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systems
drug metabolism
23
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Undergraduate 3
10/22/2011

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Term
factors that affect a drug's ADME
Definition
-solubility
-size
-route of administration
-functional groups
Term
drug characteristics that favor absorption
Definition
-uncharged
-nonpolar
-right pka and right ph
-low mw
-lipid soluble
Term
excretion
Definition
drug is eliminated unchanged in urine, bile, exhaled air, sweat, breast milk, and saliva
Term
biotransformation
Definition
drug is changed to facilitate elimination in urine and bile
Term
total clearance
Definition
removal of drug from plasma. sum of excretion and biotransformation.
Term
xenobiotics
Definition
drugs are foreign substances
Term
microsomal enzymes
Definition
CYPs, FMO
Term
non-microsomal enzyme
Definition
transferases, GSH conjugase, alcohol/aldehyde dehydrogenase, hydrolytic enzymes, and other oxidative enzymes
Term
family of CYP450
Definition
>40% of the same amino acids
Term
subfamily of cyp450
Definition
> 60% of same amino acids
Term
isoform of cyp450
Definition
members of a subfamily that each have 60% of the same amino acids
Term
induce 1A2
Definition
phenobarbital, rifampin, tobacco
Term
induce 2C9
Definition
rifampin
Term
induce 2C19
Definition
rifampin
Term
induce 2D6
Definition
rifampin
Term
induce 2E1
Definition
ethanol
Term
induce 3A4
Definition
barbituates, rifampin, st. john's wort
Term
inhibit 1A2
Definition
cimetidine
Term
inhibit 2C9
Definition
fluconazole, ketoconazole
Term
inhibit 2C19
Definition
cimetidine, ketoconazole
Term
inhibit 2D6
Definition
cimetidine
Term
inhibit 2E1
Definition
disulfiram
Term
inhibit 3A4
Definition
ketoconazole, itraconazole, fluconazole, cimetidine, grapefruit juice
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