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Atazanavir

It is an antiretroviral medication used to treat and prevent HIV/AIDS. More

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Description

It is an antiretroviral medication used to treat and prevent HIV/AIDS.

Generic Name

Atazanavir

Chemical names

Atazanavir; Reyataz; Latazanavir; Zrivada

Brand names

Anzavir-R, Atazor, Synthivan, Virataz, Virataz-R

IUPAC name

methyl N-[(1S)-1-{[(2S,3S)-3-hydroxy-4-[(2S)-2-[(methoxycarbonyl)amino]-3,3-dimethyl-N'-{[4-(pyridin-2 yl)phenyl]methyl}butanehydrazido]-1-phenylbutan-2-yl]carbamoyl}-2,2 dimethylpropyl]carbamate

Pharmacokinetics

  • Absorption: Oral bioavailability is 60-68%.
  • Distribution: 86% protein bound
  • Metabolism: Liver
  • Excretion: 20% (faeces) and 7% (urine) 

Actions

It inhibits the Gag-Pol polyproteins and virus-specific processing of viral Gag in HIV-1 infected cells by binding to the active site of HIV-1 protease selectively, thus preventing the formation of mature virions. Atazanavir is not active against HIV-2.

Dosage/Dosage form

The recommended dose is 400 mg (Capsule)

Therapeutic uses

Treatment of HIV-1 infection

Adverse effects/Side effects

Stevens-Johnson syndrome and erythema multiforme. Nausea, vomiting, abdominal pain, darrhoea, taste disturbances, anorexia, flatulence, increased appetite, sleep disturbances, asthenia, fatigue, headache, dizziness, paraesthesia, hypoaesthesia, myalgia, arthralgia, alopecia, pruritus and renal insufficiency.

Interaction

  • May increase plasma concentrations of antiarrhythmics, diltiazem and hormonal contraceptives when used concurrently.
  • Plasma levels may be increased by azole antifungals.
  • May increase the metabolism of theophylline.
  • Coadmin with PDE5 inhibitor may lead to visual changes and priapism.
  • Concurrent usage with cisapride or pimozide may lead to serious cardiac arrhythmias. 
  • Increased risk of myopathy when used with lovastatin or simvastatin. 
  • Concurrent usage with indinavir may lead to increased hyperbilirubinaemia. 
  • Increased risk of sedation and respiratory depression when used with midazolam or triazolam. 
  • Increased risk of irinotecan toxicity when used together.
  • Increased risk of viral resistance when coadministered with St John's wort.

Contraindications

  • Hypersensitivity.
  • Lactation.

Storage

Store between 15-30°C

Information

Molecular weight

704.8555

Molecular formula

C38H52N6O7

CAS number

198904-31-3

Precautions

  • Avoid use in severe hepatic impairment.
  • Caution when used in patients with DM, haemophilia or history of cardiac conduction disorders.
  • Maintain adequate hydration.
  • May prolong PR interval on ECG. 
  • Monitor for signs of lipodystrophy.
  • Discontinue if acute haemolytic anaemia occurs.