False about protease inhibitors in HIV is -
Ans. is 'b' i.e., Of all protease inhibitors saquinavir is the most powerful inhibitor of CYP3A4 "Saquinavir is a weak inhibitor of CYP3A4". About other options All protease inhibitors (especially ritonavir and lopinavir) are potent inhibitors of CYP3A4 - Ritonavir has the most pronounced inhibitory effect, while saquinavir has the least. o Most HIV protease inhibitors are substrates for P-glycoprotein drug transpoer (P-gp), which is an efflux pump encoded by the mdr 1 gene. Goodman & Gilman 1 lth/e 1297 Indinavir and atazanavir can cause indirect hyperbilirubinemias with ove jaundice.
They are powerful enzyme inhibitors
Of all the protease inhibitors saquinavir is the most powerful inhibitor of CYP3A4
They cause hepatotoxicity
All protease inhibitors are substrates for P glycoprotein coded by MDR gene.