An antiretroviral drug to treat HIV/AIDS taken by mouth.
It may be used for prevention after a needlestick injury or other potential exposure (postexposure prophylaxis).
It is generally recommended for use with other antiretrovirals.
It appears to be safe to use during pregnancy.
It is a protease inhibitor, that works by blocking HIV protease.
It is distinguished from other protease inhibitors in that it has lesser effects on lipid profile and appears to be less likely to cause lipodystrophy. There may be some cross-resistant with other protease inhibitors.
Lipodystrophy can cause a person to lose fat from some parts of the body, while gaining it in others, including on organs like the liver. It can be congenital and acquired.
Body fat or adipose tissue just underneath the skin keeps a person warm and provides protective cushioning, helping maintain healthy sugar levels in the blood, a complex metabolic process.
The affected person is unable to maintain fat tissue beneath the skin, that can lead to severe, life-threatening consequences over time.
(Common side effects)
• headache
• fever
• nausea
• jaundice
• abdominal pain
• insomnia
(Severe side effects)
• rashes such as erythema multiforme
• hyperglycemia
(Contraindication to diseases)
• previous hypersensitivity (e.g. Stevens-Johnson syndrome, erythema multiforme, toxic skin eruptions)
(Contraindication to drugs)
• alfuzosin
• rifampin
• irinotecan
• lurasidone
• pimozide
• triazolam
• orally administered midazolam
• ergot derivatives, cisapride
• Hypericum perforatum
• lovastatin
• simvastatin
• sildenafil
• indinavir
• nevirapine
It inhibits the UDP glucuronosyltransferase family 1 member A1 (UGT1A1).
UGT1A1 is the enzyme that detoxifies neurotoxic bilirubin by conjugating it with glucuronic acid. It also plays a critical role in the detoxification and excretion of endogenous and exogenous lipophilic compounds mainly in the liver and gastrointestinal tract. Its impaired or reduced activity causes unconjugated hyperbilirubinemia (Gilbert's syndrome and Crigler-Najjar syndrome) and side effects of drug treatment such as SN-38 (active metabolite of the anticancer drug irinotecan)-induced toxicity.
Cf. ritonavir, lopinavir
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