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