近日，美国食品和药物管理局（FDA）已批准（利匹韦林 rilpivirine：商品名Edurant），联合其他抗逆转录病毒药物治疗无HIV治疗史（首次治疗）的HIV-1型感染的成人患者。 Edurant属于非核苷类逆转录酶抑制剂（NNRTI），该类药物通过阻断HIV病毒复制来发挥作用。Edurant为高活性的抗逆转录病毒治疗（HAART）药物之一，通过抑制血液中HIV病毒载量发挥作用。Edurant丸剂餐时服用，每日一次。 FDA药品评价与研究中心抗菌产品办公室主任、医学博士、公共卫生硕士Edward Cox说：“不同的HIV药物会产生不同的效应反应或显示不同的副作用。Edurant的获批为HIV患者提供了另一种可获得的治疗方案。” 批准日期：2011年5月20日；Company: Tibotec Pharmaceuticals EDURANT(盐酸利匹韦林[rilpivirine])片，口服使用 首次美国批准：2011 近期重大变化 剂量和给药：02/2018 作用机理 利匹韦林是一种抗病毒药物[参见微生物学]。 适应症及用法 EDURANT是一种人类免疫缺陷病毒1型(HIV-1)特异性非核苷逆转录酶抑制剂(NNRTI)，与其他抗逆转录病毒药物联合应用治疗12岁及12岁以上体重至少35kg的幼稚患者HIV-1感染。HIV-1 RNA小于或等于100000拷贝/ml。 使用限制： ·与HIV-1RNA小于或等于100000拷贝/mL的受试者相比，在治疗开始时HIV-1RNA大于10万拷贝/mL的受试者经历病毒学失败(HIV-1RNA≥50拷贝/mL)。 剂量与给药 每次一片，每日一次，饭后服用。 ·对于在怀孕前已经采用稳定EDURANT方案并受到病毒学抑制(HIV-1RNA小于50拷贝/mL)的孕妇，建议剂量是每天随餐口服一片25毫克。 ·利福布汀联合用药：利福布汀联合用药期间，每天随餐服用2片25mg利福韦林。 剂型和强度 25毫克片剂 禁忌症 联合应用EDURANT禁忌使用利比韦林血浆浓度显著降低的药物，这可能导致病毒学应答的损失和可能的耐药性和交叉耐药性。 警告和注意事项 •皮肤和超敏反应：在售后经验中已经报告严重的皮肤和超敏反应，包括嗜酸性粒细胞病和系统性症状(DRESS)药物反应和利比韦林方案。如果过敏或皮疹伴全身症状或肝血清生化指标升高，立即停止治疗，并密切监测临床状态，包括肝血清生化指标。 肝毒性：据报道，包括乙型肝炎或丙型肝炎病毒合并感染在内的肝脏疾病患者或基线转氨酶升高的住院患者存在肝脏不良反应。未发生肝病的患者中有少数发生肝毒性。在用EDURANT治疗前和治疗期间监测潜在肝病患者的肝功能测试，如Bor C型肝炎病毒合并感染或转氨酶显著升高。 也考虑在没有肝功能异常或其他危险因素的患者中监测肝功能测试。 •抑郁症：有报道称存在严重的抑郁症。建议对重度抑郁症患者立即进行医学评估。 患者可发展为体脂或免疫重建综合征的再分配/蓄积。 不良反应 最常见的药物不良反应（发病率＞2%）至少是中度至重度（＞2级）为抑郁障碍， 头痛、失眠和皮疹。 要报告预期的不良反应，请联系Janssen.、LP、1-800-JansSEN(1-800-526-7736)或FDA、1-800-FDA-1088或www.fda.gov/med.。 药物相互作用 考虑与已知有扭转发作风险的药物联合用药的替代方案。 EDURANT不应与NNRTIS联合使用。 Eururand与诱导或抑制CYP3AAME的药物共同作用，影响瑞利韦林的血浆浓度。 联合用药与提高胃pH值的药物可能会降低血浆中rILPIVIN的浓度。 ·参照不宜与EDURANT联合使用的其他药物和可能需要剂量或方案镇痛的其他药物的全处方信息。 在特定人群中的使用 妊娠：与妊娠期相比，妊娠期总瑞利韦林暴露率普遍较低。 哺乳期：由于HIV传播的可能性，感染HIV的妇女应被告知不要母乳喂养。 包装供应/储存和搬运 EDURANT（RiPIVILIN）片剂以白色为白色，薄膜包衣，圆形，双凸形，6.4毫米片。每片含有27.5毫克的盐酸雷匹韦林，相当于25毫克的雷匹韦林。每一片都是一边“TMC”，一边是“25”。 EDURANT药片在瓶子中包装如下： 25毫克药片瓶 30（NDC 59667—27—01）。 将伊杜兰特药片放在原来的瓶子里，以防光线。贮藏剂片剂在25°C（77°F）；允许15°至30°C（59°-86°F）的漂移（参见USP控制）室温。 完整资料附件： 1）：https://www.janssenmd.com/pdf/edurant/edurant_pi.pdf 2）：https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202022s011lbl.pdf EDURANT(rilpivirine hydrochloride tablet) DESCRIPTION EDURANT (rilpivirine) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1). EDURANT is available as a white to off-white, film-coated, round, biconvex, 6.4 mm tablet for oral administration. Each tablet contains 27.5 mg of rilpivirine hydrochloride, which is equivalent to 25 mg of rilpivirine. Rilpivirine hydrochloride is a white to almost white powder. Rilpivirine hydrochloride is practically insoluble in water over a wide pH range. Each EDURANT tablet also contains the inactive ingredients croscarmellose sodium, magnesium stearate, lactose monohydrate, povidone K30, polysorbate 20 and silicified microcrystalline cellulose. The tablet coating contains hypromellose 2910 6 mPa.s, lactose monohydrate, PEG 3000, titanium dioxide and triacetin. CLINICAL PHARMACOLOGY Microbiology Mechanism of Action Rilpivirine is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) and inhibits HIV-1 replication by non-competitive inhibition of HIV-1 reverse transcriptase (RT). Rilpivirine does not inhibit the human cellular DNA polymerases alpha, beta and gamma EDURANT is a human immunodeficiency virus type 1 (HIV-1) specific, non-nucleoside reverse transcriptase inhibitor (NNRTI) indicated: In combination with other antiretroviral agents for the treatment of HIV-1 infection in treatment-naïve adult patients. The following points should be considered when initiating therapy with EDURANT: More EDURANT treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced virologic failure compared to subjects with HIV-1 RNA less than 100,000 copies/mL at the start of therapy. The observed virologic failure rate in EDURANT treated subjects conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz. More subjects treated with EDURANT developed lamivudine/emtricitabine associated resistance compared to efavirenz. Co-administration of EDURANT is contraindicated with drugs where significant decreases in rilpivirine plasma concentrations may occur, which may result in loss of virologic response and possible resistance and cross-resistance. WARNINGS AND PRECAUTIONS Caution should be given to prescribing EDURANT with drugs that may reduce the exposure of rilpivirine. Caution should be given to prescribing EDURANT with drugs with a known risk of Torsade de Pointes. Depressive Disorders: Severe depressive disorders (depressed mood, depression, dysphoria, major depression, mood altered, negative thoughts, suicide attempt, suicidal ideation) have been reported. Immediate medical evaluation is recommended for severe depressive disorders. Patients may develop redistribution/accumulation of body fat or immune reconstitution syndrome. DRUG INTERACTIONS EDURANT should not be used in combination with NNRTIs. Co-administration of EDURANT with drugs that induce or inhibit CYP3A4 may affect the plasma concentrations of rilpivirine. Co-administration of EDURANT with drugs that increase gastric pH may decrease plasma concentrations of rilpivirine. Refer to the Full Prescribing Information for other drugs that should not be co-administered with EDURANT and for other drugs that may require a change in dose or regimen. USE IN SPECIFIC POPULATIONS Pregnancy: Use during pregnancy only if the potential benefit justifies the potential risk. Pregnancy registry available. Nursing Mothers: Mothers should not breastfeed due to the potential for HIV transmission. ADVERSE REACTIONS The most common adverse drug reactions to EDURANT (incidence > 2%) of at least moderate to severe intensity (geq Grade 2) were depression, insomnia, headache and rash. About EDURANT® EDURANT(rilpivirine) is a prescription medicine that is used with other antiretroviral medicines to treat Human Immunodeficiency Virus-1 (HIV-1) in people 12 years of age and older and who weigh at least 77 lbs (35 kg): Have never taken HIV medicines before, and Have an amount of HIV in their blood (called "viral load") that is no more than 100,000 copies/mL EDURANT® is not recommended for patients less than 12 years of age or who weigh less then 77 lbs (35 kg) Please read Important Safety Information below, and talk to your healthcare provider to learn if EDURANT® is right for you.