Generic Name: Ledipasvir + Sofosbuvir
Therapeutic Class: Hepatic Antiviral: HCV NS5A & NS5B Polymerase Inhibitor
Indications
This combination is indicated for the treatment of chronic hepatitis C virus (HCV) infection in adults and pediatric patients (3 years and older):
- Genotypes: Specifically effective against HCV genotypes 1, 4, 5, and 6.
- Cirrhosis: Suitable for patients without cirrhosis or with compensated cirrhosis. For decompensated cirrhosis, it is used in combination with Ribavirin.
- HCV/HIV Co-infection: Used in patients co-infected with HIV-1.
Dosage & Administration
Must be prescribed and monitored by a specialist (Hepatologist or Gastroenterologist).
- Standard Dose: One tablet (90 mg Ledipasvir + 400 mg Sofosbuvir) taken once daily.
- Administration: Can be taken with or without food. Consistency in timing is crucial for maintaining viral suppression.
- Treatment Duration: Typically 8, 12, or 24 weeks depending on prior treatment history and the presence of cirrhosis.
Description & Pharmacokinetics
This combination provides two direct-acting antiviral agents with distinct mechanisms of action.
Mechanism of Action:
Pharmacokinetics:
Mechanism of Action:
- Ledipasvir: An inhibitor of the HCV NS5A protein, which is required for viral RNA replication and assembly of HCV virions.
- Sofosbuvir: An inhibitor of the HCV NS5B RNA-dependent RNA polymerase, acting as a chain terminator to stop viral replication.
Pharmacokinetics:
- Absorption: Peak plasma concentrations are achieved in 4–4.5 hours (Ledipasvir) and 0.8–2 hours (Sofosbuvir).
- Protein Binding: Ledipasvir is >99.8% bound; Sofosbuvir is 61–65% bound.
- Excretion: Ledipasvir is primarily excreted in feces; Sofosbuvir is mainly excreted in urine.
Side Effects
Common side effects observed during clinical trials:
- Common: Fatigue, headache, and nausea.
- Psychological: Insomnia or irritability (less common).
- Serious: Symptomatic bradycardia (slow heart rate) when used with Amiodarone. Allergic reactions (rash, swelling) may occur.
Extra Important Information: Usage Insights
- HBV Reactivation: Screening for Hepatitis B (HBV) is mandatory before starting therapy to prevent life-threatening HBV reactivation.
- Antacid Interaction: Ledipasvir absorption is pH-dependent. Antacids, H2 blockers, and PPIs can significantly reduce its effectiveness.
- Amiodarone Warning: Co-administration with Amiodarone is NOT recommended due to the risk of serious bradycardia.
- Compliance: Missing doses can lead to treatment failure or viral resistance.
Storage
Store below 30°C in the original package. Keep the bottle tightly closed to protect from moisture.
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