Review of Pharmacokinetics Flashcards
- unique pharmacokinetics of large molecules:
- ______ administration
- slow tissue distribution leading to ________ kinetics
- variable half lives, -mabs have long half life
- unique adverse effect profile
parenteral
multi compartment
for 2 drugs to be _______, Cmax, Tmax, and AUC must be equivalent
bioequivalen
strongly plasma protein bound drugs and very large drugs (heparin) distribute in?
plasma water (3 Liters in 70 kg man)
large water soluble drugs such as mannitol distribute in?
extracellular water (0.2 L/kg)
small water soluble drugs such as ethanol distribute in ?
TBW (0.6 L/kg)
drugs that avidly bind tissues such as chloroquine distribute in?
tissue concentration (>0.7 L/kg)
main enzyme for metabolism of 50-60% of current drugs? extensively expressed in GI cells and liver, often responsible for first pass
CYP3A4
phenobarbital, phenytoin, carbamezepine, rifampin enzyme induction?
CYP2C9, CYP2C19
glucocorticoids, anticonvulsants, rifampin, St Johns wort enzyme induction?
CYP3A4
isoniazid, chronic alcohol, carcinogenic nitrosamines enzyme induction? importnat for acetaminophen toxicity
CYP2E1
phenobarbital, primidone, phenytoin, carbamezepine, rifampic, polycyclic chemical, glucocorticoids, chornic alcoho and St Johns wort and key _______ of metabolism
inducers
cimetidine, erythromycin, ketoconazole, chloramphenicol, disulfiram, acute alcohol, and grapefruit juice are key _______ of metabolism
inhibitors
warfarin:
- deficiency of CYP2CP ______ biological effect
- mutation in VKORC1 ________ biological effect
increases
decreases
isoniazid for TB:
- ADR leads to ________
- gene: N-acetyltransferase
hepatotoxicity, neurotox
mercaptopurine for ALL:
- ADR hematological toxicity
- gene:
thiopurine S-methyltransferase
