Liver Part 1: Viral Hepatitis and Acute Liver Failure
Hepatitis B nucleos(t)ide analogues · Hepatitis C direct-acting antivirals · Hepatitis D · N-acetylcysteine
Hepatitis B: Nucleos(t)ide Analogues
| Agent |
Resistance Barrier |
Key Advantage |
Key Caution |
| Entecavir |
High (3 mutations needed) |
First-line treatment-naive; potent suppression |
Not preferred after lamivudine failure (cross-resistance) |
| Tenofovir disoproxil fumarate |
Highest (no documented resistance) |
Preferred after lamivudine failure |
Nephrotoxicity; bone mineral density loss with long-term use |
| Tenofovir alafenamide |
Highest |
Lower nephrotoxicity and bone effects; preferred in renal impairment |
Higher cost; not approved in all markets for all HBV indications |
| Lamivudine (old) |
Low (~20%/year) |
Historical; widely available |
No longer first-line; high resistance rate |
Hepatitis C: Direct-Acting Antiviral Drug Classes
NS3/4A Protease Inhibitors (-previr)
Glecaprevir, Voxilaprevir, Grazoprevir
- Block viral serine protease → prevents polyprotein cleavage
- Contraindicated in decompensated cirrhosis (worsens liver function)
- CYP3A4 inhibitors: strong CYP3A4 inducers (rifampin) cause treatment failure
NS5B Polymerase Inhibitor
Sofosbuvir (Nucleoside Analogue)
- Chain terminator of RNA-dependent RNA polymerase
- Pan-genotypic; backbone of most regimens
- P-glycoprotein substrate: P-gp inducers reduce absorption
- Fatal bradycardia with amiodarone — contraindicated combination
NS5A Inhibitors (-asvir)
Velpatasvir, Ledipasvir, Pibrentasvir
- Block replication complex assembly and virion assembly
- Ledipasvir: requires acidic absorption environment — avoid high-dose proton pump inhibitors
- Pan-genotypic agents: velpatasvir, pibrentasvir
Acute Liver Failure: N-Acetylcysteine and King’s College Criteria
N-Acetylcysteine Mechanism
Glutathione Replenishment
- Acetaminophen → CYP2E1/3A4 → NAPQI (reactive metabolite)
- NAPQI + glutathione → detoxified (normal doses)
- Overdose: glutathione depleted → NAPQI causes centrilobular necrosis
- N-acetylcysteine: cysteine precursor → replenishes glutathione
- Start within 8 hours: virtually eliminates severe hepatotoxicity
- Give even at >24 hours: still reduces mortality in established ALF
King’s College Criteria
Urgent Transplant Evaluation Threshold
- Acetaminophen ALF: arterial pH <7.3 after resuscitation; OR all three of: PT >100 s + creatinine >300 µmol/L + grade III–IV encephalopathy
- Non-acetaminophen ALF: PT >100 s alone; OR any 3 of 5: unfavorable etiology, age extremes, jaundice-to-encephalopathy >7 days, bilirubin >300 µmol/L, PT >50 s
- Meeting criteria: refer immediately for liver transplant evaluation
Critical Rule — Sofosbuvir + Amiodarone
Sofosbuvir combined with amiodarone has caused serious and fatal bradycardia including complete heart block. Amiodarone is absolutely contraindicated with sofosbuvir-containing hepatitis C regimens. Screen for amiodarone use before starting any direct-acting antiviral.