英文药名: Emtriva(Emtricitabine Capsules) 中文药名: 恩曲他滨胶囊 品牌药生产厂家: Gilead Sciences Inc 药品简介 FDA已经批准其上市核苷逆转录酶抑制剂Emtriva (emtricitabine)，用于与其他抗逆转录酶药物联合治疗HIV感染患者。Emtriva为一天服用一次，200mg/粒的胶囊剂。 临床试验已对用Emtriva进行初始治疗及已用过其他药物治疗的患者进行了Emtriva的相关评价。 Emtriva是Gilead Science公司上市的第二种一天一次用抗逆转录药物。Gilead在1996年从Emory大学引进此药。Gilead上市的第一种HIV治疗药Viread片剂(tenofovir disoproxil fumarate)为一日用药一次的核苷逆转录酶抑制剂，2001年已得到FDA的上市批准。 Emtriva被批准的适应症为与其他逆转录酶药物合用，治疗被HIV-1感染的成人患者。对照试验中，当与其他抗逆转录药物合用时，Emtriva可有效抑制HIV的复制，病人体内的病毒载量明显减少。 病人在接受Emtriva后，临床试验中最常见的不良反应为头痛，腹泻，恶心，皮疹，这些反应一般为轻中度。在单独使用核苷类似物或是与其他抗逆转录合用时，也有病人出现乳酸性酸中毒或伴有脂肪变性的肝肿大。 被HIV和慢性乙肝病毒同时感染的患者，也有报告称在停用Emtriva后，乙肝病情加重。肾功能障碍患者用药时应被严格监控，必要时需要剂量间隔调整。 恩曲他滨是由美国抗病毒药物的专业开发公司Gilead Sciences公司作为抗HIV、HBV药物开发的新产品。2003年7月，恩曲他滨（Emtriva）在美国被批准用于与其它抗转录病毒药物联用于成人HIV-1感染的治疗 。Emtriva是一种最新的核苷类逆转录酶抑制剂，这也是Gilead Sciences公司所开发的继Viread（tenofovir disoproxil fumarate）之后第二个每日给药一次的治疗艾滋病的抗逆转录病毒药物。 部分中文恩曲他滨处方资料（仅供参考） 【中文通用名】恩曲他滨胶囊 【别　名】Emtriva，FTC 【英文TNN名】EmtricItabine 【药品性质】处方药 【药品分类】国外最新药品 -> 抗微生物新药 【药理毒理】本品是一种新型核苷类逆转录酶抑制剂，对Hiv-1HIv-2及HBV均有抗病毒活性。本品口服后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。 【药代动力学】给雄性小鼠口服和静注单剂量本品100mg/kg100mg／kg或600mg／kg，结果显示，本品吸收好，清除快，且在研究所使用的剂量范围内其药代动力学呈剂量依赖性，总清除速率快接近于肾血流量。对HIV感染者单独给予本品100～1200mg，Tmax为1．25～1．61h。HIV感染者接受本品一日200mg，其血浆半衰期7．5～8h，本品三磷酸盐的细胞内半衰期大约为39h。 【适应症】与其他抗逆转录病毒药物联合用于成人Hiv感染的治疗。 【剂　型】恩曲他滨胶囊；200mg/粒。 【用法用量】18岁以上成人口服用药，每次200㎎，每日1次。空腹服用，也可与食物同服。肾功能不良者应调整剂量，改为200mg，隔日1次或每3天1次。 【不良反应】 1．全身腹痛、无力、头痛。 2．消化系统腹泻、消化不良、恶心、呕吐。 3.骨骼肌肉: 关节痛、肌痛。 4.神经系统: 睡梦异常、抑郁、头晕 、失眠、神经痛、外周神经炎、感觉异常。 5．呼吸系统: 咳嗽加重、鼻炎。 6. 皮肤疹。 【禁　忌】 1.已知对本品或其中任一组分过敏者禁用。 2.禁用于晚期肾病及肝功能不全者。 【慎用】 1.孕妇服用本品可能对胎儿和新生儿有不利影响。本品可通过乳脲分泌也可影响受乳婴儿，一般不推荐孕妇和哺乳期妇女使用本品。 2.老年人选择剂量时应慎重，可根据其肝、肾、心功能的衰退、伴发疾病以及其他药物治疗的影响，酌情减量服用。 【注意事项】 1.本品主要经肾排泄，故肾功能不全患者服用本品应减量。 2.儿童尚未建立安全有效的依据，故儿童不推荐使用。 3.尚无特效解救药，药物过量采用支持治疗。 【药物相互作用】本品不影响肝微粒体酶P 450酶系统，不产生由此介导的相互作用，与替诺氟韦、茚地那韦、泛昔洛韦、司坦夫定合用，药代动力学几乎无影响。 EMTRIVA-emtricitabine capsule EMTRIVA-emtricitabine solution Gilead Sciences, Inc. ---------- HIGHLIGHTS OF PRESCRIBING INFORMATION These highlights do not include all the information needed to use EMTRIVA safely and effectively. See full prescribing information for EMTRIVA. EMTRIVA (emtricitabine) capsule for oral use EMTRIVA (emtricitabine) solution for oral use Initial U.S. Approval: 2003 INDICATIONS AND USAGE EMTRIVA, a nucleoside analog HIV-1 reverse transcriptase inhibitor, is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. (1)   DOSAGE AND ADMINISTRATION EMTRIVA may be taken without regard to food. (2.1) Adult Patients (18 years of age and older) (2.2): EMTRIVA capsules: one 200 mg capsule administered once daily orally. EMTRIVA oral solution: 240 mg (24 mL) administered once daily orally. Pediatric Patients (0–3 months of age) (2.3): EMTRIVA oral solution: 3 mg/kg administered once daily orally. Pediatric Patients (3 months through 17 years) (2.4): EMTRIVA oral solution: 6 mg/kg up to a maximum of 240 mg (24 mL) administered once daily orally. EMTRIVA capsules: for children weighing more than 33 kg who can swallow an intact capsule, one 200 mg capsule administered once daily orally. Dose interval adjustment in adult patients with renal impairment (2.5): Hemodialysis Patients: If dosing on day of dialysis, give dose after dialysis. DOSAGE FORMS AND STRENGTHS Capsules: 200 mg (3) Oral solution: 10 mg per mL (3)   CONTRAINDICATIONS EMTRIVA is contraindicated in patients with previously demonstrated hypersensitivity to any of the components of the products. (4)   WARNINGS AND PRECAUTIONS Products with same active ingredient: Do not use with other emtricitabine-containing products (e.g., ATRIPLA and TRUVADA). (5.3) Redistribution/accumulation of body fat: Observed in patients receiving antiretroviral therapy. (5.5) Immune reconstitution syndrome: May necessitate further evaluation and treatment. (5.6)   ADVERSE REACTIONS Most common adverse reactions (incidence ≥10%) are headache, diarrhea, nausea, fatigue, dizziness, depression, insomnia, abnormal dreams, rash, abdominal pain, asthenia, increased cough, and rhinitis. Skin hyperpigmentation was very common (≥10%) in pediatric patients. (6) To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at 1-800-GILEAD-5 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch   USE IN SPECIFIC POPULATIONS Nursing mothers: Women infected with HIV should be instructed not to breast feed. (8.3) Pediatrics: Dose adjustment based on age and weight. (2.3, 2.4, 12.3) See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling  Revised: 07/2009  ---------------------------------------------------------------------- Emtriva (emtricitabine) What is Emtriva? •Emtriva is an HIV medication. It is in a category of HIV medicines called nucleoside reverse transcriptase inhibitors (NRTIs). Emtriva prevents HIV from entering the nucleus of healthy CD4 cells. This prevents the cells from producing new virus and decreases the amount of virus in the body.   •Emtriva, manufactured by Gilead Sciences, was approved by the U.S. Food and Drug Administration for the treatment of HIV in 2003.   •Emtriva is available in pharmacies as a single drug, which is always combined with other HIV drugs, or in the fixed-dose combination tablets Truvada (Viread and Emtriva) and Atripla (Viread, Emtriva, and Sustiva [efavirenz]).   •Emtriva is also active against the hepatitis B virus (HBV), the virus responsible for hepatitis B. Although it has not been approved by the FDA for the treatment of hepatitis B, some doctors prescribe it to treat both hepatitis B and HIV. See What is known about side effects? below for more important information regarding Emtriva and hepatitis B.   •Gilead has established a patient assistance program (PAP) for people living with HIV who do not have private or public health insurance and are unable to afford Emtriva. What is already known about Emtriva? •For adults, the recommended Emtriva dose is one 200mg capsule once a day.   •Emtriva is approved for HIV-positive children. The correct dose of Emtriva will depend on the child's weight. For infants between 0 and 3 months, the correct dose is 3 mg per kilogram (mg/kg)of body weight, given once a day using the liquid formulation of the drug. For children 3 months to 17 years of age, the liquid formulation dose is 6 mg/kg once a day. Emtriva pills can also be taken by children weighing more than 33 kg—one 200 mg capsule once a day. To learn about treatment options for children, click here.   •The chemical structure of Emtriva looks very much like that of Epivir (lamivudine).   •Emtriva won't likely be effective for people who have already taken and become resistant to Epivir. This is because one of the key changes, or mutations, in HIV's genetic structure that occurs as a result of Epivir therapy also causes resistance to Emtriva.   •Studies have demonstrated that Emtriva is effective for the treatment of HIV when combined with other HIV drugs, usually with at least one other nucleoside reverse transcriptase inhibitor (NRTI) and either a protease inhibitor or non-nucleoside reverse transcriptase inhibitor (NNRTI). Emtriva should not be taken alone (as monotherapy) or with just one other HIV drug.   •For HIV-positive adults beginning HIV drug therapy for the first time, Emtriva is listed as a "preferred" NRTI option—used in combination with Viread (tenofovir)—by the United States Department of Health and Human Services in its treatment guidelines. To learn more about these recommendations and options, click here.   •Therapy with Emtriva can cause certain changes (mutations) in HIV's structure to occur. Some mutations will prevent Emtriva from working against HIV. The key mutation that causes resistance to Emtriva (the M184V mutation in HIV's reverse transcriptase gene) can cause the virus to be at least partially resistant to other NRTIs, and will likely prevent the NRTI Epivir from working at all against the virus. However, Emtriva resistance might make the virus even more sensitive to other NRTIs, most notably Retrovir (even if HIV has mutations in its structure that would normally cause it to be resistant to Retrovir) and Viread.   •Emtriva also appears to be active against the hepatitis B virus (HBV), a virus that can cause liver damage in a small number of people infected by it. Clinical trials are examining the activity of Emtriva against HBV in both patients with and without HIV infection. What about drug interactions? •Emtriva should not be taken at the same time as Atripla, Truvada, Epivir or other combination tablets that contain Epivir (for example, Epzicom, Combivir, or Trizivir). This is because these medications contain the same or similar active ingredients as Emtriva.   •No significant drug interactions have been identified. However, this does not mean that other interactions aren't possible. More research is needed to understand the possible interactions between Emtriva and other medications. What is known about side effects? •The most common side effects caused by drug regimens containing Emtriva are headache, diarrhea and nausea. Other side effects include allergic reaction, dizziness, sleeping problems, abnormal dreams, vomiting, indigestion, stomach pain, pain, weakness and rash. Skin discoloration (small spots and freckles) may also happen with Emtriva.   • Lactic acidosis, which can be fatal, and severe liver problems have been reported in people taking nucleoside reverse transcriptase inhibitors (NRTIs). Contact your doctor immediately if you experience nausea, vomiting, or unusual or unexpected stomach discomfort; weakness and tiredness; shortness of breath; weakness in the arms and legs; yellowing of the skin or eyes; or pain in the lower stomach area.   • If you have hepatitis B and HIV and plan to stop taking Emtriva, you need close medical follow-up and for several months and your doctor might want to frequently check your liver enzymes after stopping treatment. This is because Emtriva is also active against the hepatitis B virus (HBV). If Emtriva is stopped abruptly, it can cause liver disease to "flare" and damage the liver.   •Other side effects may occur as a result of taking Emtriva. Be sure to discuss any and all side effects you experience while taking HIV medications with your healthcare provider. Can pregnant women take Emtriva? •Emtriva is classified by the FDA as a pregnancy category B drug. Pregnancy category B means that animal studies have failed to demonstrate a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women. HIV-positive women who become pregnant should discuss the benefits and possible side effects of HIV treatment to help protect their babies from HIV (see our lesson called Family Planning, Pregnancy & HIV).   •It is not known whether Emtriva passes into breast milk and what effect they may have on a nursing baby. To prevent transmission of the virus to uninfected babies, it is recommended that HIV-positive mothers not breast-feed. What should I tell my doctor before taking Emtriva? •Before taking this medication, tell your doctor if you have: kidney disease or liver disease (including hepatitis B).   •Tell your doctors and pharmacists about all medicines you take. This includes prescription medications, over-the-counter products, or herbal/natural remedies. Where can I learn more about clinical trials of Emtriva? •If you would like to find out if you are eligible for any clinical trials that include Emtriva, there is an interactive web site run by ACRIA, the AIDS Community Research Initiative of America.   •Another useful service for finding clinical trials is AIDSinfo.nih.gov, a site run by the U.S. National Institutes of Health. --------------------------------------------------------------- 原产地英文商品名: EMTRIVA CAPSULE 200MG/CAP 30CAPS/BOTTLE 原产地英文药品名: EMTRICITABINE 中文参考商品译名: EMTRIVA胶囊剂 200毫克/胶囊 30胶囊/瓶 中文参考药品译名: 恩曲他滨 生产厂家中文参考译名: GILEAD 生产厂家英文名: GILEAD --------------------------------------------------------------- 原产地英文商品名: EMTRIVA CAPSULE 200MG/CAP 60CAPS/BOTTLE 原产地英文药品名: EMTRICITABINE 中文参考商品译名: EMTRIVA胶囊剂 200毫克/胶囊 60胶囊/瓶 中文参考药品译名: 恩曲他滨 生产厂家中文参考译名: GILEAD 生产厂家英文名: GILEAD