Antiretroviral, HIV protease inhibitor
ATC code: J05AE08 (Atazanavir)
Brand names
Reyataz
Competitive inhibitor of HIV-1 protease, the enzyme that cleaves viral polyproteins into functional proteins. Without cleavage, virions remain immature and non-infectious. Metabolised by CYP3A4 and itself inhibits CYP3A4 and UGT1A1. Absorption is gastric acid dependent – PPIs reduce bioavailability substantially.
Second line
Atazanavir is a second-line HIV-1 protease inhibitor. GeSIDA 2024 places it as an option when dolutegravir or bictegravir are not tolerated, usually combined with ritonavir or cobicistat as a booster plus 2 NRTIs. Advantage over other protease inhibitors – minimal lipid impact. Main limitation – gastric acid dependent absorption.
6 pairs found. Sorted from critical to minor.
Mechanism
CYP3A4 inhibition – fatal ergotism. Fatal cases reported.
Symptoms
Limb ischaemia, stroke.
Management
Combination contraindicated.
Mechanism
Omeprazole raises gastric pH – atazanavir solubility drops, bioavailability falls 75%. ART fails with resistance risk.
Symptoms
Rising HIV viral load on apparently ongoing therapy.
Management
Combination contraindicated. Switch omeprazole to ranitidine (H2 blocker) given 12 hours apart from atazanavir.
Mechanism
CYP3A4 inhibition by atazanavir raises pimozide – torsades de pointes.
Symptoms
QT prolongation, syncope.
Management
Combination contraindicated.
Mechanism
Strong CYP3A4 induction – atazanavir falls 80%. ART failure.
Symptoms
Rising viral load.
Management
Combination contraindicated.
Mechanism
Atazanavir inhibits CYP3A4. Simvastatin rises 10+ fold – fatal rhabdomyolysis.
Symptoms
Myalgia, dark urine within 5-10 days.
Management
Combination contraindicated. Switch to pravastatin or rosuvastatin.
Mechanism
Atazanavir inhibits CYP3A4. Atorvastatin rises 8-fold – rhabdomyolysis risk.
Symptoms
Myalgia, weakness, dark urine, rising CK within 5-10 days.
Management
Cap atorvastatin at 10 mg/day. Better – pravastatin 40 mg.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
HIV pregnancy registry shows no increase in birth defects. Can be used in pregnancy when ART is needed.
Breastfeeding by women with HIV is not recommended in Spain regardless of regimen.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Atazanavir is evaluated for the following indications with varying evidence strength: HIV infection (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Atazanavir (≥ 1 in 100): Hyperbilirubinaemia (without hepatocellular injury), Scleral icterus, Nausea, Rash, Headache. See the Safety section for uncommon and serious reactions.
FDA category B. HIV pregnancy registry shows no increase in birth defects. Can be used in pregnancy when ART is needed.
Breastfeeding by women with HIV is not recommended in Spain regardless of regimen.
Atazanavir is contraindicated in: PPI co-administration (omeprazole, esomeprazole) – ART failure; Simvastatin, lovastatin – rhabdomyolysis; Pimozide, ergotamine, oral midazolam, cisapride, rifampicin, St John's wort; Severe hepatic impairment. Full list in the Safety section.