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27 Cards in this Set

  • Front
  • Back
receptor
macromolecule that interacts with drug, initiating biochem rxns leading to effect
ligand
binds to receptor, ie. drug (aka 1st messenger)
agonist
binds to receptor & MIMICS effect of endogenoid
antagonist
binds to receptor & BLOCKS binding of endogenoid
partial agonist
has less max response than true agonist
potency
QUANTITY of drug to produce desired effect
efficacy
MAX CAPACITY of drug to initiate response when bound
covalent receptor binding
prolonged, irreversible
noncovalent receptor binding
ionic, Hbonds, VDW, reversible
Desensitization
less response to same [drug] bc of continued stimulation, due to less receptors, mech for chronic tolerance
Supersensitivity
after chronic reduction of receptor stimulation, so rebound effect
competitive antagonism
direct competition for 1 binding site, reversible, higher [ ] wins
ex. atropine +Ach
Naloxone +morphine
Noncompetitive antagonism
antagonist works at diff site but can inactivate response of agonist, irreversible binding
ex. aspirin+cyclooxygenase
mecamylamine+nicotine
Chemical antagonism
direct chem interaction, agonist inactive, chelation
ex. heparin+protamimne
dimercaprol+mercury
Functional/physiological antagonism
2 agonist with opposing functions/mech
ex. prednisone+insulin
Ach+epinephrine (para vs. sympathetic)
metabolic antagonism
2nd compd reduces effects by increasing elimination
phenobarbital+oral anticoagulant
antibiotic+oral contraceptive
Additive effect
agonists have similar effect that combines to overall greater effect 1+1>2
gemtamicin+tobramycin
gemtamicin+furosemide
Potentiation
another compd that increases effect of 2nd compound
probenecid+penecillin
alcohol+barbiturate
Graded dose response
individual, %max response
Quantal dose response
population, %indvls responded
maximal asymptote
efficacy (up/down)
Potency controlled by
receptor density
efficacy of stimulation response of tissue
affinity
efficacy
more potent
takes less drug to have effect, curve to the left
competitive antagonist curve
shift to right
no change in max effect
surmountable by greater [ ]
max response can be achieved
noncompetitive antagonist curve
antagonist at different site can block agonist
not surmountable
can't achieve max response
Therapeutic dose
LD/ED =margin of safety
greater=safer
TI=40/20=2
2x therapeutic dose=toxic