Atazanavir Sulfate (6 brand names, 3 dosage forms, 1 route)
Available dosage forms: CAPSULE, TABLET, POWDER.
Routes of administration: ORAL.
Brand Names
- ATAZANAVIR SULFATE
- ATAZANAVIR SULFATE AND RITONAVIR
- ATAZANAVIR SULFATE; RITONAVIR
- ATAZANAVIR SULFATE;RITONAVIR;LAMIVUDINE;ZIDOVUDINE
- EVOTAZ
- REYATAZ
Indications and Usage
Atazanavir capsule is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and in pediatric patients 6 years and older weighing at least 15 kg. Limitations of Use: Atazanavir capsules are not recommended for use in pediatric patients below the age of 3 months due to the risk of kernicterus [see Use in Specific Populations (8.4)]. Use of atazanavir capsules with ritonavir in treatment-experienced patients should be guided by the number of baseline primary protease inhibitor resistance substitutions [see Microbiology (12.4)].
Contraindications
Atazanavir capsules are contraindicated: in patients with previously demonstrated clinically significant hypersensitivity (e.g., Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to any of the components of atazanavir capsules [see Warnings and Precautions (5.2)]. when coadministered with drugs that are highly dependent on CYP3A or UGT1A1 for clearance, and for which elevated plasma concentrations of the interacting drugs are associated with serious and/or life-threatening events (see Table 6). when coadministered with drugs that are strong inducers of CYP3A due to the potential for loss of therapeutic effect and development of resistance. Coadministration is contraindicated with, but not limited to, the following drugs listed in Table 6: Table 6: Drugs Contraindicated with Atazanavir Capsules (Information in the table applies to atazanavir capsules with or without ritonavir, unless otherwise indicated) a See Drug Interactions, Table 16 (7) for parenterally administered midazolam. b See Drug Interactions, Table 16 (7) for sildenafil when dosed as VIAGRA® for erectile dysfunction. Drug Class Drugs within class that are contraindicated with atazanavir capsules Alpha 1-adrenoreceptor antagonist Alfuzosin Antiarrhythmics Amiodarone (with ritonavir), quinidine (with ritonavir) Anticonvulsants Carbamazepine, phenobarbital, phenytoin Antimycobacterials Rifampin Antineoplastics Apalutamide, encorafenib, irinotecan, ivosidenib Antipsychotics Lurasidone (with ritonavir), pimozide Benzodiazepines Orally administered midazolama, triazolam Ergot Derivatives Dihydroergotamine, ergonovine, ergotamine, methylergonovine GI Motility Agent Cisapride Hepatitis C Direct-Acting Antivirals Elbasvir/grazoprevir; glecaprevir/pibrentasvir Herbal Products St. John’s wort (Hypericum perforatum) Lipid-Modifying Agents: Lomitapide, lovastatin, simvastatin Phosphodiesterase-5 (PDE-5) Inhibitor Sildenafilb when dosed as REVATIO® for the treatment of pulmonary arterial hypert
Adverse Reactions
The following adverse reactions are discussed in greater detail in other sections of the labeling: cardiac conduction abnormalities [see Warnings and Precautions (5.1)] rash [see Warnings and Precautions (5.2)] hyperbilirubinemia [see Warnings and Precautions (5.8)] chronic kidney disease [see Warnings and Precautions (5.5)] nephrolithiasis and cholelithiasis [ see Warnings and Precautions (5.6)]
Mechanism of Action
Atazanavir is an HIV-1 antiretroviral drug [see Microbiology (12.4)] .
Overdosage
Human experience of acute overdose with atazanavir is limited. Single doses up to 1200 mg (three times the 400 mg maximum recommended dose) have been taken by healthy participants without symptomatic untoward effects. A single self-administered overdose of 29.2 g of atazanavir in a patient with HIV-1 (73 times the 400 mg recommended dose) was associated with asymptomatic bifascicular block and PR interval prolongation. These events resolved spontaneously. At atazanavir doses resulting in high atazanavir exposures, jaundice due to indirect (unconjugated) hyperbilirubinemia (without associated liver function test changes) or PR interval prolongation may be observed [see Warnings and Precautions (5.1, 5.8) and Clinical Pharmacology (12.2)]. Treatment of overdosage with atazanavir should consist of general supportive measures, including monitoring of vital signs and ECG, and observations of the patient’s clinical status. If indicated, elimination of unabsorbed atazanavir should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid removal of unabsorbed drug. There is no specific antidote for overdose with atazanavir. Since atazanavir is extensively metabolized by the liver and is highly protein bound, dialysis is unlikely to be beneficial in significant removal of this medicine.