Merck & Co., Inc.
Pharmacological Class:
HCV NS3/4A protease inhibitor
Active Ingredient(s):
Boceprevir 200mg; caps.
Indication(s):
Chronic hepatitis C genotype 1 infection, in combination with peginterferon alfa and ribavirin (PR) in adult patients with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy. Not for use as monotherapy.
Pharmacology:
Boceprevir inhibits the hepatitis C virus (HCV) non-structural protein 3 serine protease by reversibly binding to an active site on this enzyme, thereby inhibiting viral replication in HCV-infected host cells.
Clinical Trials:
In a placebo-controlled study, adding boceprevir to PR significantly increased the sustained virologic response rates compared to PR alone. In subjects with cirrhosis at baseline, the sustained virologic response was higher in those who were given boceprevir + PR for 44 weeks (after lead-in therapy with PR) compared to those given response-guided therapy based on results at treatment weeks 8 through 24.
In another study, in patients who failed previous therapy with PR, adding boceprevir to PR significantly increased the sustained virologic response rates compared to PR alone. In those with cirrhosis at baseline, sustained virologic response was higher in patients treated with boceprevir + PR for 44 weeks (after lead-in therapy with PR) compared to those who received response-guided therapy.
Legal Classification:
Rx
Adults:
≥18yrs: Take with food. 800mg three times daily. Start after 4 weeks therapy with peginterferon and ribavirin. Without cirrhosis: continue treatment as indicated by HCV-RNA levels at weeks 8, 12, and 24 (see literature). With cirrhosis: continue for 44 weeks. Do not reduce dose. Discontinue if HCV-RNA levels indicate futility (see literature).
Children:
<18yrs: not recommended.
Contraindication(s):
Concomitant potent CYP3A4/5 inducers (eg, carbamazepine, phenobarbital, phenytoin, rifampin, St. John’s Wort) or narrow therapeutic index CYP3A4/5 substrates (eg, alfuzosin, cisapride, ergot derivatives, lovastatin, simvastatin, drosperinone, pimozide, sildenafil or tadalafil for PAH, triazolam, oral midazolam). Pregnant women and men whose partners are pregnant (note: ribavirin is Cat.X). Review peginterferon and ribavirin contraindications.
Warnings/Precautions:
Female patients and partners must have (–) pregnancy test before therapy, use appropriate effective contraception, and undergo monthly pregnancy test. Monitor CBC w. differential, HCV-RNA. Co-infection with HBV or HIV. Decompensated cirrhosis. Organ transplant recipients. Pregnancy (Cat.B). Nursing mothers: not recommended.
Interaction(s):
See literature. Concomitant rifabutin, salmeterol, efavirenz, concomitant colchicine in renal or hepatic impairment: not recommended. Potentiates CYP3A4/5 substrates (eg, amiodarone, bepridil, propafenone, quinidine, flecainide, trazodone, desipramine, azole antifungals, clarithromycin). Antagonizes ethinyl estradiol. Antagonized by potent CYP3A4/5 inhibitors. Monitor warfarin, digoxin, dihydropyridine calcium channel blockers, bosentan, protease inhibitors, immunosuppressants, opioids. Concomitant ketoconazole, itraconazole: max 200mg/day. Concomitant atorvastatin: max 20mg/day. Colchicine, PDE5 inhibitors for ED (eg, sildenafil, tadalafil, vardenafil), alprazolam, IV midazolam: reduce doses and monitor. Corticosteroids: avoid, monitor if needed.
Adverse Reaction(s):
Fatigue, nausea, headache, dysgeusia, worsening anemia, neutropenia.
How Supplied:
Bottles (12 caps/bottle)—28
Last Updated:
6/21/2011
VICTRELIS
制造商：
默克制药公司
NS3/4A蛋白酶抑制剂类药物：丙型肝炎病毒
活性成分（S）：Boceprevir 200毫克;帽。
指示（S）：慢性丙型肝炎基因型1感染，与聚乙二醇干扰素α和利巴韦林（PR）的成人患者的代偿期肝病，包括肝硬化，以前未经治疗，或谁没有以前的干扰素和利巴韦林治疗相结合。不适用于作为单一疗法使用。
药理学：Boceprevir抑制丙型肝炎病毒（HCV）非结构蛋白3可逆约束力的这种酶的活性部位的丝氨酸蛋白酶，从而抑制丙型肝炎病毒感染的宿主细胞中的病毒复制。
临床试验：在安慰剂对照研究中，加入boceprevir公关显著增加的持续病毒学应答率相比，公关单独。在受试者在基线肝硬化，这些人分别给予44周（铅治疗与公关后的持续病毒学应答）boceprevir + PR较高的响应引导治疗基于星期的治疗结果相比8至24 。
在另一项研究中，在失败与公关以往的治疗中，加入boceprevir公关的患者显着增加的持续病毒学应答率比公关单独。肝硬化在基线的持续病毒学应答，在治疗44周（铅治疗与公关后boceprevir + PR）的患者比那些收到的响应引导治疗。
法律分类：RX
成人：≥18yrs：随身携带食物。每天800毫克三个时代。与聚乙二醇干扰素和利巴韦林治疗4周后开始。无肝硬化：继续表示在8，12和24周HCV - RNA的水平（见文献）的治疗。肝硬化：持续44个星期。不要减少剂量。停止，如果HCV - RNA的水平表明徒劳的（见文献）。
儿童：<18yrs：不推荐。
禁忌（S）：同时服用强效CYP3A4 / 5的诱导剂（如卡马西平，苯巴比妥，苯妥英钠，利福平，圣约翰草）或狭窄的治疗指数CYP3A4 / 5底物（如，阿夫唑嗪，西沙必利，麦角衍生物，洛伐他汀，辛伐他汀，drosperinone ，匹莫齐特，西地那非或他达拉非的多环芳香烃，三唑仑，咪达唑仑口服）。孕妇和其合作伙伴是怀孕（注：利巴韦林Cat.X）。审查聚乙二醇干扰素和利巴韦林的禁忌。
警告/注意事项：必须有女性患者和合作伙伴（ - ）妊娠试验治疗前，使用适当，有效的避孕，并每月进行怀孕测试。监视器央行瓦特差，HCV - RNA的。与乙肝病毒或艾滋病毒的感染。代偿性肝硬化。器官移植。怀孕（Cat.B）。哺乳母亲：不推荐。
相互作用（S）：参见文献。伴随利福布丁，沙美特罗，伴随肾功能或肝功能不全的秋水仙素依非韦伦：不推荐。 Potentiates CYP3A4 / 5底物（如胺碘酮，苄普地尔，普罗帕酮，奎尼丁，氟卡尼，曲唑酮，地昔帕明，唑类抗真菌药，克拉霉素）。拮抗炔雌醇。拮抗强效CYP3A4 / 5抑制剂。监视器华法林，地高辛，二氢吡啶类钙通道阻滞剂，波生坦，蛋白酶抑制剂，免疫抑制剂，阿片类药物。同时服用酮康唑，伊曲康唑：最大200mg/day。同时服用阿托伐他汀：最大20mg/day。秋水仙素，磷酸二酯酶抑制剂对ED（例如，西地那非，他达拉非，伐地那非），阿普唑仑，咪达唑仑四：减少剂量和监测。皮质类固醇激素：避免，如果需要的话监控。
（S）的不良反应：疲劳，恶心，头痛，味觉障碍，恶化性贫血，嗜中性白血球减少症。
如何提供：瓶（12帽/瓶）-28
最后更新：2011年6月21日
