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25 Cards in this Set
- Front
- Back
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the degree of receptor occupancy multiplied by a certain number called intrinsic activity
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effect of a drug on a receptor
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EC50 or ED50
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Drug concentration
that produces 50% of maximum effect (of that drug) = potency |
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True or False.
Potency = KD |
false.potency
does not = KD it is =EC50 or ED50 |
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Tor F? If two or more drugs produce the same effect but differ in potency, the parallel S-curves suggest that the drugs have the same mechanism of action.
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true.The drug that has the lowest Ec50 is considered as the most potent drug even though the drugs under consideration have the same maximum effect(drug response)
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E max versus potencies
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Drugs Exhibit Unique Potencies for Inducing Effect despite having the same Emax.
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A more potent drug will have its Effect-Dose curve to the left of a less potent drug.
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True.
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The unit of intrinsic efficacy is moles/litre.
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NO!!
It is unit- less. |
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Two divisions of agonists based on their differences in their intrinsic efficacies
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full agonist
partial agonist |
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Characteristics of Noncompetitive Antagonism
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Produces a non-parallel shift in concentration-response curve of agonist
Full effect of agonist cannot be restored by increasing concentration of agonist |
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Mechanisms of Noncompetitive Antagonism
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Antagonist binds irreversibly to the agonist binding pocket
Allosteric Antagonism Antagonism of downstream response-generating machinery Physiological Antagonism |
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It is possible to identify which mechanism of non competitive antagonism accounts for an inhibition from dose response curves.
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false.Dose-response curves provide no information !
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---------- bind to the inactive state
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inverse agonists
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effect measured in an individual
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Graded-increases in graded fashion with increased dose
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an effect that is either present or absent
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Quantal
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Pharmacodynamic Variability
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The SLOPE of the cumulative frequency distribution
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TI is always a good predictor of safety
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False
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range between ED50 and start of TD50 curve
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Therapeutic Window
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Clinical efficacy can be achieved with having no intrinsic efficacy.T/F
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Correct!
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the combinrd effect is greater than the sum of two drugs
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Synergism
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the combined effect is equal to the sum of two drugs
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Additive
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represents a frequency of distribution(% of population responding to a drug
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Quantal dose-response curve
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Therapeutic effect
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The ratio of the concentration which is required to cause toxicity for 50 % of the population to the concentration which is required to cause 50 % of the maximum effect
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the ratio of the lethal dose to 1% of population to the effective dose to 99% of the population (LD1/ED99).
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The Certain Safety Factor
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toxicities that arise from inappropriate activation or inhibition of an intended drug target receptor
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on-target AE
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toxicities that arise from an unintended drug target receptor
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off-target AE
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