---------------------------------------------------------------
 详细处方信息以本药内容附件PDF文件（201921918084019.pdf）的“原文Priscribing Information”为准
---------------------------------------------------------------
部分中文恩曲他滨处方资料（仅供参考）

【产品简介】
1981年，一种疾病被确定为获得性免疫缺乏综合症（AIDS），这种疾病严重破坏人体免疫系统，几乎没有例外的导致人体死亡。AIDS是由人免疫缺陷病毒（HIV）感染导致人体防御机能缺陷，而易于发生感染和肿瘤的临床综合症。HIV是单股RNA病毒，分为HIV-1和HIV-2两种。在世界范围内的HIV以HIV-1为主，占95%，HIV-2集中在西非地区。HIV病毒密码通过逆转录酶（reverse transcriptase）蛋白酶（protease）和整合酶（integrase）来表达。HIV一旦进入靶细胞，病毒RNA就在逆转录酶作用下逆转录为DNA，从而进行繁殖。因此，逆转录酶抑制剂是最早开发的抗HIV品种。最先用于临床的齐多呋啶（AZT）就是种逆转录酶抑制剂。
90年代中期，研究发现，一种叫拉米呋啶的逆转录酶抑制剂在抑制HIV病毒的同时，也能进入肝细胞内抑制HBV复制过程中必需的酶——HBV聚合酶，有效阻止HBV病毒的合成和复制。由于拉米夫定不能彻底消灭潜伏于肝细胞的静止状态的的HBV DNA（称为cccDNA），所以需长期服用拉米夫定，使病毒长期被抑制，并通过机体自身的免疫应答，从而取得持久的效果。因此也将它作为乙肝药开发并取得巨大成功。现贺普丁（拉米呋啶的商品名， 葛兰素史克生产）是国内疗效最好、用量最大的乙肝药，每年的销售额逾6亿元。
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。

【中文通用名】恩曲他滨

【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)
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.

---------------------------------------------------------------
 详细处方信息以本药内容附件PDF文件（201921918084019.pdf）的“原文Priscribing Information”为准
---------------------------------------------------------------