Mechanism of PGP transport

CAPILLARY

LUMEN

BRAIN (ECF)

or CSF

Tight junctions

Endothelium

PI

PI

PI

Blocked by modulator

PGP

PGP

PI

passive diffusion

active transport

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• P-glycoprotein (P-gp) can actively transport drug from cells, resulting in:
  • decreased drug absorption (gastrointestinal tract)
  • enhanced elimination into bile (liver) and urine (kidney)
  • prevention of drug entry into the central nervous system (blood-brain-barrier)