Shelf: Drug Metabolism
Terms
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- oxidation
- phase I
- reduction
- phase I
- hydroxylation
- phase I
- dealkylation
- phase I
- deamination
- phase I
- desulfuration
- phase I
- dechlorination
- phase I
- hydrolysis
- phase I
- glucoronidation
- phase II
- sulfation
- phase II
- acetylation
- phase II
- glutathione conjugation
- phase II
- methylation
- phase II
- glycine conjugation
- phase II
- major site of drug metabolism
- liver
- CYP3A4 location
- intestinal epithelium
- alcohol dehydrogenase location
- stomach
- 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
- 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
- carbamazepine and clomipramine
- grapefruit juice
- p-glycoprotein
- MDR protein- export drug out of cells