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25 Cards in this Set

  • Front
  • Back
the degree of receptor occupancy multiplied by a certain number called intrinsic activity
effect of a drug on a receptor
EC50 or ED50
Drug concentration
that produces 50%
of maximum effect (of that drug)
= potency
True or False.
= KD
does not = KD
it is =EC50 or ED50
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.
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)
E max versus potencies
Drugs Exhibit Unique Potencies for Inducing Effect despite having the same Emax.
A more potent drug will have its Effect-Dose curve to the left of a less potent drug.
The unit of intrinsic efficacy is moles/litre.
It is unit- less.
Two divisions of agonists based on their differences in their intrinsic efficacies
full agonist
partial agonist
Characteristics of Noncompetitive Antagonism
Produces a non-parallel shift in concentration-response curve of agonist

Full effect of agonist cannot be restored by increasing concentration of agonist
Mechanisms of Noncompetitive Antagonism
Antagonist binds irreversibly to the agonist binding pocket
Allosteric Antagonism
Antagonism of downstream response-generating machinery
Physiological Antagonism
It is possible to identify which mechanism of non competitive antagonism accounts for an inhibition from dose response curves.
false.Dose-response curves provide no information !
---------- bind to the inactive state
inverse agonists
effect measured in an individual
Graded-increases in graded fashion with increased dose
an effect that is either present or absent
Pharmacodynamic Variability
The SLOPE of the cumulative frequency distribution
TI is always a good predictor of safety
range between ED50 and start of TD50 curve
Therapeutic Window
Clinical efficacy can be achieved with having no intrinsic efficacy.T/F
the combinrd effect is greater than the sum of two drugs
the combined effect is equal to the sum of two drugs
represents a frequency of distribution(% of population responding to a drug
Quantal dose-response curve
Therapeutic effect
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
the ratio of the lethal dose to 1% of population to the effective dose to 99% of the population (LD1/ED99).
The Certain Safety Factor
toxicities that arise from inappropriate activation or inhibition of an intended drug target receptor
on-target AE
toxicities that arise from an unintended drug target receptor
off-target AE