Products
Atazanavir is commercially available in capsule form (Reyataz). It has been approved in many countries since 2004. Generic versions were registered in 2017.
Structure and properties
Atazanavir (C38H52N6O7, Mr = 704.9 g/mol) is present in drugs as atazanavir sulfate, a white to slightly yellow crystalline powder that is sparingly soluble in water.
Effects
Atazanavir (ATC J05AE08) has antiviral properties against HIV-1, with effects based on inhibition of HIV protease, which plays a central role in viral maturation and replication. Atazanavir has a half-life of approximately 12 hours.
Indications
For the treatment of HIV-1 infection (combination antiretroviral therapy).
Dosage
According to the SmPC. Capsules are taken once daily with a meal. Atazanavir is combined with a pharmacokinetic booster such as ritonavir or cobicistat. These are CYP inhibitors that reduce the metabolic breakdown of the drug.
Contraindications
- Hypersensitivity
- Hepatic insufficiency
- Combination with certain drugs
Full details of precautions and interactions can be found in the drug label.
Interactions
Atazanavir is a substrate of CYP3A4 and a weak substrate of P-glycoprotein. Drug-drug interactions are possible with CYP substrates, inhibitors, and inducers.
Adverse effects
The most common possible adverse effects include nausea, vomiting, jaundice, rash, headache, abdominal pain, sleep disturbances, peripheral neurologic symptoms, dizziness, muscle pain, diarrhea, depression, and fever.
