Classes
DEA Class; Rx
Common Brand Names; Evotaz
- HIV, ART Combos
Description
Fixed-dose combination product containing a protease inhibitor (PI) and a pharmacokinetic enhancer
Used with other antiretrovirals to treat HIV-1 infection in treatment-naive and experienced adults and pediatric patients weighing 35 kg or more
Use in treatment-experienced patients should be guided by the number of baseline primary PI resistant substitutions
Indications
Indicated in combination with other antiretroviral (ART) agents for treatment of human immunodeficiency virus type 1 (HIV-1)
Contraindications
Previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions)
Coadministration 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
Coadministration with drugs that strongly induce CYP3A and may lead to lower exposure and loss of efficacy of atazanavir/cobicistat
Adverse Effects
- Total bilirubin >2.5 xULN (65%)
- Ocular icterus, all grades (15%)
- Jaundice, all grades (13%)
- Nausea, all grades (12%)
- Jaundice, grades 2-4 (5%)
- Rash, grades 2-4 (5%)
- Creatinine kinase >10 xULN (5%)
- Serum amylase >2 xULN (4%)
- ALT/AST >5 xULN (3%)
- Ocular icterus, grades 2-4 (3%)
- Glycosuria ≥1000 mcg/dL (3%)
- Hematuria >75 RBC/HPF (3%)
- GGT >5 xULN (2%)
- Nausea, grades 2-4 (2%)
- Nephrolithiasis (2%)
- Gastrointestinal disorders: Diarrhea, vomiting, upper abdominal pain (<2%)
- General disorders and administration site conditions: Fatigue (<2%)
- Musculoskeletal and connective tissue disorders: Rhabdomyolysis (<2%)
- Nervous system disorders: Headache (<2%)
- Psychiatric disorders: Depression, abnormal dreams, insomnia (<2%)
- Renal and urinary disorders: Nephropathy, Fanconi syndrome (<2%)
Warnings
Atazanavir prolongs the PR interval of the electrocardiogram in healthy subjects and in subjects with HIV-1 infection treated with atazanavir, abnormalities in atrioventricular (AV) conduction were asymptomatic and generally limited to first-degree AV block; reports of second-degree AV block and other conduction abnormalities
Cases of Stevens-Johnson syndrome, erythema multiforme, and toxic skin eruptions, including drug rash, eosinophilia and systemic symptoms (DRESS) syndrome, have been reported; mild-to-moderate maculopapular skin eruptions have also been reported in atazanavir clinical trials and generally did not result in treatment discontinuation
Effects on serum creatinine: Assess eCrCl before initiating; cobicistat decreases estimated creatinine clearance, owing to inhibition of tubular secretion of creatinine, without affecting actual renal glomerular function
Chronic kidney disease in HIV-infected patients treated with atazanavir, with or without ritonavir reported; consider alternatives to therapy in patients at high risk for renal disease or with preexisting renal disease; renal laboratory testing (including serum creatinine, estimated creatinine clearance, and urinalysis with microscopic examination) should be conducted in all patients prior to initiating therapy and continued during treatment
Cases of nephrolithiasis and/or cholelithiasis have been reported during postmarketing surveillance in patients receiving atazanavir
Patients with underlying hepatitis B or C viral infections or marked elevations in transaminases may be at increased risk for developing further transaminase elevations or hepatic decompensation
Pregnancy and Lactation
Cases of lactic acidosis syndrome, sometimes fatal, and symptomatic hyperlactatemia have occurred in pregnant women using atazanavir in combination with nucleoside analogues
The CDC recommends that HIV infected mothers in the United States not breastfeed their infants to avoid risking postnatal transmission of HIV to infant
Unknown whether atazanavir or cobicistat are secreted in human milk
Maximum Dosage
300 mg/150 mg PO daily.
300 mg/150 mg PO daily.
weighing 35 kg or more: 300 mg/150 mg PO daily.
weighing less than 35 kg: Safety and efficacy have not been established.
weighing 35 kg or more: 300 mg/150 mg PO daily.
weighing less than 35 kg: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Atazanavir/cobicistat
EVOTAZ Oral Tab: 300-150mg