Atazanavir
REYATAZ
What it isHIV protease inhibitor; HIV infection.
Why this oneIts relatively favorable lipid profile distinguishes it from older boosted protease inhibitors.
What limits itPPIs impair absorption. Benign indirect hyperbilirubinemia causes visible jaundice; nephrolithiasis and PR prolongation also occur.
FDA-approved for
- HIV infection (2003)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection | Treatment-naive adults | 300 mg + ritonavir 100 mg QD (400 mg QD if ritonavir-intolerant) | 300 mg + ritonavir 100 mg QD | 400 mg/day |
| HIV-1 infection | Treatment-experienced adults | 300 mg + ritonavir 100 mg QD | 300 mg + ritonavir 100 mg QD | 300 mg + ritonavir 100 mg QD |
| HIV-1 infection | Pediatric 6 to <18 y, ≥15 kg | 200 mg (15–<35 kg) or 300 mg (≥35 kg) + ritonavir 100 mg QD | weight-based QD | 300 mg + ritonavir 100 mg QD (adult dose) |
Renal No adjustment incl. severe impairment; treatment-naive ESRD on hemodialysis: 300 mg + ritonavir 100 mg; not recommended in treatment-experienced ESRD on hemodialysis
Hepatic Child-Pugh A: 400 mg; Child-Pugh B: 300 mg; not recommended in severe (Class C), or with ritonavir in any degree of hepatic impairment
Instructions
- Take with food; do not open the capsules
- Separate dosing when given with H2-receptor antagonists or PPIs
- Must be given with ritonavir in pregnancy and in treatment-experienced patients
Contraindications
- Coadministration with drugs highly dependent on CYP3A or UGT1A1 for clearance where elevated levels cause serious/life-threatening events
- Coadministration with strong CYP3A inducers (risk of loss of efficacy and resistance)
- Contraindicated drugs (label Table 6, not exhaustive): alfuzosin; amiodarone (with ritonavir), quinidine (with ritonavir); carbamazepine, phenobarbital, phenytoin; rifampin; apalutamide, encorafenib, irinotecan, ivosidenib; lurasidone (with ritonavir), pimozide; orally administered midazolam, triazolam; dihydroergotamine, ergonovine, ergotamine, methylergonovine; cisapride; elbasvir/grazoprevir, glecaprevir/pibrentasvir; St. John's wort; lomitapide, lovastatin, simvastatin; sildenafil when dosed as Revatio for PAH; indinavir; nevirapine
Cautions
- PR-interval prolongation / cardiac conduction abnormalities
- Severe skin reactions (SJS, erythema multiforme, DRESS) — discontinue if severe rash
- Asymptomatic indirect hyperbilirubinemia — do not dose-reduce
- Hepatotoxicity in HBV/HCV co-infection
- Chronic kidney disease, nephrolithiasis, cholelithiasis
- New-onset/worsening diabetes and hyperglycemia
- Immune reconstitution syndrome; fat redistribution
- Increased bleeding in hemophilia
Adverse reactions
- Nausea
- Jaundice/scleral icterus
- Rash
- Headache
- Abdominal pain
- Vomiting
- Insomnia
- Peripheral neurologic symptoms
- Dizziness
- Myalgia
- Diarrhea
- Depression
- Fever
Pregnancy Human/animal data suggest no increased major birth-defect risk; must be given with ritonavir; monitor neonates for hyperbilirubinemia; APR registry
Lactation Present in human milk; breastfeeding not recommended due to HIV-1 transmission and potential adverse reactions
NO BOXED WARNINGS
Principal riskVisible jaundice from indirect hyperbilirubinemia
Cost, est. cash$10–$500/month
Generic entry2014
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Atazanavir ballicule
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