ATAZANAVIR
(a-ta-zan'a-vir)
Reyataz
Classifications: anti-infective; antiviral agent; antiretroviral agent; protease inhibitor
Prototype: Saquinavir
Pregnancy Category: B
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100 mg, 150 mg, 200 mg capsules
Atazanavir is an HIV-1 protease inhibitor that selectively inhibits the replication of HIV. Protease plays a major role in
the virus-specific processing of viral Gag and Gag-Pol gene products into key structural proteins and replication enzymes
of HIV-1 needed in the replication process of HIV-1 infected cells. Thus, protease is necessary for the production of mature
virions.
Protease inhibition renders the virus noninfectious. Because HIV protease inhibitors inhibit the HIV replication cycle after
translation and before assembly, they are active in acutely and chronically infected cells. Thus, atazanavir reduces the viral
load and increases CD4+ cell count.
Treatment of HIV infection in combination with other antiretroviral agents.
Hypersensitivity to atazanavir; severe hepatic insufficiency; lactation; concurrent administration of any of the following:
rifampin, irinotecan, midazolam, triazolam, bepridil, dihydroergotamine, ergotamine, ergonovine, methylergonovine, lovastatin,
simvastatin, pimozide, indinavir, St. John's wort; lactation; lactase deficiency.
Moderate hepatic impairment, hepatitis B or C; pregnancy (category B); neonates, infants, children; elderly, females, diabetes
mellitus, diabetic ketoacidosis; hemophilia, hepatic disease; hepatitis; jaundice, hypercholesterolemia, hyperglycemia, hypertriglyceridemia;
lactic acidosis, pancreatitis, obesity.
HIV Infection (treatment-naïve)
Adult: PO 400 mg once/d with a light meal
HIV Infection (treatment-experienced)
Adult: PO 300 mg once/d plus 100 mg ritonavir with food
Hepatic Impairment
Reduce dose to 300 mg once/d in moderate hepatic insufficiency; not recommended for use in severe hepatic insufficiency
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Oral
- Give with a light meal, not on an empty stomach.
- When coadministered with efavirenz, give atazanavir 300 mg and ritonavir 100 mg with efavirenz 600 mg (all as a single daily
dose with food). Atazanavir without ritonavir should not be coadministered with efavirenz.
- When coadministered with didanosine buffered formulations, give atazanavir (with food) 2 h before or 1 h after didanosine.
- Give 2 h before/1 h after antacids or buffered drugs.
- Store at 15°–30° C (59°–86° F).
Body as a Whole:
Peripheral neuropathy, fever, pain, fatigue, allergic reaction, angioedema, asthenia, burning sensation, chest pain, edema, facial atrophy, generalized
edema, heat sensitivity, infection, malaise, pallor, peripheral edema, photosensitivity, substernal chest pain, sweating. CNS:
Headache, depression, insomnia, dizziness, abnormal dream, abnormal gait, agitation, amnesia, anxiety, confusion, convulsion, decreased
libido, emotional lability, hallucination, hostility, hyperkinesia, hypesthesia, increased reflexes, nervousness, psychosis,
sleep disorder, somnolence, suicide attempt, twitch. CV:
Cardiac arrest, heart block (PR prolongation), hypertension, myocarditis, palpitation, syncope, vasodilatation. GI: Hyperbilirubinemia, jaundice, nausea, vomiting, diarrhea, abdominal pain, anorexia, aphthous stomatitis, colitis, constipation, dental pain, dyspepsia, enlarged abdomen, esophageal
ulcer, esophagitis, flatulence, gastritis, gastroenteritis, gastrointestinal disorder, hepatitis, hepatomegaly, hepatosplenomegaly,
increased appetite, liver damage, liver fatty deposit, mouth ulcer, pancreatitis, peptic ulcer. Endocrine: Decreased male fertility. Hematologic: Ecchymosis, purpura. Metabolic: Lipodystrophy syndrome, hypercholesterolemia, hypertriglyceridemia. Musculoskeletal: Myalgia, arthralgia. Respiratory: Cough, dyspnea, hiccup. Skin:
Rash, alopecia, cellulitis, dermatophytosis, dry skin, eczema, nail disorder, pruritus, seborrhea, urticaria, vesiculobullous rash. Special Senses: Otitis, taste perversion, tinnitus. Urogenital: Abnormal urine, amenorrhea, crystalluria, gynecomastia, hematuria, impotence, kidney calculus, kidney failure, kidney pain,
menstrual disorder, oliguria, pelvic pain, polyuria, proteinuria, urinary frequency, urinary tract infection.
Drug: May increase levels and toxicity of cyclosporine, systemic lidocaine, sirolimus, tacrolimus; increase risk of myopathy and rhabdomyolysis with atorvastatin, lovastatin, simvastatin; may increase risk of heart block with diltiazem;
antacids, h2-receptor antagonists, proton pump inhibitors may decrease absorption of atazanavir; ritonavir may increase atazanavir levels; may increase toxicity of irinotecan; increased risk of prolonged sedations with benzodiazepines; indinavir may increase risk of hyperbilirubinemia; didanosine, efavirenz, rifampin may decrease atazanavir levels; ergotamine, ergonovine dihydroergotamine, bepridil, pimozide may cause serious adverse reactions; may increase risk of hypotension, visual changes, and priapism with sildenafil, tadalafil, vardenafil.
Herbal:
St. John's wort may decrease atazanavir levels.
Absorption: 68% absorbed into systemic circulation; taking with food enhances bioavailability. Peak: 2–2.5 h. Metabolism: Metabolized in liver by CYP3A4. Elimination: 70% excreted in feces, 13% excreted in urine. Half-Life: 7 h.
Assessment & Drug Effects
- Monitor CV status and ECG closely, especially with concurrent treatment with other drugs known to prolong the PR interval.
- Lab tests: Baseline and periodic LFTs; total bilirubin if jaundiced; periodic PT/INR with concurrent warfarin therapy; monitor
blood glucose closely, especially if diabetic.
Patient & Family Education
- Do not alter the dose or discontinue therapy without consulting physician.
- Inform physician of all prescription, nonprescription, or herbal meds being used.
- Report promptly any of the following: dizziness or lightheadedness; muscle pain (especially with concurrent statin therapy);
severe nausea, vomiting (especially if red or "coffee-ground" in appearance), stomach pain, black tarry stools; yellowing
of skin or whites of eyes; skin rash or itchy skin; sore throat, fever, or other S&S of infection; unexplained tiredness or
weakness.
- If taking both sildenafil and atazanavir, promptly report any of the following sildenafil-associated adverse effects: hypotension,
visual changes, or prolonged penile erection.
1%)
Canadian drug name; 
Prototype drug