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Pharmacology General 5145fbc1

False about protease inhibitors in HIV is -

A
They are powerful enzyme inhibitors
B
Of all the protease inhibitors saquinavir is the most powerful inhibitor of CYP3A4
C
They cause hepatotoxicity
D
All protease inhibitors are substrates for P glycoprotein coded by MDR gene.
High-Yield Explanation
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.

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