Boceprevir


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Chronic hepatitis C
Adult: Patients w/ compensated liver disease who are previously untreated or who have failed previous therapy: 800 mg tid (7-9 hrly) in combination w/ peginterferon alfa and ribavirin for a duration based on treatment response. Max: 2,400 mg/day. Missed dose: Skip dose if <2 hr before the next dose; if ≥2 hr before next dose, take the missed dose and resume normal dosing schedule.
Renal Impairment
No dosage adjustment needed.
Hepatic Impairment
No dosage adjustment needed.
Cách dùng
Should be taken with food. Take w/ meals or w/ a light snack.
Chống chỉ định
Hypersensitivity to boceprevir. Patient w/ autoimmune hepatitis. Male partners of pregnant women. Concomitant use w/ drugs highly dependent on CYP3A4/5 for clearance or strong CYP3A4/5 inducers. Pregnancy.
Thận trọng
Patient at risk for QT interval prolongation. Patient w/ platelet count <100,000/mm3 and/or serum albumin <35 g/L and/or signs of coagulapathy (INR >1.7). Lactation.
Phản ứng phụ
Anaemia, fatigue, headache, nausea, vomiting, taste disturbances; increased incidence of infection, blood dyscrasias (e.g. pancytopenia, leucopenia, neutropenia, thrombocytopenia), dry eyes or changes in vision, thyroid disturbances, reduced appetite, wt loss, dehydration, metabolic disturbances; palpitations, changes in BP, psychiatric disturbances, resp effects, CNS effects, tinnitus, alopecia, muscle and joint pain; frequent urination, erectile dysfunction, weakness, fever, chills, malaise.
Potentially Fatal: Rarely, deafness, haemolysis, thyroid neoplasms, cardiac arrhythmias, thrombotic disorders, pleural fibrosis and pleuritic pain, retinopathy, cerebral and retinal ischaemia, MI, cholecystitis, pancreatitis and gastritis. Serious acute hypersensitivity reactions (e.g. urticaria, angioedema, drug rash w/ eosinophilia and systemic symptoms (DRESS), Stevens-Johnson syndrome).
PO: X (when used in combination w/ ribavirin & peg-interferon alfa), B (as monotherapy)
Thông tin tư vấn bệnh nhân
This drug may cause fatigue, dizziness, syncope, BP fluctuations and blurred vision, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor CBC w/ differential and platelet count, baseline serum albumin, serum HCV-RNA, signs of infection and worsening of liver function.
Tương tác
May increase plasma concentrations of doxazosin, tamsulosin, and medicines known to prolong QT interval (e.g. amiodarone, quinidine, methadone, pentamidine, some neuroleptics).
Potentially Fatal: Elevated plasma concentrations w/ drugs highly dependent on CYP3A4/5 for clearance (e.g. midazolam, bepridil, pimozide, halofantrine, tyrosine kinase inhibitors, simvastatin, quetiapine, alfuzosin, silodosin, ergot derivatives). Reduced plasma exposure w/ strong CYP3A4/5 inducers (e.g. carbamazepine, phenytoin, phenobarbital, rifampicin).
Food Interaction
Food enhances absorption by up to 65%. Decreased serum concentration w/ St John's wort.
Tác dụng
Description: Boceprevir is a selective hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A) protease inhibitor. It binds reversibly to the NS3 protease active site serine (Ser139) through α-ketoamide functional group to inhibit viral replication in HCV-infected host cells.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Food enhances absorption by up to 65%. Time to peak plasma concentration: 2 hr.
Distribution: Volume of distribution: Approx 772 L. Plasma protein binding: Approx 75%.
Metabolism: Undergoes hepatic metabolism via the aldo-ketoreductase (AKR)-mediated pathway to inactive metabolites; to a lesser extent, oxidative metabolism by CYP3A4 or CYP3A5.
Excretion: Mainly via faeces (79%) w/ less than 10% as unchanged drug. Mean elimination half-life: Approx 3.4 hr.
Đặc tính

Chemical Structure Image
Boceprevir

Source: National Center for Biotechnology Information. PubChem Database. Boceprevir, CID=10324367, https://pubchem.ncbi.nlm.nih.gov/compound/Boceprevir (accessed on Jan. 21, 2020)

Bảo quản
Store between 2-8°C until expiration date or below 30°C for up to 3 mth.
Phân loại MIMS
Phân loại ATC
J05AP03 - boceprevir ; Belongs to the class of antivirals for treatment of HCV infections. Used in the treatment of hepatitis C viral infections.
References
Anon. Boceprevir. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/07/2015.

Buckingham R (ed). Boceprevir. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/07/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Boceprevir. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 13/07/2015.

Victrelis Capsules. U.S. FDA. https://www.fda.gov/. Accessed 13/07/2015.

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  • Victrelis
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