Atazanavir

Indications
 Oral
HIV infection
Adult: Treatment-naive patient: 400 mg once daily or 300 mg once daily with ritonavir 100 mg once daily. If used with efavirenz: 400 mg with efavirenz 600 mg and ritonavir 100 mg; all given as single daily dose. For treatment-experienced patient: 300 mg once daily taken with 100 mg of ritonavir daily.
Hepatic impairment: Child-Pugh category B: Atazanavir should be used alone (for treatment naive patients) in doses of 300 mg daily.
Contraindications
 Hypersensitivity. Lactation. Concurrent admin with cisapride, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), rifampin, irinotecan, midazolam, triazolam, pimozide, simvastatin, lovastatin, indinavir, PPIs or St John's wort.
Warnings / Precautions
 Hepatic impairment; avoid use in severe impairment. Maintain adequate hydration. Monitor for signs of lipodystrophy. Caution when used in patients with DM, haemophilia or history of cardiac conduction disorders. Discontinue if acute haemolytic anaemia occurs. May prolong PR interval on ECG. Redistribution and accumulation of body fat may occur. Pregnancy.
Adverse Reactions
 Nausea, vomiting and diarrhoea. Taste disturbances, abdominal pain, anorexia, increased appetite, flatulence, asthenia, fatigue, sleep disturbances, headache, dizziness, paraesthesia, hypoaesthesia, myalgia, arthralgia, alopecia, pruritus and renal insufficiency. Myositis and rhabdomyolysis. Skin rashes may occasionally be severe.
Potentially Fatal: Stevens-Johnson syndrome and erythema multiforme.
Overdose Reactions
 Symptoms may include jaundice due to indirect (unconjugated) hyperbilirubinemia or PR interval prolongation. Treatment is supportive e.g. monitoring of vital signs and ECG, and observations of patient's clinical status. Unabsorbed drug may be removed by emesis or gastric lavage. Activated charcoal may also be used to aid in the removal of unabsorbed drug. Dialysis may not be beneficial.
Drug Interactions
 May increase the metabolism of theophylline. May increase plasma concentrations of antiarrhythmics, diltiazem and hormonal contraceptives when used concurrently. Reduced plasma levels when used with enzyme inducers e.g. carbamazepine, phenytoin, phenobarbital. Plasma levels may be increased by azole antifungals. Coadmin with PDE5 inhibitor may lead to visual changes and priapism.
Potentially Fatal: Increased risk of myopathy when used with lovastatin or simvastatin. Increased risk of sedation and respiratory depression when used with midazolam or triazolam. Increased risk of acute ergot toxicity when used with ergotamine, dihydroergotamine, ergonovine or methyergonovine. Concurrent usage with cisapride or pimozide may lead to serious cardiac arrhythmias. Concurrent usage with indinavir may lead to increased hyperbilirubinaemia. Increased risk of viral resistance when used with PPIs, rifampin. Increased risk of irinotecan toxicity when used together.
See Below for More atazanavir Drug Interactions
Food Interactions
 Increased risk of viral resistance when coadministered with St John's wort.
Mechanism of Actions
 Atazanavir is a HIV-protease inhibitor with antiviral activity against HIV. It works by inhibiting HIV-1 protease, thus preventing cleavage of the gag-pol polyprotein resulting in immature, noninfectious virus. It is used in combination with other antiretrovirals for the treatment of HIV-1 infection.
Absorption: Rapidly absorbed with a Tmax of approx 2.5 hr. Steady-state is achieved within days 4 and 8.
Distribution: 86% bound to serum proteins. Binds to α-1-acid glycoprotein and albumin.
Metabolism: Extensively metabolised. Major biotransformation pathways: Monooxygenation and dioxygenation.
Excretion: Mean elimination half-life: Approx 7 hr at steady-state in healthy individual and HIV-infected patients after a daily single oral dose of 400 mg. Unchanged drug accounted for about 20% (faeces) and 7% (urine) of the administered dose.
Storage Conditions
 Oral: Store between 15-30°C.
ATC Classification
 J05AE08 - atazanavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.
Storage
 Oral: Store between 15-30°C.
Available As
  • Atazanavir 100 mg
  • Atazanavir 150 mg
  • Atazanavir 200 mg
  • Atazanavir 300 mg

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