Atripla是一种三合一的抗爱滋病药物sustiva (efavirenz), emtriva (emtricitabine) 和viread(tenofovir disoproxil fumarate), 一天只需服用一次的新型药物 药品名称 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 生产商:Bristol-Myers-Squibb和Gilead Sciences, LLC. 药品介绍 FDA批准ATRIPLA每日1次单一药片药物疗法用于治疗HIV-1感染的成年人 7月12日，百时美施贵宝公司和加州生物技术公司（Gilead Sciences Inc．）宣布美国FDA已经批准了ATRIPLA[依发韦仑（efavirenz）600mg／恩曲他滨（emtricitabine）200mg／替诺福韦酯（tenofovir disoproxil fumarate）300mg]用于治疗HIV—1感染的成年人。ATRIPLA是首种作为单独疗法或者与其他药物联合治疗HIV的每日1次单一药片药物。 Atripla(Efavirenz/Emtricitabine/Tenofovir Disoproxil Fumarate Tablets) Information on Atripla Learn more about usage, cautions, and possible side effects . Tablets Chemical Name: EFAVIRENZ (eh-FAV-er-enz), EMTRICITABINE (em-trye-SYE-ta-been), and TENOFOVIR DISOPROXIL FUMARATE (te-NOE-fo-veer dye-soe-PROX-ill FYOU-mar-ate) Common uses This medicine is an antiretroviral combination medicine used alone or with other medicines to treat human immunodeficiency virus (HIV) infection in adults. Before using WARNING: SEVERE AND SOMETIMES FATAL LACTIC ACIDOSIS (buildup of lactic acid in the blood) has occurred in some patients taking this type of medicine. The risk may be greater in women, patients who are very overweight, or patients who have been taking nucleoside medicines (such as emtricitabine) for a long time. CONTACT YOUR DOCTOR IMMEDIATELY if you develop extreme weakness or tiredness; unusual muscle pain; trouble breathing; stomach pain with nausea or vomiting; cold feeling, especially in the arms and legs; severe or persistent dizziness or lightheadedness; or fast or irregular heartbeat. SEVERE AND SOMETIMES FATAL LIVER PROBLEMS have also occurred in some patients taking this type of medicine. CONTACT YOUR DOCTOR IMMEDIATELY if you develop yellowing of the skin or eyes, dark urine, pale stools, loss of appetite, severe or persistent nausea, or stomach pain. THIS MEDICINE ISNOTAPPROVED TO TREAT HEPATITIS B INFECTION. Safety and effectiveness have not been confirmed in patients who have both HIV and hepatitis B. Some patients with hepatitis B who were treated with similar medicines have had severe worsening of liver problems after they have stopped treatment. Patients with both HIV and hepatitis B who take this medicine should have medical exams and liver function tests performed for at least several months after they stop taking this medicine. Some medicines or medical conditions may interact with this medicine. INFORM YOUR DOCTORORPHARMACIST of all prescription and over-the-counter medicine that you are taking. DO NOT TAKE THIS MEDICINE if you are taking any other medicinescontaining efavirenz, emtricitabine, or tenofovir. DO NOT TAKE THIS MEDICINE if you are taking any medicines containing lamivudine, or if you are taking astemizole, carbamazepine, cisapride, midazolam, triazolam, terfenadine, ergot medicines (such as ergotamine or ergonovine), St. John's wort, or voriconazole. ADDITIONAL MONITORING OF YOUR DOSE ORCONDITION may be needed if you are taking adefovir dipivoxil, cidofovir, acyclovir, valacyclovir, ganciclovir, valganciclovir, hormonal birth control (such as birth control pills), certain antifungal medicines(suchasitraconazoleorketoconazole), clarithromycin, certain medicines for high cholesterol (such as atorvastatin, pravastatin, or simvastatin), didanosine, HIV protease inhibitors (such as amprenavir, atazanavir, fosamprenavir, indinavir, lopinavir, ritonavir, or saquinavir alone), medicines for seizures (such as phenytoin or phenobarbital), methadone, rifabutin, rifampin, sertraline, or warfarin. DO NOT START OR STOP any medicine without doctor or pharmacist approval. Inform your doctor of any other medical conditions including a history of bone problems, diabetes, mood or mental problems, suicidal thoughts or actions, substance abuse, kidney problems, dialysis, liver problems (such as hepatitis B infection), seizures, very overweight, allergies, pregnancy, or breast-feeding. USE OF THIS MEDICINE IS NOT RECOMMENDED if you have a history of abnormal liver function tests, severe liver problems (such as enlarged liver or fatty liver), moderate to severe kidney problems, or lactic acidosis. Use of this medicine in children under age 18 is not recommended. Discuss with your doctor the risks and benefits of giving this medicine to your child. Contact your doctor or pharmacist if you have any questions or concerns about taking this medicine. Directions Follow the directions for using this medicine provided by your doctor. An additional patient information leaflet is available with this medicine. Read it carefully. Ask your doctor, nurse, or pharmacist any questions that you may have about this medicine. TAKE THIS MEDICINE BY MOUTH ON AN EMPTY STOMACH at least 1 hour before or 2 hours after eating. TAKE THIS MEDICINE WITH water. STORE THIS MEDICINE at room temperature at 77 degrees F (25 degrees C) in the original container, away from heat and light. Brief storage between 59 to 86 degrees F (15 to 30 degrees C) is permitted. Do not use this medicine if the seal over the bottle opening is broken or missing. Take this medicine regularly to receive the most benefit from it. Taking this medicine at the same time each day will help you to remember. CONTINUE TO USE THIS MEDICINE even if you feel well. Do not miss any doses. IF YOU MISS A DOSE OF THIS MEDICINE, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. DO NOT take 2 doses at once. Cautions DO NOT TAKE THIS MEDICINE if you have had an allergic reaction to it or are allergic to any ingredient in this product. DO NOT EXCEED THE RECOMMENDED DOSE OR CHANGE THE DOSE of this medicine without checking with your doctor. Exceeding the recommended dose of this medicine may not provide additional benefits and may increase the risks of side effects. DO NOT STOP USING THIS MEDICINE without first checking with your doctor. This may cause the amount of the virus to increase or may make the virus harder to treat. Also some conditions (such as Hepatitis B infection) may become worse when the medicine is suddenly stopped. LABORATORY AND/OR MEDICAL TESTS, including liver function, kidney function, and bone density tests may be performed to monitor your progress or to check for side effects. KEEP ALL DOCTOR AND LABORATORY APPOINTMENTS while you are taking this medicine. THIS MEDICINE MAY INTERFERE with certain laboratory tests (such as drug tests). Make sure laboratory personnel and your doctors know you use this medicine. THIS MEDICINE IS NOT A CURE FOR HIV INFECTION and will not prevent you from spreading HIV infection to others through blood or sexual contact. Use barrier methods of birth control (such as condoms) if you have HIV infection. THIS MEDICINE MAY IMPROVE IMMUNE SYSTEM FUNCTION. This may reveal hidden infections in some patients. Tell your doctor right away if you notice symptoms of infection (such as fever, sore throat, weakness, cough, or shortness of breath) after you start taking this medicine. THIS MEDICINE WILL ADD TO THE EFFECTS OF ALCOHOL and other depressants (such as sleep aids or tranquilizers). Ask your pharmacist if you have questions about which medicines are depressants. This medicine may cause dizziness or drowsiness. DO NOT DRIVE, OPERATE MACHINERY, OR DO ANYTHING ELSE THAT COULD BE DANGEROUS until you know how you react to this medicine. Using this medicine alone, with other medicines, or with alcohol may lessen your ability to drive or to perform other potentially dangerous tasks. CHECK WITH YOUR DOCTOR to see if you should take a calcium and vitamin D supplement while you are taking this medicine. BEFORE YOU BEGIN TAKING ANY NEW MEDICINE, either prescription or over-the-counter, check with your doctor or pharmacist. This includes St. John's wort. FOR WOMEN: THIS MEDICINE HAS BEEN SHOWN TO CAUSE HARM to the human fetus. Avoid becoming pregnant while you are taking this medicine. IF YOU SUSPECT THAT YOU COULD BE PREGNANT, contact your doctor immediately. FOR WOMEN USING HORMONAL BIRTH CONTROL (such as birth control pills), this medicine may decrease the effectiveness of your birth control. To prevent pregnancy, always use an additional form of birth control such as a condom or diaphragm. IT IS UNKNOWN if this medicine is excreted in the breast milk. Mothers infected with HIV should not breast-feed. There is a risk of passing the HIV infection or this medicine to the baby. IF YOU HAVE DIABETES, this medicine may affect your blood sugar. Check blood sugar levels closely and ask your doctor before adjusting the dose of your diabetes medicine. MONITOR BLOOD GLUCOSE on a regular basis, as directed by your doctor. Possible side effects SIDE EFFECTS that may occur while taking this medicine include diarrhea, discoloration of the skin, dizziness, drowsiness, gas, headache, heartburn, stomach upset, strange dreams, tiredness, trouble sleeping, trouble concentrating, or vomiting. These side effects tend to go away after a few weeks. If they continue or are bothersome, check with your doctor. Changes in body fat may occur while you are taking this medicine (e.g., increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Check with your doctor for more information. CHECK WITH YOUR DOCTOR AS SOON AS POSSIBLE if you experience agitation; anxiety; chronic back pain; a change in the frequency of urination or in the amount of urine produced; loss of appetite; loss of coordination; nervousness; muscle or joint pain; signs or infection (such as cough, fever, sore throat, or runny nose); or tingling or numbness of the hands, feet, or skin. CONTACT YOUR DOCTOR IMMEDIATELY if you experience behavior changes (such as angry or aggressive behavior); confusion; hallucinations; memory loss; symptoms of lactic acidosis (such as extreme weakness or tiredness, fast or irregular heartbeat, unusual muscle pain, severe stomach pain with nausea and vomiting, severe dizziness or lightheadedness, or feeling cold in the arms or legs); mood or mental changes (such as depression, delusions, paranoia, or suicidal thoughts or actions); symptoms of liver problems (such as yellowing of the skin or eyes, dark urine, loss of appetite, pale stool, severe or persistent nausea, or unusual fatigue); reddened, blistered or swollen skin; or seizures. An allergic reaction to this medicine is unlikely, but seek immediate medical attention if it occurs. Symptoms of an allergic reaction include rash, itching, swelling, severe dizziness, or trouble breathing. Drug interactions Drug interactions can result in unwanted side effects or prevent a medicine from doing its job. Use our drug interaction checker to find out if your medicines interact with each other. If you take too much IF OVERDOSE IS SUSPECTED, contact your local poison control center or emergency room immediately. Additional information If you have any questions concerning how to prevent spreading HIV infection to other people, ask your doctor, nurse, or pharmacist. Always use a condom during sexual intercourse. DO NOT SHARE THIS MEDICINE with others for whom it was not prescribed. DO NOT USE THIS MEDICINE for other health conditions. KEEP THIS MEDICINE out of the reach of children. IF YOU WILL BE USING THIS MEDICINE FOR AN EXTENDED PERIOD OF TIME, be sure to obtain necessary refills before your supply runs out. --------------------------------------------------- ATRIPLA Rx Add Drug To My List Compare to related Drugs View/edit/Compare drugs in my list Select the drug indication to add to your list ATRIPLA Viral infections  Only 4 drugs may be compared at once Generic Name and Formulations: Efavirenz 600mg, emtricitabine 200mg, tenofovir disoproxil fumarate 300mg; tabs. Company: Bristol-Myers Squibb and Gilead Select therapeutic use: Viral infections 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. Contraindications: Concomitant voriconazole. Warnings/Precautions: Risk of lactic acidosis or severe hepatomegaly with steatosis; suspend if occur. Women, obesity, prolonged nucleoside exposure, other risk factors for hepatic dysfunction: increased risk of toxicity. Not for treating chronic hepatitis B virus; test for HBV before starting therapy and monitor patients co-infected with HBV and HIV during and for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection). Assess CrCl prior to initiating therapy in all patients. Monitor CrCl, serum phosphorus, urine glucose and protein prior to initiation and periodically during therapy in patients at risk for renal impairment. 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, simeprevir, adefovir dipivoxil or other NNRTIs, psychoactive, and/or hepatotoxic drugs. Potentiates didanosine levels; monitor closely; discontinue or reduce didanosine dose if toxicity develops. Potentiates, and is potentiated by ritonavir (monitor liver function and for adverse events). Tenofovir levels increased by lopinavir/ritonavir, darunavir + ritonavir, ledipasvir/sofosbuvir; monitor and 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), antimalarials. Antagonizes saquinavir (do not use as sole protease inhibitor). 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). Pharmacological Class: Non-nucleoside reverse transcriptase inhibitor + reverse transcriptase inhibitors (nucleoside + nucleotide analogue). 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. Generic Availability: NO How Supplied: Tabs—30 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）600 mg/Emt-riva（emtricitabine,恩曲他滨）200 mg/Viread（tenofovir disoproxil fumar- ate，替诺福韦酯）300 mg。 Efavirenz是一种非核苷酸逆转录酶的抑制剂，其活性主要受HIV-1逆转录酶的非竞争性抑制的调节，但对HIV-2逆转录酶及人体细胞的DNA聚合酶 α，β，γ,δ没有抑制作用，其化学名：（S）-6-chloro-4- （cyclopropylethynyl）-1，4-dihydro-4-（trifluoromethyl）- 2H-3，1-benzo-xazin-2-one，分子式：C14H9CIF3NO2，相对分子质量315.68。白色到淡粉色结晶状粉末，几乎不溶于水。 Emtricitabine的化学名为：5-fluoro-1-（2R , 5S）- [2-（hydroxymethyl）-1，3-oxathiolan-5-yl]cyt-osine，分子式:C8H10FN3O3S,相对分子质量247.24。白色至灰白色结晶状粉末，25℃水中溶解度约为112 mg· mL-1。主要用于成年人HIV-1感染的治疗，作用机制为首先被磷酸化为具有细胞活性的5'-三磷酸盐，5'-三磷酸盐通过进入病毒DNA主链，与主链结合，导致链终止，从而抑制HIV-1逆转录酶及HBV DNA聚合酶活性。 Tenofovir disoproxil fumarate化学名：9-[（R）-2 [[bis[[（isopropoxycarbonyl）oxy]-meth-oxy]phos- phin州methoxy]propyl]adenine fumarate（1:1），化学式：C19H30N5O10P.C4H404，相对分子质量635.52。白色至灰白色结晶状粉末，25℃水中的溶解度约为 13.4 mg·mL-1。服用后可迅速被吸收并降解成活性物质替诺福韦，然后被细胞的酶磷酸化转变成活性代谢产物替诺福韦双磷酸盐，替诺福韦双磷酸盐可通过直接竞争性的与天然脱氧核糖底物相结合而抑制HIV-1逆转录酶，及通过插入DNA中终止 DNA链，其对哺乳动物的DNA聚合酶α，β及线粒体的聚合酶γ的抑制作用较弱。 Atripla是首个作为单独疗法或与其他药物联合治疗HIV的每日1次服药的药物，用于治疗HIV-1 感染的成年人。主要不良反应有腹泻、头痛、呕吐、腹痛、反胃及皮疹。 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 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。 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！