Category: pharmacological
Aliases: Reyataz, ATV
HIV protease inhibitor — competitive inhibition of HIV-1 aspartyl protease blocks gag/gag-pol polyprotein cleavage and prevents production of mature virions. Almost always coadministered with a CYP3A4 booster (cobicistat or ritonavir) for adequate exposure. Distinctive among PIs for its inhibition of UGT1A1 — causes asymptomatic Gilbert-like unconjugated hyperbilirubinemia in most users (visible as scleral icterus at high exposure); not hepatotoxic, doesn't require discontinuation. Requires acid for absorption — clinically significant interaction with PPIs / H2 blockers / antacids. Otherwise generally well tolerated long-term. PK (Reyataz label, boosted 300/100 mg PO qd with RTV at SS): Cmax 6129 ng/mL, AUC(0-24) 57039 ng·h/mL, Tmax ~2.5 h, t½ 9-18 h boosted (7-8 h unboosted). Light meal ↑ AUC ~33% + Cmax ~40% (food taken with dose). CL/F ≈ 5.3 L/h, V/F ≈ 91 L.
PO: 12h