Atazanavir

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[edit] BRAND NAMES

[edit] STRUCTURE

Atazanavir.jpg

[edit] MECHANISM OF ACTION

Atazanavir, is a protease inhibitor. It blocks an enzyme required for the proteolytic cleavage of the viral polyprotein precursors to the individual proteins found in infectious HIV. The cleavage of these viral polyproteins is essential for the maturation of infectious virus.
Atazanavir binds to the active site of HIV protease and prevents cleavage of the polyproteins, resulting in the formation of immature non-infectious viral particles.

Atazanavir, taken in combination with other antiviral medicines, reduces the amount of HIV in the blood and keeps it at a low level.
Atazanavir does not cure HIV infection or AIDS, but it may delay the damage to the immune system and the development of infections and diseases associated with AIDS.

Atazanavir is used with Ritonavir, another protease inhibitor that is used as a ‘booster’. Ritonavir inhibits CYP3A4, that normally metabolizes protease inhibitors, therfore, it slows down the rate at which Atazanavir is broken down, increasing its levels in the blood.

[edit] INDICATIONS

Atazanavir is indicated in combination with ritonavir and other antiretroviral agents, to treat patients aged six years and over who are infected with human immunodeficiency virus type 1 (HIV-1), a virus that causes acquired immune deficiency syndrome (AIDS)

[edit] DOSAGE

  • Adults (aged 18 years or over): the recommended dose is 300 mg once a day with ritonavir 100 mg once daily with food.
  • Pediatric patients (6 to less than 18 years of age): the dose depends on body weight. There is no suitable dose for patients weighing less than 15 kg. Each dose must be taken with 100 mg ritonavir and food.
    • 15 to less than 20 kg: 150 mg of Atazanavir + 100 mg of Ritonavir
    • 20 to less than 40 kg: 200 mg of Atazanavir + 100 mg of Ritonavir
    • at least 40 kg: 300 mg of Atazanavir + 100 mg of Ritonavir

[edit] CONTRAINDICATIONS

[edit] WARNINGS AND PRECAUTIONS

  • Cardiac conduction abnormalities: PR interval prolongation may occur in some patients. Use with caution in patients with preexisting conduction system disease or when administered with other drugs that may prolong the PR interval
  • Rash: Discontinue if severe rash develops.
  • Hyperbilirubinemia: Most patients experience asymptomatic increases in indirect bilirubin, which is reversible upon discontinuation. Do not dose reduce. If a concomitant transaminase increase occurs, evaluate for alternative etiologies.
  • Hepatotoxicity: Atazanavir should be used with caution in patients with hepatic impairment (5.5). Patients with hepatitis B or C infection are at risk of increased transaminases or hepatic decompensation. Monitor hepatic laboratory tests prior to therapy and during treatment.
  • Nephrolithiasis and cholelithiasis have been reported. Consider temporary interruption or discontinuation.
  • Patients receiving Atazanavir may develop new onset or exacerbations of diabetes mellitus/hyperglycemia, immune reconstitution syndrome, and redistribution/accumulation of body fat.
  • Hemophilia: Spontaneous bleeding may occur and additional factor VIII may be required

[edit] INTERACTIONS

  • Coadministration of Atazanavir can alter the concentration of other drugs and other drugs may alter the concentration of atazanavir. The potential drug-drug interactions must be considered prior to and during therapy

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US)
  • Nursing Mothers: The Centers for Disease Control and Prevention recommend that HIV-infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV. It is not known whether atazanavir is present in human milk. Because of both the potential for HIV transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are taking Atazanavir

[edit] SIDE EFFECTS

Most common adverse reactions are nausea, jaundice, scleral icterus (yellowing of the eyes), rash, headache, abdominal pain, vomiting, insomnia, peripheral neurologic symptoms, dizziness, myalgia, diarrhea, depression, fever, lipodystrophy syndrome (changes in the distribution of body fat) and fatigue.

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[edit] BIBLIOGRAPHY

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