First Previous Next Last Index
First Pass Metabolism
 
Slide 9 of 22
 
Speaker notes: When a protease inhibitor or drug enters the body and is absorbed, it must overcome certain barriers:
P-glycoprotein is encountered in enterocytes:
  • this may be important for certain PIs which are actually effluxed back into the gastrointestinal tract.
Cytochrome P450 (CYP P450) is found in enterocytes as well as in large amounts in the liver:
  • first-pass metabolism by CYP P450 is important, and affects many drugs in the PI class.
  • CYP 3A4 is particularly implicated.
  • this first-pass effect and rapid hepatic clearance may reduce PI concentrations to below the viral IC50/IC95 by the end of the dosing interval.

top of the page

Copyright © 1999- The University of Liverpool.
All rights reserved. Site developed and maintained
by The University of Liverpool and
eMed-Media