Company: MSD Ireland (Human Health) Ltd.
Legal category: Prescription. GMS reimbursable. Sport permitted.
Active ingredients: Elbasvir/grazoprevir 50/100mg.
Description: Beige, oval film‑coated tablet marked 770.
Presentation: 28, price on request.
Indication: Treatment of chronic hepatitis C in patients with genotypes 1a, 1b and 4.
Pharmacology: Elbasvir (HCV NS5A inhibitor) and grazoprevir (HCV NS3/4A inhibitor) combine two direct-acting antiviral agents which provide distinct mechanisms of action and non-overlapping resistance profiles to target HCV at multiple steps in the viral lifecycle. HCV NS5A, is essential for viral RNA replication and virion assembly. The HCV NS3/4A protease is necessary for the proteolytic cleavage of the HCV encoded polyprotein and is essential for viral replication.
Dosage: Adult: Swallow whole once daily. Genotype 1a, Zepatier for 12 weeks (consider Zepatier for 16 weeks plus ribavirin in patients with baseline HCV RNA level >800,000 IU/ml and/or presence of specific NS5A polymorphisms causing ≥5-fold reduction in elbasvir activity); genotype 1b, Zepatier for 12 weeks; genotype 4, Zepatier for 12 weeks (consider Zepatier for 16 weeks plus ribavirin in patients with baseline HCV RNA level >800,000 IU/ml). If vomiting occurs within 4 hours, take additional tablet. Elderly: As per adults. Children: Under 18 years, not recommended.
Contraindications: Hypersensitivity to the active substances or to any of the excipients. Moderate or severe hepatic impairment. Lactation.
Special precautions: Not recommended: HCV genotypes 2, 3, 5 and 6. Perform hepatic testing prior to therapy, at week 8, and as clinically indicated (with additional testing at week 12 for patients receiving 16 weeks of therapy). Seek immediate medical advice if onset of fatigue, weakness, lack of appetite, nausea and vomiting, jaundice or discoloured faeces occur. Consider discontinuation if ALT levels >10 X ULN. Discontinue if ALT elevation accompanied by signs of liver inflammation or increasing conjugated bilirubin, alkaline phosphatase, or international normalised ratio. Safety and efficacy not established: Liver transplant recipients, HCV/HBV co‑infected patients. Retreatment (including drugs of same class), efficacy not established. Pregnancy (assess risk/ benefit). Male patients and female partners of male patients taking ribavirin must use effective form of contraception; see ribavirin SPC. Patients requiring ribavirin (see ribavirin SPC prior to initiation). Driving/using machines (fatigue reported). Contains lactose, sodium.
Drug interactions: Contraindicated: Organic anion transporting polypeptide 1B (OATP1B) inhibitors, CYP3A or P-gp inducers, St. John’s wort, bosentan, efavirenz, etravirine, elvitegravir/ cobicistat/ emtricitabine/ tenofovir disoproxil fumarate (fixed-dose combination), modafinil, some anticonvulsants/ protease inhibitors/ immunosuppressants. Not recommended: Strong CYP3A inhibitors, some antifungals/ antimycobacterials. P-gp inhibitors (minimal effect), BCRP substrates, BSEP, tacrolimus, some anticoagulants. Atorvastatin, fluvastatin, lovastatin, simvastatin daily doses >20mg; rosuvastatin daily doses >10mg. Laboratory abnormalities.
Adverse drug reactions: Decreased appetite, insomnia, anxiety, depression, headache, dizziness, gastrointestinal disorders, pruritus, alopecia, arthralgia, myalgia, fatigue, irritability.
Full prescribing information and references available from MSD Ireland (Human Health) Ltd. Telephone: (01) 2998700.
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