Term
| enzymes and transporter proteins |
|
Definition
responsible for normal metabolism
significant role in drug absorption in the GI tract and portal system (Ff and Fg) |
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|
Term
|
Definition
oxidase that converts endogenous and exogenous (drugs) substrates into more excretable molecules
super family of enzymes
in liver, GI, kidney, pancreas
responsible for phase I metabolism of >50% of medications |
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|
Term
| cyp450 enzyme family includes |
|
Definition
|
|
Term
|
Definition
primary subfamily enzyme in humans
in liver, GI, kidney, pancreas |
|
|
Term
|
Definition
liver: 30%
jejunum: 70%
high variable concentrations between people: 10 - 100 fold diff in liver and 30 fold diff in intestine |
|
|
Term
| P-glycoprotein (PGP) transporters |
|
Definition
plasma membrane glycoprotein belonging to an ATP-binding cassette (ABC) transporter superfamily
energy dependent drug efflux pump
promotes excretion of medications into bile, GI tract, or urine
limits transport of drugs across BBB |
|
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Term
|
Definition
| liver, small intestine, kidney, panacrease, brain, spleen, lung, adrenal gland, testes |
|
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Term
|
Definition
| its possible since cyp and pgp share substrates, location in tissues, and location in epithelial cells of tissue |
|
|
Term
| cyp3a and pgp concentrated in? |
|
Definition
| in many tissues including the intestines and liver |
|
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Term
| cyp3a enzymes _______ drug intestinal absorption by _______ drugs before the can be absorbed into the ______. |
|
Definition
decrease
metabolizing
portal circulation |
|
|
Term
| pgps _______ intestinal absorption by ______ drugs from the intracellular space back into the ______ |
|
Definition
decrease
pumping
intestinal lumen |
|
|
Term
| _______ bioavailability of drugs that are substrates for cyp enzymes and pgps |
|
Definition
|
|
Term
| first-pass metabolism (first-pass loss) Fh |
|
Definition
drug absorbed from GI into portal circulation
metabolized by the liver
fraction of drug does not reach systemic absorption |
|
|
Term
| the liver metabolizes some drugs thus _____ delivered to the ______ |
|
Definition
decreasing the amount
systemic circulation Fh |
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|
