of UNAIDS in December 2006 shows that there are currently 39.5 million HIV/AIDS patients in the world. In 2006 alone, there were 4.3 million new infections and 2.9 million people died of AIDS.
The AIDS drug Atripla contains three drugs: efavirenz, emtricitabine and tenofovir disoproxil fumarate at a daily dose.
FDA approves the first tablet Atripla for the treatment of human immunodeficiency virus type 1 (HIV-1) infection (containing three doses of widely used antiretroviral drugs: fixed doses of efavirenz, emtricitabine and tenofovir) It can be used alone or in combination with other antiretroviral drugs to treat HIV-1 infected adult patients.
Atripla is also the first drug to treat HIV/AIDS one tablet at a time, and it uses at least three highly active antiretrovirals when starting treatment in accordance with the recommended principles of HIV infection.
Atripla simplifies the treatment of HIV-1 infection, making it easier for patients to adhere to treatment and helping to reduce the development of resistance to achieve long-term control of HIV-1 infection.
A 48-week clinical study of 244 patients with HIV-1 infection demonstrated that the combination of efavirenz, emtricitabine and tenofovir was safe and effective, with 80% of patients having significantly reduced HIV. The number of CD4 cells increased significantly.
Atripla's label includes a warning box that the drug can cause lactic acidosis. Patients with chronic hepatitis B can exacerbate hepatitis B infection after discontinuing Atripla (the FDA has not approved this indication). Other serious adverse events that may result include severe hepatotoxicity, kidney damage, and major depression. The most common adverse reactions are headache, dizziness, abdominal pain, nausea, vomiting, and rash.
Any questions, please follow the doctor's advice!
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