General Flashcards
Inducers
Anticonvulsants: phenytoin, barbiturates, carbamazepine Anti TB: rifampin glucocorticoids anti fungal: griseofulvin chronic alcoholism aromatic hydrocarbon - smoking St. Johns Wort
Inhibitors
Anti ulcer: cimetidine, omeprazole antibiotic: chloramphenicol, macrolides, ciprofloxacin, quinupristin/dalfopristin Anti TB: INH anti HIV: ritonavir anti fungal: ketoconazole anti convulsants: valproic acid amiodarone SSRI acute alcohol grapefruit juice
phase 2 reactions
glucuronidation acetylation glutathione methylation sulfate conjugation glycine conjugation
phase 1 reactions
oxidation reduction deamination dealkylation hydrolysis
steady state
4-5 half lives
increase number of receptors
up regulation
decrease number of receptors
down regulation
exposure of cells to agonists produces a cAMP mediated response; reduced cAMP mediated response is observed in the continued presence of agonists
desensitization
cells recover full responsiveness to a subsequent addition of agonists
resensitization - tachyphylaxis
if resensitization fails to occur, or occurs incompletely
tolerance
used to generate information regarding the margin of safety - therapeutic index
quantal dose
Ec50 is less than Kd, in a system with ______
spare receptors
effects of drug as function
healthy volunteers 25-50
safety and pharmacokinetics
phase 1 new drug
determine efficacy and safety volunteer 100 - 200 single blind design efficacy and broader range of toxicity phase A - dosing phase B - efficacy and toxicity
phase 2 new drug
volunteer 1000-10000 safety and efficacy double and third blind tech efficacy, safety, and toxicity studied phase A - prior to NDA phase B - after NDA but before approval
phase 3 new drug