Manufacturer:
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

制造商：
默克制药公司
药理分类：
丙型肝炎病毒蛋白酶抑制剂NS3/4A
活性成分（补）：
Boceprevir 200毫克;上限。

指示（补）：
慢性丙型肝炎基因型1感染，与聚乙二醇干扰素α和成人患者代偿性肝脏疾病，包括肝硬化，谁是谁以前未经处理或没有以前的干扰素和利巴韦林治疗利巴韦林（PR）的组合。不作为单一疗法使用。

药理作用：
Boceprevir可逆性结合，抑制了对这种酶的活性部位，从而抑制丙型肝炎病毒感染的宿主细胞的病毒复制的丙型肝炎病毒（HCV）的非结构蛋白3丝氨酸蛋白酶。

临床试验：
在安慰剂对照研究中，加入boceprevir的公关显着增加的持续病毒学应答率比单独公关。与基线肝硬化科目，持续病毒学反应较高，但谁分别给予44个星期boceprevir+公关（后铅与公关治疗）比较，通过24至者给予响应引导治疗结果的基础上在治疗8周。
在另一项研究中，患者谁失败，公关之前的治疗，增加boceprevir的公关显着增加的持续病毒学应答率比单独公关。在基线与肝硬化，这些持续的病毒反应，高于同boceprevir +公关患者治疗44周（后铅与公关治疗）相比，谁收到的响应引导治疗。

法律分类：
接收
成人：
≥18yrs：取食物。 800毫克，每日三次。
4周后开始与聚乙二醇干扰素和利巴韦林治疗。没有肝硬化：继续治疗由丙型肝炎病毒RNA水平表示在8周，12和24条（见文献）。肝硬化：持续44周。不要减少剂量。如果停止HCV- RNA的水平表明徒劳（见文献）。
儿童：
“18yrs：不推荐。
禁忌（补）：
伴随强大的CYP3A4 / 5诱导剂（如卡马西平，苯巴比妥，苯妥英钠，利福平，圣约翰草）或治疗指数狭窄的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，口服咪唑安定）。怀孕妇女和男人的合作伙伴是怀孕（注：利巴韦林是Cat.X）。回顾聚乙二醇干扰素和利巴韦林禁忌症。
警告/注意事项：
女性患者和合作伙伴必须有（-）治疗前怀孕测试，使用适当，有效的避孕措施，并进行每月妊娠试验。央行监测瓦特差，丙型肝炎病毒RNA。合作与乙肝病毒或艾滋病毒感染。失代偿期肝硬化。接受器官移植者。妊娠（Cat.B）。哺乳母亲：不推荐。
互动（补）：
见文献。伴随利福布丁，沙美特罗，依非韦伦，肾或肝功能不全伴秋水仙素：不推荐。 Potentiates的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，唑类抗真菌剂，克拉霉素）。拮抗炔雌醇。强有力的CYP3A4的拮抗/5抑制剂。监测华法林，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。伴随酮康唑，伊曲康唑：最大200mg/day。伴随阿托伐他汀：最大20mg/day。秋水仙素，为的对外债务（例如，西地那非，他达拉非，伐地那非），阿普唑仑，咪达唑仑静脉PDE5抑制剂：减少剂量和监视器。皮质类固醇：避免，如果需要监控。
不良反应（补）：
疲劳，恶心，头痛，味觉障碍，不断恶化的贫血，中性粒细胞减少。
如何提供：
瓶（12帽/瓶）-28