exam 3 Flashcards
cyps account for 70% of metabolism . whtat cyps are involved most inmeyabolism
VYP3A4/5, CYP 2D6, 2C19. 2B6
what organ plays the most role in metabolism
liver
0examples of prodrugs:
probenecid
codeine: ctyp 2d6 removes methyl group and yields morphine
contributer to unexpected metabolism
DDI/ food interactions
induces expression
natural variability
cyps that have genetic variation:
cyp2c9: decreased functional genee varient exists
cyp2c19: defective gene varient in 3-16% of individuals
cyp2d6: highly polymorphic
phase !! metabolism enzyme examples
NAT
COMT
TPMT
when should you watch for metabolism variability
regulates a majorroute of elimination
yields pharmacologically active metabolites
the drup has a narrow TI
role of membrane transporters:
move nutrients or metabolites/ toxins across membranes
three sides of membrane
basolateral membrane: access to organs, often facing blood
intracellular membrane:
apical membrane
influx
movement of ions into cells
efflux:
movement of ions out of cell
OASTPs
OATP1. mediates hepatic uptake of drugs
influx transporters examples
OATP PEPT1 ASBT MCT1 oct2
efflux transporters examples
BCRP
PGP
OATP1 and OATP2 function
mediate uptake into gut
clearance
total elimination of drug from body