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