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CYP families

PK

QuestionAnswer
CYP1 activation of procarcinogenic compounds substrates: caffeine, phenacetin inhibitor: furafylline
CYP2 important for drug metabolism
CYP2A6 metabolism of coumarin and nicotine (metabolite cotinine) effect on smoking behavior
CYP2B6 metabolism of anticancer drugs cyclophosphamide and ifosfamide
CYP2C9 principal CYP2C in liver substrates are weakly acidic (ex: NSAIDS, warfarin, tolbutamide, phenytoin) *2 and *3 have reduced catalytic activity
CYP2C19 91% identity with CYP2C9 substrates: anticonvulsant mephenytoin, omeprazole, andtiplatlet drug clopodogrel (plavix)
CYP2D6 mainly present in the liver metabolis of somme drugs requireing biometabolism, substrates: mostly basic, any CNS drugs (codiene, amitriptyline and haloperidol), debrisoquine (antihypertensive)
CYP2E1 ethanol is both an inducer and substrate industrial chemicals are substrates, many be activated to carcinogins
CYP3A4 major cyp in human liver responsiblile for metabolism of 50% of drugs major p450 in epithelial barrier of the small intestine
Created by: Kachmiel
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