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