Names and pronunciation
(at-a-za-na′veer) Reyataz
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Drug reference
(at-a-za-na′veer) Reyataz
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Func. class.: Antiretroviral
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Chem. class.: Protease inhibitor
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ACTION: Inhibits human immunodefi- ciency virus (HIV-1) protease, which pre- vents maturation of the infectious virus
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USES: HIV-1 infection in combination with other antiretroviral agents
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CONTRAINDICATIONS: Hyper- sensitivity, Child-Pugh Class C Precautions: Pregnancy, breastfeeding, children, geriatric patients, hepatic dis- ease, alcoholism, drug resistance, AV block, diabetes, dialysis, females, hemo- philia, hypercholesterolemia, immune reconstitution syndrome, lactic acidosis, pancreatitis, cholelithiasis, serious rash
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SIDE EFFECTS CNS: Headache, depression, dizziness, insomnia, peripheral neuropathy CV: Increased PR interval GI: Vomiting, diarrhea, abdominal pain, nausea, hepatotoxicity, cholelithiasis INTEG: Rash, Stevens-Johnson syn- drome, photosensitivity, DRESS MISC: Fatigue, fever, arthralgia, back pain, cough, lipodystrophy, pain, gyneco- mastia, nephrolithiasis; lactic acidosis, hyperbilirubinemia (pregnancy, females, obesity), immune reconstitution syndrome
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INTERACTIONS Increase: levels, toxicity of immunosup- pressants (cycloSPORINE, sirolimus, tacro- limus), sildenafil, antifungals (itraconazole, ketoconazole, voriconazole), tricyclic anti- depressants, warfarin, calcium channel blockers, clarithromycin, clorazepate, diaz- ePAM, irinotecan, HMG-CoA reductase inhibitors, antidysrhythmics, midazolam, triazolam, ergots, pimozide, other protease inhibitors; monitor for toxicity (amprenavir, A darunavir, fosamprenavir, indinavir, nelfina- vir, ritonavir, saquinavir) Increase: effects of estrogens, oral con- traceptives (unboosted), decreased (boosted with ritonavir) Increase: atazanavir levels—CYP3A4 substrates, CYP3A4 inhibitors Increase: hyperbilirubinemia—indinavir Decrease: telaprevir level when used with atazanavir and ritonavir Increase: QT prolongation—salmeterol, clarithromycin, romiDEPsin, ranolazine; dose reduction of each of these products may be needed Increase: effect of alfuzosin, ARIPiprazole, benzodiazepine, brentuximab, cabazitaxel, carBAMazepine, cilostazol, colchicine, corti- costeroids, eletriptan, eplerenone, crizotinib, DOCEtaxel, ixabepilone, iloperidone, lurasi- done, maraviroc, muscarinic receptor antag- onists, nilotinib, opioids, vinca alkaloids (vin- CRIStine, vinBLAStine), vilazodone, vasopressin antagonists, dasatinib, lapatinib, SORAfenib, traZODone, risperIDONE, raltegra- vir, QUEtiapine Decrease: atazanavir levels—CYP3A4 inducers, rifAMPin, antacids, didanosine, efavirenz, proton pump inhibitors, H2-receptor antagonists; give atazanavir 2 hr before or 1 hr after these products Drug/Herb Decrease: atazanavir levels—St. John’s wort; avoid concurrent use Increase: myopathy, rhabdomyolysis— red yeast rice Drug/Lab Test Increase: AST, ALT, total bilirubin, amy- lase, lipase, CK Decrease: HB, neutrophils, platelets Drug/Food • Increased drug bioavailability (to be taken with food)
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DOSAGE AND ROUTES Antiretroviral-naive patients • Adult: PO 400 mg/day (unable to take ritonavir); 300 mg with ritonavir 100 mg/day • Child ≥6 yr/adolescent ≥40 kg: PO 300 mg with ritonavir 100 mg daily, or 400 mg/day (unable to take ritonavir) • Child ≥6 yr/adolescent Capsules, ≥6 years, ≥35-39 kg: atazanavir 300 mg with ritonavir 100 mg orally once daily with food • Child ≥6 yr/adolescent Capsules, ≥6 years, 15 kg to less than 35 kg: atazanavir 200 mg with ritonavir 100 mg orally once daily with food Antiretroviral-experienced patients • Adult: PO 300 mg with ritonavir 100 mg daily • Pregnant adults/adolescents (second/ third trimester) with H2 blocker or tenofo- vir: PO 400 mg with ritonavir 100 mg daily • Child ≥6 yr/adolescent ≥40 kg: PO 300 mg with ritonavir 100 mg daily • Child ≥6 yr/adolescent 20 to <40 kg: PO 200 mg with ritonavir 100 mg daily • Children and adolescents ≥25 kg: PO (oral powder) 300 mg q24hr with ritonavir 100 mg q24hr • Children 15 to 24 kg: PO (oral powder) 250 mg q24hr with ritonavir 80 mg q24hr • Infants and children ≥3 mo and 5 to 14 kg: PO (oral powder) 200 mg q24hr with ritonavir 80 mg q24hr Hepatic dose • Adult: PO Child-Pugh B: 300 mg/day; Child-Pugh C: do not use Renal dose • Adult: PO Therapy-naive and HD: 300 mg daily; with ritonavir: 100 mg daily; therapy experienced and HD: do not use
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Available forms: Capsules 100, 150, 200, 300 mg; oral powder 50 mg/packet
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Administer: • Capsules: With food; 2 hr before or 1 hr after antacid or didanosine; swallow capsule whole, do not open • Oral powder: Use with food or bever- age; mix 1 tablespoon of food with pow- der, feed, then add another tablespoon of food to container, mix, and feed; or mix with 30 mL of liquid, give, then add an- other 15 mL of liquid to cup to remove residual, give; use within 1 hr of mixing
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Assess: • For hepatic failure; hepatic studies: ALT, AST, bilirubin; do not use in Child-Pugh C • For lactic acidosis, hyperbilirubinemia (females, pregnancy, obesity); if pregnant, call Antiretroviral Pregnancy Registry 800-258-4263; do not breastfeed; use additional contraception when boosted with ritonavir • PR interval in those taking calcium channel blockers, digoxin, monitor ECG • For signs of infection, anemia, neph- rolithiasis • Bowel pattern before, during treat- ment; if severe abdominal pain with bleeding occurs, product should be dis- continued; monitor hydration • Viral load, CD4 count throughout treatment • Monitor blood glucose in those with diabetes • Monitor for opportunistic infections/ autoimmune disorder during treatment • Serious rash (Stevens-Johnson syn- drome, DRESS): most rashes last 1-4 wk; if serious, discontinue product • Immune reconstitution syndrome: time of onset is variable when given with combination antiretroviral therapy
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Evaluate: • Therapeutic response: increasing CD4 counts; decreased viral load, resolution of symptoms of HIV-1 infection
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take as prescribed with other anti- retrovirals as prescribed; if dose is missed, to take as soon as remembered up to 1 hr before next dose; not to dou- ble dose or share with others • That product must be taken daily to maintain blood levels for duration of therapy • To report yellowing of skin, sclera • To notify prescriber if diarrhea, nausea, vomiting, rash occurs; dizziness, light- headedness may occur; ECG may be altered • That product interacts with many products, including St. John’s wort; to advise prescriber of all products, herbal products used • That redistribution of body fat may occur, the effect is not known • That product does not cure HIV-1 in- fection, prevent transmission to others; only controls symptoms • That if taking phosphodiesterase type 5 inhibitor with atazanavir, there may be in- creased risk of phosphodiesterase type 5 inhibitor–associated adverse events (hypo- tension, prolonged penile erection); to notify physician promptly of these symptoms • Pregnancy/breastfeeding: that reg- istration with Antiretroviral Pregnancy Registry is strongly encouraged for preg- nant patients; to notify prescriber if preg- nancy is planned or suspected; to use additional contraception when boosted with ritonavir HIGH ALERT
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PHARMACOKINETICS Rapidly absorbed, absorption increased with food, peak 2½ hr, 86% protein bound, extensively metabolized in liver by CYP3A4, 27% excreted unchanged in urine/feces (minimal), half-life 7 hr
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• Child ≥6 yr/adolescent ≥40 kg: PO 300 mg with ritonavir 100 mg daily, or 400 mg/day (unable to take ritonavir)
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• Child ≥6 yr/adolescent Capsules, ≥6 years, ≥35-39 kg: atazanavir 300 mg with ritonavir 100 mg orally once daily with food
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• Child ≥6 yr/adolescent Capsules, ≥6 years, 15 kg to less than 35 kg: atazanavir 200 mg with ritonavir 100 mg orally once daily with food Antiretroviral-experienced patients
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• Pregnant adults/adolescents (second/ third trimester) with H2 blocker or tenofo- vir: PO 400 mg with ritonavir 100 mg daily
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• Child ≥6 yr/adolescent ≥40 kg: PO 300 mg with ritonavir 100 mg daily
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• Child ≥6 yr/adolescent 20 to <40 kg: PO 200 mg with ritonavir 100 mg daily
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• Children and adolescents ≥25 kg: PO (oral powder) 300 mg q24hr with ritonavir 100 mg q24hr
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