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42 Cards in this Set
- Front
- Back
oxidation
|
phase I
|
|
reduction
|
phase I
|
|
hydroxylation
|
phase I
|
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dealkylation
|
phase I
|
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deamination
|
phase I
|
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desulfuration
|
phase I
|
|
dechlorination
|
phase I
|
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hydrolysis
|
phase I
|
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glucoronidation
|
phase II
|
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sulfation
|
phase II
|
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acetylation
|
phase II
|
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glutathione conjugation
|
phase II
|
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methylation
|
phase II
|
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glycine conjugation
|
phase II
|
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major site of drug metabolism
|
liver
|
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CYP3A4 location
|
intestinal epithelium
|
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alcohol dehydrogenase location
|
stomach
|
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other names for CYP
|
mixed function oxidases (MFO)
monoxygenases |
|
CYP450 requires...
|
reducing agent- NADPH
flavoprotein- NADPH CYP450 reductase |
|
CYP
2 d 6 |
super family
gene family (1-12) subfamily (a-z) gene |
|
parent drug binds to oxidized/reduced form of CYP450
|
oxidized (FE3+)
|
|
what happens to morphine when metabolized?
|
morphine-6-glucoronide = 100x more potent than morphine
and morphine-3-glucoronide = inactive |
|
what happens when minoxidil is metabolized?
|
minoxidil sulfate = active
|
|
phenytoin
|
CYP inducer
|
|
carbamazepine
|
cyp inducer
|
|
barbituates
|
cyp inducer
|
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rifampin
|
cyp inducer
|
|
ethanol
|
cyp inducer
|
|
griseofulvin
|
cyp inducer
|
|
st. john's wort
|
cyp inducer
|
|
aromatic hydrocarbons
|
cyp inducer
|
|
macrolide antibiotics
|
cyp inhibitor
|
|
triazole antifungals
|
cyp inhibitor
|
|
ritonavir (HIV protease inhibitor)
|
cyp inhibitor
|
|
fluoxetine
|
cyp inhibitor
|
|
nefazodone
|
cyp inhibitor
|
|
cimetidine
|
cyp inhibitor
|
|
-dipine's
|
grapefruit juice
|
|
-statins
|
grapefruit juice
|
|
cyclosporine
|
grapefruit juice
|
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carbamazepine and clomipramine
|
grapefruit juice
|
|
p-glycoprotein
|
MDR protein- export drug out of cells
|