Metabolism of Drugs - Exam 3 Flashcards

1
Q

definition of metabolism of drugs

A

chemical alteration of the drug molecule by the cells of the animal

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2
Q

bioinactivation

A

detoxification, most common, parent drug -> inactivate

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3
Q

bioactivation

A

lethal synthesis, “prodrug” -> active drug

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4
Q

liver as a site of biotransformation

A

most common site, sER, hepatocyte cytoplasm, mitochondria, lysosomes, nuclear envelope, plasma membrane

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5
Q

other tissue sites of biotransformation

A

nervous tissue, kidney, GI epithelium, lungs, skin, plasma

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6
Q

example of active drug -> active metabolite

A

aspirin converted to salicylic acid

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7
Q

example of inactive drug -> active metabolite

A

cortisone -> cortisol

prenisone -> prednisolone

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8
Q

example of nontoxic drug -> toxic metabolite

A

parathion -> paroxon

ethylene glycol -> glyoxylic acid “lethal transformation”

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9
Q

antifreeze toxicity is an example of ________ ; includes what 2 toxic metabolites

A

biotransformation; glycoaldehyde & glycoxylate

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10
Q

microsomal enzymes

A

non-specific, large groupings of enzymes, cause oxidation, reduction, hydrolysis, & conjugation to glucuronic acid

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11
Q

T/F: enzymatic reactions are saturable

A

true

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12
Q

T/F: enzymes can inhibited or induced by drugs

A

true

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13
Q

Phase I reactions include

A

oxidation, reduction, hydrolysis; non-synthetic

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14
Q

Phase II reactions include

A

conjugation; synthetic

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15
Q

definition of oxidation

A

loss of one or more electrons by a substance, gain O2, remove H+; most common biotransformation reaction

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16
Q

definition of reduction

A

gain of one or more electrons by a substance, gain H+, remove O2

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17
Q

definition of hydrolysis

A

splitting of a molecule into fragments by the addition of H2O

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18
Q

microsomal oxidation phase I

A

sER

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19
Q

nonmicrosomal oxidation phase I

A

cytoplasm, mitochondria

20
Q

microsomal reduction phase I

A

reduction of chloramphenicol

21
Q

nonmicrosomal reduction phase I

A

aldehyde reduction of chloral hydrate

22
Q

lipid soluble drugs must go to phase ____ prior to excretion

23
Q

conjugation reactions phase II

A

combination of a drug or its metabolite with an endogenous substance

24
Q

conjugation is deficient in

A

neonates & cats

25
metabolite conjugates are usually
inactive, water soluble, and non toxic
26
most common & microsomal conjugation reaction
glucuronic acid (glucurodination)
27
cats are deficient in
glucuronyl transferases
28
dogs are deficient in
acetylating enzymes
29
ruminants have less
plasma pseudocholerestinase
30
ruminants and horses have high levels of
oxidative enzymes
31
pigs are deficient in
sulfate conjugating enzymes
32
birds lack
oxidative enzymes
33
first pass effect occurs with which type of drug administration
oral
34
hepatic first pass metabolism criteria
liver before systemic circulation metabolized by liver high hepatic extraction ratio
35
results of hepatic first pass metabolism
drug metabolized before distribution | decrease oral bioavailability
36
enzyme inducers
drugs that stimulate the liver to produce more metabolic enzymes
37
only what enzymes are inducible by drugs
microsomal
38
T/F enzyme induction is irreversible
false
39
examples of drug enzyme inducers
phenobarbital, phenylbutazone, griseofulvin, rifampin
40
enzyme inhibitors
drugs that inhibit liver production of metabolic enzymes
41
examples of drug enzyme inhibitors
chloramphenicol, cimetidine, ketoconazole
42
decreased distribution = decreased
metabolism because less drug can get to the liver
43
what tissue is common site for drug storage
adipose
44
drug storage in other tissues can lead to
re-distribution & delayed clinical effects
45
food enzyme inducer
charbroiled
46
food enzyme inhibitor
grapefruit juice
47
animals in the tropics may have less
biotransformation