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Indications and Dosage
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.
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Renal Impairment
No dosage adjustment needed.
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Hepatic Impairment
No dosage adjustment needed.
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Administration
Should be taken with food. Take w/ meals or w/ a light snack.
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Contraindications
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.
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Special Precautions
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.
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Adverse Reactions
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). |
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PO: X (when used in combination w/ ribavirin & peginterferon α), B (as monotherapy)
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Patient Counseling Information
This drug may cause fatigue, dizziness, syncope, BP fluctuations and blurred vision, if affected, do not drive or operate machinery.
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Monitoring Parameters
Monitor CBC w/ differential and platelet count, baseline serum albumin, serum HCV-RNA, signs of infection and worsening of liver function.
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Drug Interactions
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). |
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Food Interaction
Food enhances absorption by up to 65%. Decreased serum concentration w/ St John's wort.
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Action
Description:
Mechanism of Action: 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. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Boceprevir, CID=10324367, https://pubchem.ncbi.nlm.nih.gov/compound/Boceprevir (accessed on Jan. 21, 2020) |
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Storage
Store between 2-8°C until expiration date or below 30°C for up to 3 mth.
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MIMS Class
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ATC Classification
J05AP03 - boceprevir ; Belongs to the class of antivirals for treatment of HCV infections. Used in the treatment of hepatitis C viral infections.
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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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