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Saquinavir
- indication:For the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues.
- pharmacologypharmacology:
- mechanism: Saquinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
- toxicity: Probably experience pain in the throat
- absorprion: Absolute bioavailability averages 4%
- halflife:
- roouteelimination: In vitro studies using human liver microsomes have shown that the metabolism of saquinavir is cytochrome P450 mediated with the specific isoenzyme, CYP3A4, responsible for more than 90% of the hepatic metabolism. Only 1% of saquinavir is excreted in the urine, so the impact of renal impairment on saquinavir elimination should be minimal.
- volumedistribution: * 700 L
- clearance: * 1.14 L/h/kg [Healthy volunteers receiving IV doses of 6, 36, and 72 mg]