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Atazanavir

Antiretroviral

Also known as ATZ, ritonavir-boosted atazanavir

Antiretroviral
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Manufacturer advises avoid —toxicity in animal studies.
FDA category + note
Top interactionssee all 12
  • Domperidone + OmeprazoleContraindicatedTextbookG&G 14e · p1245-1266
  • H2 Receptor AntagonistsContraindicatedTextbookG&G 14e · p1245-1266
  • Pantoprazole + DomperidoneContraindicatedTextbookG&G 14e · p1245-1266
  • ParietContraindicatedTextbookG&G 14e · p1245-1266

Mechanism

Atazanavir is an antiretroviral protease inhibitor that specifically targets the HIV-1 protease enzyme. It competitively binds to the active site of HIV-1 protease, preventing the cleavage of viral gag-pol polyproteins into their functional components. This inhibition leads to the production of immature, non-infectious viral particles, thereby disrupting the viral life cycle and reducing the viral load in HIV-infected patients.

Indications

HIV infection (as part of combination ART)HIV infection in pregnancy (as part of combination ART, with careful assessment by a specialist)HIV-1 and HIV-2 infection in adults and pediatric patients older than 3 months of age and weighing at least 5 kgHIV (in combination regimens)

Dosing

Adult
300 mg OD with ritonavir 100 mg taken at meal time.
Hepatic adjustment
Avoid in moderate impairment in those with co-existing moderate or severe renal impairment, and in severe impairment (risk of increased exposure)

Pharmacokinetics

Half-life
6.5–7.9
Bioavailability
Protein binding
86%
Metabolism
CYP3A4
Excretion
7% (renal, unchanged)

Contraindications

  • Moderate hepatic impairment in those with co-existing moderate or severe renal impairment
  • Severe hepatic impairment (risk of increased exposure)

Side effects

Common
unconjugated hyperbilirubinemiadiarrheanauseajaundice (in some patients without liver damage due to inhibition of hepatic glucuronyl transferase)
Serious
  • cholecystitis
  • cholelithiasis
  • cholestasis
  • hepatic function abnormalities
  • kidney stones
  • minimal dyslipidaemia and other metabolic complications

Pregnancy & lactation

Pregnancy

Manufacturer advises avoid —toxicity in animal studies.

Lactation

Manufacturer advises avoid —present in milk in animal studies.

Drug interactions

Domperidone + Omeprazole
Contraindicated
Textbook

Substantially reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

Proton pump inhibitors should be avoided in patients receiving atazanavir without ritonavir.

Source: G&G 14e · p1245-1266

H2 Receptor Antagonists
Contraindicated
Textbook

Reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

H2 receptor antagonists should be avoided in patients receiving atazanavir without ritonavir.

Source: G&G 14e · p1245-1266

Pantoprazole + Domperidone
Contraindicated
Textbook

Substantially reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

Proton pump inhibitors should be avoided in patients receiving atazanavir without ritonavir.

Source: G&G 14e · p1245-1266

Pariet
Contraindicated
Textbook

Substantially reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

Proton pump inhibitors should be avoided in patients receiving atazanavir without ritonavir.

Source: G&G 14e · p1245-1266

Rabeprazole + Domperidone
Contraindicated
Textbook

Substantially reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

Proton pump inhibitors should be avoided in patients receiving atazanavir without ritonavir.

Source: G&G 14e · p1245-1266

Rifampin
Contraindicated
Textbook

Significantly reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

Contraindicated.

Source: G&G 14e · p1245-1266

Atorvastatin
Severe
Textbook-cited

Increased risk of rhabdomyolysis and myopathy.

Avoid concurrent use; if needed, use lowest statin dose

Source: KDT 7e · p948

Carbamazepine
Severe
Textbook-cited

Carbamazepine toxicity (diplopia, ataxia, drowsiness)

Avoid concurrent use or adjust dose with monitoring

Source: KDT 7e · p948

Cyclosporine
Severe
Textbook-cited

Nephrotoxicity and immunosuppression toxicity

Monitor cyclosporine levels and reduce dose

Source: KDT 7e · p948

Glibenclamide
Severe
Textbook-cited

Hypoglycemia.

Avoid concurrent use or adjust dose

Source: KDT 7e · p948

Gliclazide
Severe
Textbook-cited

Hypoglycemia

Avoid concurrent use or adjust dose

Source: KDT 7e · p948

Glimepiride
Severe
Textbook-cited

Hypoglycemia

Avoid concurrent use or adjust dose

Source: KDT 7e · p948

Related guidelines

Other Antiretroviral drugs

Ask House about Atazanavir

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-10 · House clinical team