AD 2-----------—-----------------------------------------------EXAM2 Flashcards
Inc GI tract motility
Dec absorption
Metoclopramide-inc motility
Some metabolites can be toxic
Acetaminophen- hepatic injury
Meperidine- seizure
Some metabolites retain same activity
Fexofenadine
Some drugs must be converted to metabolites to be active
Produg
Enalapril-> must be hydrolyzed to enalaprilat (active)
Poor metabolizer
If not prodrug,
Inc efficacy, inc risk of ADR
Extensive metabolizer
Normal metabolizer
Poor metabolizer
If prodrug,
Dec efficacy, dec ADR
Rapid or ultra rapid metabolizer
If prodrug
Inc efficacy, inc AD
Phase I
Oxidation and reduction
ADR % (drug-drug interaction)
3-5%
Drug metabolism
Phase I
CYP1A2
Induced by tobacco
Inhibitor- quinolones, fluvoxamine, cimetidine
3A4. *****
Located in GUt, Liver
Not polymorphic
3A4 metabolizes majority of meds
Is inhibited by ketoconazole (antifungal), Cimetidine, grapefruit juice
Is induced by Rifampin(antimicrobiol)- induce metabolites, dec plasma concentra, dec efficacy
2C9
Warfarin- metabolized by 2C9
2C19
Anticonvulsants
Omeprazole can be metabolized by enzyme and inhibit this enzyme as well.
2D6
2nd most drug metabolizer
Cardiovascular, neurologic drugs
Codein (prodrug)-> morphine
Ultra-rapid metabolizers of CYP2D6 have inadequate responses to standard doses of B blockers, narcotic analgesics, or antidepressants. Require higher doses for clinical effectiveness