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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Protease inhibitors
atazanavir
J05AE08
Forms & Strengths
- Capsules: 150 mg, 200 mg, 300 mg
- Oral Powder: 50 mg packet
Adult Dosing
- Treatment-naive: 300 mg once daily with ritonavir 100 mg once daily with food
- Treatment-naive (unboosted): 400 mg once daily with food (not currently preferred)
- Treatment-experienced: 300 mg with ritonavir 100 mg once daily with food
- Pregnancy: 300 mg with ritonavir 100 mg once daily (second and third trimesters)
Pediatric Dosing
- Neonates (at least 3 months) and Children (35 kg to <40 kg): 200 mg with ritonavir 100 mg once daily
- Children (40 kg and greater): 300 mg with ritonavir 100 mg once daily
- Oral powder dosing based on strict weight-band matrices with ritonavir boosting
Indications
- Treatment of HIV-1 infection in combination with other antiretroviral agents
- Post-exposure prophylaxis for HIV in occupational and non-occupational settings (as part of combination regimens)
Mechanism of Action
- Aza-peptide HIV-1 protease inhibitor
- Selectively binds to the HIV-1 protease active site, inhibiting the cleavage of viral Gag-Pol polyproteins
- Prevents the maturation of infectious, mature viral particles
Contraindications
- Known hypersensitivity to atazanavir
- Co-administration with drugs highly dependent on CYP3A for clearance and whose elevated plasma concentrations cause serious/life-threatening events (e.g., alfuzosin, mefloquine, pimozide, cisapride, ergot derivatives, sildenafil for PAH, lovastatin, simvastatin, triazolam, oral midazolam)
- Co-administration with rifampin, St. John's wort, and proton pump inhibitors (in treatment-naive patients)
Adverse Reactions
- Hyperbilirubinemia (unconjugated hyperbilirubinemia, jaundice, scleral icterus)
- Nephrolithiasis and cholelithiasis
- PR interval prolongation (first-, second-, or third-degree AV block)
- Hyperglycemia, new-onset diabetes mellitus, or exacerbation
- Fat redistribution and immune reconstitution inflammatory syndrome
- Nausea, diarrhea, headache, fatigue, jaundice
Drug Interactions
- CYP3A4 inhibitors (e.g., ritonavir) increase atazanavir concentrations
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort) significantly decrease atazanavir efficacy
- Acid-reducing agents (PPIs, H2RAs, antacids) decrease atazanavir absorption; use with caution and follow specific separation or boosting rules
- Tenofovir DF concentrations may be increased; monitor renal function
- HCV direct-acting antivirals (e.g., glecaprevir/pibrentasvir, sofosbuvir/velpatasvir) have complex interactions requiring careful monitoring
- Statins (atorvastatin, rosuvastatin): increased risk of myopathy; use lowest possible doses
Curated Content: Needs Vetting Before Put to Clinical Use