Drug Transporters Flashcards
what is transporter redundancy
when transports have an overlapping number of substrates
what processes are involved in renal clearance
tubular active secretion
active reabsorption
effect of GI efflux transporters
reduced F
effect of GI uptake transporters
enable oral administration with actives or poor passive permeability
tubular reabsorption
can be passive
mediated by transporters
what is biliary excretion
transporters into bile tract may rate-control hepatic clearance
what is hepatic metabolism
transporters into hepatocytes may rate-control hepatic clearance
statins
liver is the sit of action and the sit of clearance
OATP1 facilitates hepatic uptake and low activity may decrease cholesterol lowering effect, increase plasma concentration and increase risk of muscle toxicity
factors that affect transporter expression
drugs, environmental chemicals, endogenous ligands (bile salts)
what are pharmacogenetics
genetic polymorphisms of transporter genes that may affect PK