Module3: Drug metabolism and Transport Flashcards
what is the primary role of metabolism?
To make drugs more water soluble
where does most metabolism occur?
The liver
what does low metabolism lead to
Delayed elimination
saturable metabolism
Prodrug
what is drug metabolism dependent on?
Protein activity
CYP2D6
CYP2C19
TPMT
polymorphism
phase 1 reactions
phase 2 reactions
solute carriers
which transporters are solute carriers?
OATP, OAT, OCT, PEPT, MCT
which transporters are on the apical side?
OCT2 deficiency is protective (T/F)
True
basolateral
which transporters mediate uptake into enterocytes?
OATP1A2 and OATP2B1
apical
canicular
Most important CYP enzyme present in the liver and responsible for 40-50% of metabolism
Transport proteins that are present on the hepatocyte canicular membrane and are important for biliary elimination
major elimination pathway thats dependent on UGT
Glucoronidation
phase 2 reaction thats carried out by sulfotransferases
Sulfation