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Death Mask Lecture
PharmacoKinetics
44
Pharmacology
Professional
12/05/2013

Additional Pharmacology Flashcards

 


 

Cards

Term
MAOI's
Definition
phenelzine, tranylcypromine, isocarboxazid and selegiline
Term
Erythromycin and Seldane (terfenadine)
Definition
fatal-Torsades de pointes
Term
pharmacodynamic interactions
Definition
a drug interaction in which the physiologic effect of one drug is altered by another drug--no change in drug concentrations
Term
additive drug interactions
Definition
pharmacodynamic interaction that results in synergistic effect; morphine and benzo's--can be beneficial
Term
cimetadine and ketoconazole
Definition
lower pH of stomach, reduced absorption
Term
erythromycin and digoxin
Definition
killing of eubacterium lentum results in decreased degradation (metabolic capacity) of drug and increases serum concentration levels
Term
sulcralfate and ciprofloxacin
Definition
bind together and reduced absorption of antibiotic
Term
iron and tetracycline
Definition
bind together and reduced absorption of antibiotic--forms insoluble compound that is not absorbed
Term
troglitazone and food
Definition
increased bioavailability
Term
cimetidine and ETOH
Definition
increased bioavailability
Term
iron and tetracycline
Definition
bind together and reduced absorption of antibiotic--forms insoluble compound that is not absorbed
Term
troglitazone and food
Definition
increased bioavailability
Term
cimetidine and ETOH
Definition
increased bioavailability
Term
aspirin
Definition
displaces warfarin from albumin binding site
Term
valproic acid
Definition
displaces phenytoin from binding site, increasing phenytoin volume of distribution and reduces concentration
Term
phenytoin and renal failure
Definition
most likely toxin build up displaces drug from protein binding sites and increases Vd
Term
quinidine
Definition
displaces digoxin from tissue binding sites and increases Vd, increases rapidly
Term
probenacid
Definition
block tubular secretions of Methotrexate and increases serum concentrations for longer
Term
HCTZ
Definition
increases lithium levels due to changes in sodium levels
Term
cimetidine
Definition
blocks tubular secretion and metabolism of procainamide
Term
Cytrochrome P-450
Definition
heme containing, location--smooth ER of liver and intestinal tract, defense mechanism
Term
14 CYP families
Definition
CYP1, CYP2, CYP3 mediate most drug metabolisms, account for 70% of the liver content
Term
CYP 3A
Definition
subfamilies name denote by uppercase letters, 20-subfamilies and CYP3A4--individual enzyme designated by second Arabic numeral
Term
CYP450 enzymes-important in drug interactions and metab (90% of drugs)
Definition
1A2, 2C9, 2C19, 2D6, 3A4 and 3A5
Term
substrate and inhibitor of CYP3A4
Definition
erythromycin
Term
substrate and inhibitor of CYP2D6, but metabolized by CYP3A4
Definition
quinidine
Term
permanent inhibition of CYP
Definition
duration depends on t1/2 of isoenzyme; once inhibited a new enzyme must be synthesized
Term
erythromycin metabolized by CYP3A4 complexes with and permanently inhibits 3A4
Definition
metabolism of theophylline may be inhibited days after administration of erythromycin
Term
competitive inhibition
Definition
most common type of inhibition, begins with first dose, max SS and reversed after 5 t1/2 after discontinuation
Term
CYP induction
Definition
causes increase synthesis of that particular isoenzyme, increased metab of any substance through that same pathway
Term
phenobarbitol and rifampin
Definition
capable of inducing a host of enzymes
Term
CYP inhibition
Definition
most often responsible for life-threatening interactions; some drugs may inhibit many isoenzymes but most are isoenzyme specific
Term
carbamazepine
Definition
autoinducer which induces its own metabolism
Term
permanent inhibition of CYP
Definition
duration depends on t1/2 of isoenzyme; once inhibited a new enzyme must be synthesized
Term
erythromycin metabolized by CYP3A4 complexes with and permanently inhibits 3A4
Definition
metabolism of theophylline may be inhibited days after administration of erythromycin
Term
competitive inhibition
Definition
most common type of inhibition, begins with first dose, max SS and reversed after 5 t1/2 after discontinuation
Term
the time of onset and offset of increased activity is related to
Definition
plasma concentration and duration of its use of inducing drug, t1/2 of drug, t1/2 of turnover of the isoenzyme
Term
phenobarb
Definition
ezyme CYP2B6 and CYP3A4,5,7; t1/2: 50-10 hours; enzyme induction one week; reversal 2-6 weeks
Term
Rifampin
Definition
t1/2: 2-3 hours, enzyme induction in 2-3 days, reversal 1-3 weeks
Term
drug features associated with potential interactions
Definition
steep dose response curve, narrow therapeutic window, dose dependent rate of metabolism (phenytoin)
Term
the time of onset and offset of increased activity is related to
Definition
plasma concentration and duration of its use of inducing drug, t1/2 of drug, t1/2 of turnover of the isoenzyme
Term
birth control and rifampin
Definition
increased breakthrough bleeding or pregnancy
Term
ACE inhibitiors
Definition
hyperkalemia
Term
inflammation and infection
Definition
may increase warfarin alone
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