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9 of 22 |
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notes: When a protease inhibitor or drug enters the body and is
absorbed, it must overcome certain barriers: |
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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.
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