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atazanavir (Reyataz, ATV/r)

Tradename: Reyataz (FDA approved 2003) Indications: - treatment of HIV1 - may be boosted with saquinavir or darunavir - acceptable for use during pregnancy [4] Contraindications: - consider alternative regimen if 2 decreased function UGT1A1 alleles [5] - concurrent use of proton pump inhibitors [6] Dosage: 1) 300 mg PO QD 2) 400 mg PO QD (without ritonavir) . * take with food, absorption requires food & gastric acidity [6] Tabs: 150, 200, 300 mg Pharmacokinetics: 1) inhibits several cyt P450's 3) metabolized by cyt P450's Adverse effects: 1) does NOT increase serum cholesterol or serum triglycerides 2) lipodystrophy ? 3) hyperbilirubinemia (unconjugated bilirubin), jaundice (reversible) 4) does NOT seem to cause hepatotoxicity - serum ALT, serum AST, serum alkaline phosphatase normal 5) nephrolithiasis 6) nausea 7) rash Drug interactions: - many - proton pump inhibitors prevent absorption Laboratory: - UGT1A1 genotyping [5] - atazanavir in amniotic fluid - atazanavir in CSF - atazanavir in cord blood - atazanavir in serum/plasma Mechanism of action: - retroviral protease inhibitor

Interactions

drug interactions drug adverse effects (more general classes)

General

antiretroviral protease inhibitor

Properties

INHIBITS: protease

Database Correlations

PUBCHEM correlations

References

  1. Prescriber's Letter 10(8):45 2003
  2. Department of Veterans Affairs, VA National Formulary
  3. Chan-Tack KM et al Atazanavir-associated nephrolithiasis: Cases from the Food and Drug Administration's Adverse Event Reporting System. AIDS 2007, 21:1215 PMID: 17502736
  4. Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016)
  5. Clinical Pharmacogenetics Implementation Consortium (CPIC) guideline information for atazanavir and UGT1A1 https://www.pharmgkb.org/guideline/PA166128738Clinical Pharmacogenetics Implementation Consortium (CPIC) guideline information for atazanavir and UGT1A1 https://www.pharmgkb.org/guideline/PA166128738
  6. Medical Knowledge Self Assessment Program (MKSAP) 17, 18 American College of Physicians, Philadelphia 2015, 2018

Component-of

atazanavir/cobicistat (Evotaz)