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17 Cards in this Set

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  • Back
Define EC_50
the potency of a drug is the concenratin oat which the drug elicits 50% of its maxiamal response
Define E_max
The efficacy is the amximal response produced by the drug
Define ED_50
the median effective dose: the dose that produces the effectiveness )therapeutic effect) in 50% of the population
Define TD_50
the median toxic dose: the dose that produces toxicity in 50% of the population
Define LD_50
the median lethal dose: the dose that produces death in 50% of the population
Define chemical antagonist
inactivate an agonist before it has the opportunity to act
Define physiologic antagonist
cuases a physiologic effect opposite ot that induced by the agonist
What does a competitive antagonist do to the agonist dose-response curve?
shifts it to the right
- decrease in potency, but same efficacy
How does Pravastatin work?
its part of the HMG CoA reductase inhibitor (statin) class.
it's a competitive inhibitor of HMG CoA
what does HMG CoA reductase do?
catalyszes reudction of HMG-CoA, the rate limiting step in cholesterol biosynthesis
where can noncompetitive antagonists bind?
- to the active site (irreversibly)
- to an allosteric site
How do you distinguish between competitive and noncompetitive antagonists?
competitive antagonists reduce potency; noncomp reduce agonist efficacy
give an example of a noncompetitive antagonist
aspirin. irreversibly acetylates cyclooxygenase (needed to generate thromboxane A2 in platelets)
give an example of a chemical antagonist
protamine. it's a protein that binds to the heparin class of anticoagulatins --> terminates heparin's effects
give an example of a physiologic antagonist
B-adrenergic blocking drugs to counteract the effects of hyperthyroidism
- prevent tachycardia
what is an inverse agonist?
abrogates the intrinsic stability of the bound receptor, or rather, stabilizing the receptor in the unbound form
define the therapeutic window
the range of doses of a drug that elicits a therapeutic response without unacceptable side effects