PHRM 835 Exam 2 Transporters Flashcards
three major drug transporters to know
-P-gp (P-glycoprotein)
-OATP (organic anion transporting protein)
-PEPT1 (peptide transporter 1)
example of efflux transporter
P-gp (P-glycoprotein)
example of uptake transporters (2)
-OATP (organic anion transporting protein)
-PEPT1 (peptide transporter 1)
P-gp is an efflux transporter affecting __________ of drugs
permeability
P-gp is also known as ?
MDR1 (multi-drug resistance 1)
true or false: inhibition of P-gp in cancer cells is expected to improve anticancer drug efficacy by increasing intracellular drug concentrations
true
P-gp is expressed on the ____ side of tissue
apical
P-gp substrate to know
Paclitaxel
most of the P-gp inhibitors are also substrates of P-gp and capable of _______ inhibiting P-gp function
competitively
true or false: inhibition of P-gp in brain is expected to increase the penetration of P-gp substrates into brain
true
(inc. conc of P-gp substrate into brain)
if you take loperamide with a P-gp inhibitor, would there be more or less metabolite in the brain than if taken without a P-gp inhibitor?
more
true or false: HIV-associated Neurocognitive Disorders occurs when HIV enters the nervous system and impacts the health of nerve cells. Combining HIV protease inhibitors (P-gp substrates) with P-gp inhibitors will likely increase the brain distribution of anti-HIV drugs
true
P-gp in the liver is expressed where?
at bile canaliculus
(bile canalicular membrane of the liver)
true or false: combining paclitaxel with a P-gp inhibitor will likely decrease biliary excretion of paclitaxel
true
(drug is biliary excreted)
true or false: biliary excretion of paclitaxel is its major elimination route. Combining paclitaxel with a P-gp inhibitor will likely decrease paclitaxel elimination from the body and increase systemic drug concentration
true
(leads to accumulation)
