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Complera（恩曲他滨+利匹韦林+富马酸替诺福韦酯）复合制剂

2011-10-10 02:09:29 作者：新特药房来源：中国新特药网天津分站浏览次数：397 文字大小：【大】【中】【小】

简介： 艾滋病新药固定剂量三合一片剂Complera（emtricitabine-rilpivirine-tenofovir disoproxil fumarate，即恩曲他滨-利匹韦林-富马酸替诺福韦酯）于2011年8月11日获得美国FDA批准。这是获准的第二个三合一 ...

关键字：Complera（恩曲他滨+利匹韦林+富马酸替诺福韦酯）复合制剂

艾滋病新药固定剂量三合一片剂Complera（emtricitabine-rilpivirine-tenofovir disoproxil fumarate，即恩曲他滨-利匹韦林-富马酸替诺福韦酯）于2011年8月11日获得美国FDA批准。这是获准的第二个三合一抗艾滋病药物。Complera适用于从未作过治疗的HIV-1感染成人患者，Complera的用法为每日1次，与餐同服。

Complera(恩曲他滨/利匹韦林/替诺福韦酯)

制造商：
Gilead Sciences公司，公司

类药物：
核苷类似物逆转录酶抑制剂+非核苷逆转录酶抑制剂。

活性成分（S）：
为200mg恩曲他滨，替诺福韦disoproxil富马酸300毫克，rilpivirine 25毫克;选项卡
指示（S）：
HIV - 1感染。

药理学：
Complera是固定剂量组合的抗病毒药物恩曲他滨，rilpivirine和替诺福韦disoproxil富马酸。

临床试验：
rilpivirine疗效是基于两项试验在抗逆转录病毒治疗，天真的成年人（ECHO和茁壮成长）48周的数据分析。在回声，背景疗法（BR），替诺福韦DF +恩曲他滨。在蓬勃发展，BR包括下列操作之一：替诺福韦DF +恩曲他滨或齐多夫定+拉米夫定或阿巴卡韦+拉米夫定。受试者随机接受两种rilpivirine 25毫克，每日一次，或依非韦伦600毫克，每日一次，除了一个BR。两项试验在48周的汇总数据的基础上，<50 HIV - 1病毒RNA拷贝/ ml接受rilpivirine /替诺福韦DF /恩曲他滨（N = 550）相比受试者接受依法韦仑/替诺福韦DF /恩曲他滨（N科目的比例= 546），分别为83％和81％。平均从基线CD4 +细胞计数增加为193 cells/mm3 rilpivirine治疗的受试者和依非韦伦治疗的受试者的182 cells/mm3。

法律分类：
接收

成人：
以一餐。 1片，每日一次。肾功能损害（肌酐清除率<50mL/min）：不推荐。

儿童：
<18岁：不推荐。

禁忌（S）：
同时服用卡马西平，奥卡西平，苯巴比妥，苯妥英钠，利福布丁，利福平，利福喷丁，埃索美拉唑，兰索拉唑，奥美拉唑，泮托拉唑，雷贝拉唑，系统性地塞米松（多单剂量），圣约翰草。

警告/注意事项：
挂起如果乳酸性酸中毒或肝损伤的发生。妇女，肥胖，长期核苷暴露，肝功能障碍的其他风险因素：风险增加毒性。不适用于治疗慢性乙型肝炎;乙型肝炎病毒测试开始之前在几个月后停止治疗（停止治疗，可能会加剧HBV感染）与HIV - 1和HBV合并感染的治疗和监测病人。肾损害：肌酐清除率监测和血清磷。可能会延长QTc间隔supratherapeutic剂量。历史或骨折或骨质疏松的风险：监测骨矿物密度（BMD）;考虑维生素D和钙的补充。怀孕（乙部件）。哺乳母亲：不推荐。

相互作用（S）：
避免伴随药物含有恩曲他滨，替诺福韦，rilpivirine，拉米夫定或阿德福韦。恩曲他滨/替诺福韦：监视器的药物，减少肾功能或竞争肾小管分泌（例如，阿德福韦酯，西多福韦，阿昔洛韦，万乃洛韦，更昔洛韦，缬更昔洛韦）。避免随之而来的或近期使用肾毒性药物。 Rilpivirine：CYP3A的抑制剂Potentiated。拮抗CYP3A的诱导剂（见禁忌）。五月拮抗唑类抗真菌药（真菌感染的突破显示器），美沙酮（监察）。独立的制酸剂（至少2个小时前或至少4个小时后）和H2受体拮抗剂（前至少12小时或4小时后）rilpivirine;提高胃内pH值的药物，可能会导致血药浓度下降。与已知的危险尖端扭转型药物的注意。

不良反应（S）：
失眠，头痛，胃肠不适，乏力，头晕，抑郁，异常梦想，皮疹，脂肪的再分配，免疫重建综合征，乳酸性酸中毒，严重的脂肪变性（可能是致命的）肝肿大。

如何提供：
标签30

最后更新：
2011年9月22日

COMPLERA

Manufacturer:

Gilead Sciences, Inc.

Pharmacological Class:

Nucleoside analogue reverse transcriptase inhibitors + non-nucleoside reverse transcriptase inhibitor.

Active Ingredient(s):

Emtricitabine 200mg, tenofovir disoproxil fumarate 300mg, rilpivirine 25mg; tabs.

Indication(s):

HIV-1 infection.

Pharmacology:

Complera is a fixed-dose combination of antiviral drugs emtricitabine, rilpivirine and tenofovir disoproxil fumarate.

Clinical Trials:

The efficacy of rilpivirine is based on the analyses of 48-week data from two trials (ECHO and THRIVE) in antiretroviral treatment-naïve adults. In ECHO, the background regimen (BR) was tenofovir DF + emtricitabine. In THRIVE, the BR consisted of one of the following: tenofovir DF + emtricitabine or zidovudine + lamivudine or abacavir + lamivudine. Subjects were randomized to receive either rilpivirine 25mg once daily or efavirenz 600mg once daily in addition to a BR. Based on the pooled data from both trials at 48 weeks, the proportion of subjects with <50 HIV-1 RNA copies/mL receiving rilpivirine/tenofovir DF/emtricitabine (N=550) compared to subjects receiving efavirenz/tenofovir DF/emtricitabine (N=546) was 83% and 81%, respectively. The mean CD4⁺ cell count increase from baseline was 193 cells/mm³ for rilpivirine-treated subjects and 182 cells/mm³ for efavirenz-treated subjects.

Legal Classification:

Adults:

Take with a meal. 1 tablet once daily. Renal impairment (CrCl<50mL/min): not recommended.

Children:

<18 years: not recommended.

Contraindication(s):

Concomitant carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole, systemic dexamethasone (more than single dose), St. John’s wort.

Warnings/Precautions:

Suspend if lactic acidosis or hepatotoxicity occurs. Women, obesity, prolonged nucleoside exposure, other risk factors for hepatic dysfunction: increased risk of toxicity. Not for treating chronic hepatitis B; test for HBV before starting therapy and monitor patients coinfected with HIV-1 and HBV during and for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection). Renal impairment: monitor CrCl and serum phosphorus. May prolong QTc interval with supratherapeutic doses. History or risk of fractures or osteopenia: monitor bone mineral density (BMD); consider Vitamin D and calcium supplementation. Pregnancy (Cat. B). Nursing mothers: not recommended.

Interaction(s):

Avoid concomitant drugs that contain emtricitabine, tenofovir, rilpivirine, lamivudine, or adefovir dipivoxil. Emtricitabine/tenofovir: Monitor drugs that reduce renal function or compete for renal tubular secretion (eg, adefovir dipivoxil, cidofovir, acyclovir, valacyclovir, ganciclovir, valganciclovir). Avoid concomitant or recent use of nephrotoxic agents. Rilpivirine: Potentiated by CYP3A inhibitors. Antagonized by CYP3A inducers (see Contraindications). May antagonize azole antifungals (monitor for breakthrough fungal infections), methadone (monitor). Separate antacids (by at least 2 hours before or at least 4 hours after) and H₂-receptor antagonists (by at least 12 hours before or 4 hours after) rilpivirine; drugs that increase gastric pH may result in decreased plasma concentrations. Caution with drugs with a known risk for torsades de pointes.

Adverse Reaction(s):

Insomnia, headache, GI upset, fatigue, dizziness, depression, abnormal dreams, rash; fat redistribution, immune reconstitution syndrome, lactic acidosis, severe hepatomegaly with steatosis (may be fatal).