EVOTAZ Dosage & Rx Info | Uses, Side Effects

Evotaz Generic Name & Formulations

Legal Class

General Description

Atazanavir 300mg, cobicistat 150mg; tabs.

Pharmacological Class

HIV-1 protease inhibitor + CYP3A inhibitor.

How Supplied

Tabs—30

Manufacturer

Bristol Myers Squibb

Generic Availability

Mechanism of Action

Atazanavir is an azapeptide HIV-1 protease inhibitor that selectively inhibits the virus-specific processing of viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions. Cobicistat is a mechanism-based inhibitor of cytochrome P450 3A (CYP3A). Inhibition of CYP3A-mediated metabolism by cobicistat increases the systemic exposure of the CYP3A substrate atazanavir.

Evotaz Indications

Indications

HIV-1 infection in combination with other antiretroviral agents.

Limitations of Use

Use in treatment-experienced patients should be guided by number of baseline primary protease inhibitor resistance substitutions.

Evotaz Dosage and Administration

Adults and Children

<35kg: not established. <3 months: not recommended. Take with food. 1 tab daily.

Evotaz Contraindications

Contraindications

Concomitant alfuzosin, ranolazine, dronedarone, carbamazepine, phenobarbital, phenytoin, colchicine (in renal/hepatic impaired), rifampin, irinotecan, lurasidone, pimozide, triazolam, oral midazolam, ergots, cisapride, elbasvir/grazoprevir, glecaprevir/pibrentasvir, St. John's wort, lomitapide, lovastatin, simvastatin, drospirenone/ethinyl estradiol, nevirapine, sildenafil (for PAH), indinavir.

Evotaz Boxed Warnings

Not Applicable

Evotaz Warnings/Precautions

Warnings/Precautions

Assess CrCl, SCr, urinalysis with microscopic exam prior to initiation and during therapy; consider discontinuing if progressive kidney disease develops. Concomitant tenofovir DF: assess baseline CrCl, urine glucose, and urine protein; if CrCl <70mL/min: not recommended; monitor serum phosphorous if risk of renal impairment. ESRD with hemodialysis in treatment-experienced or hepatic impairment: not recommended. Preexisting or at high risk for renal disease: consider alternatives. Cardiac conduction abnormalities; consider ECG monitoring if preexisting marked 1^st -degree AV block or 2^nd/3^rd -degree AV block. Consider interruption or discontinuation if nephrolithiasis or cholelithiasis occurs. Liver disease, hepatitis B and/or C, marked elevations in transaminases: monitor LFTs before and during therapy. Consider alternatives if jaundice or scleral icterus occurs. Diabetes. Hemophilia. Elderly. Pregnancy (use alternative therapy), nursing mothers: not recommended.

Evotaz Pharmacokinetics

Absorption

Tmax: 2 hours (atazanavir); 2 hours (cobicistat).

Distribution

Bound to human plasma proteins: 86% (atazanavir); ~98% (cobicistat).

Metabolism

Atazanavir: CYP3A (major), glucuronidation, N-dealkylation, hydrolysis, oxygenation with dehydrogenation (minor).
Cobicistat: CYP3A (major), CYP2D6 (minor).

Elimination

Half-life: 7.2 hours (atazanavir); 3.5 hours (cobicistat).
% excreted for atazanavir: Not determined.
% excreted for cobicistat: fecal (86.2%), renal (8.2%).

Evotaz Interactions

Interactions

See Contraindications. Separate dosing with concomitant H₂ receptor antagonists, PPIs (not recommended in treatment-experienced), antacids, enteric-coated didanosine. Concomitant tenofovir DF with concomitant or recent nephrotoxic agents, other antiretrovirals that require CYP3A inhibition (eg, HIV protease inhibitors, elvitegravir), ritonavir or ritonavir-containing products, CYP2C8 substrates with narrow therapeutic indices (eg, paclitaxel, repaglinide), H₂ receptor antagonists (in treatment-experienced), efavirenz, etravirine, boceprevir, simeprevir, sofosbuvir/velpatasvir/voxilaprevir, apixaban, rivaroxaban, dabigatran etexilate, atorvastatin, avanafil, inhaled/nasal steroids, salmeterol, voriconazole: not recommended. May need to adjust dose of insulin, antidiabetics, dasatinib, nilotinib, sildenafil, tadalafil, vardenafil, perphenazine, risperidone, thioridazine, buprenorphine, naloxone, methadone, tramadol, bosentan, rifabutin, sedatives/hypnotics, rosuvastatin (max 10mg/day); monitor. Concomitant maraviroc: give maraviroc 150mg twice daily. Potentiates quetiapine: consider alternative antiretrovirals; if coadministration necessary, reduce quetiapine to ⅙ of current dose and monitor. Monitor concomitant antiarrhythmics, digoxin, vincristine, vinblastine, warfarin, clonazepam, lamotrigine, SSRIs, TCAs, trazodone, fentanyl, immunosuppressants, other statins, β-blockers, CCBs. Concomitant clarithromycin, erythromycin, telithromycin, CYP3A-inducing anticonvulsants (eg, eslicarbazepine, oxcarbazepine), systemic corticosteroids (eg, dexamethasone): consider alternatives. Use alternative non-hormonal methods of contraception. See full labeling.

Evotaz Adverse Reactions

Adverse Reactions

Jaundice, rash (may be severe; discontinue if occurs), ocular icterus; hyperbilirubinemia, fat redistribution, immune reconstitution syndrome, hyperglycemia, CKD.

Evotaz Clinical Trials

See Literature

Evotaz Note