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
monitor safety of new drug under actual conditions of use in large numbers of patients
post marketing surveillance - phase 4 new drug
treatments for basic drug poisoning
ammonium chloride
vit C
cranberry juice
treatments for acidic poisoning
sodium bicarb
acetazolanide
organic acid which acts on organic anion transporters and urate transporters in pct
competes with and inhibits uric acid reabsorption in pct
uric acid reabsorption is reduced and more will be excreted
probenecid
also inhibits penicillin secretion in PT
when penicillin secretion is reduced, more of the drug remains in body, prolonging its duration of action
aspirin inhibits uric acid secretion
probenecid
treatment for acetaminophen overdose
N acetyl cysteine
genetically predisposed people - with abnormal functioning pseudocholinesterase enzyme; not metabolized quickly; prolonged neuromuscular paralysis
succinylcholine
activates receptor to produce an effect of its own, but of a lesser level, in absence of full agonist
partial agonist
based on physical property of drug
physical antagonism
based chemical property resulting in an inactive property
chemical antagonism
two drugs can act on different receptors or by different mech. but counteract each others effect
physiological antagonism
when antagonist interferes with binding of the agonist with its receptor and inhibits generation of response
receptor antagonism
