Konorev Into to Pharmacodynamics Flashcards
non-covalent bonds from strongest to weakest
ionic
hydrogen
hydrophobic
van der waals
dose response curve
x axis =
y axis =
what kind of curve
x = drug dose y = response
-hyperbolic curve
2 phases of dose response curve
linear and plateua
dose response curve using log
gives sigmoidal curve
what is Emax and what axis
maximal effect that can be produced by the drug
on Y axis
what is ED50
dose of the drug that produces 50% of its maximal effect
what is the affinity of a drug for receptor
how readily and tightly that drug binds to its receptor
KD is what
equilibrium dissociation constant
drug concentration at which 50% of drug receptor binding sites are occupied by the drug
the lower the Kd the ___ the affinity of drug for receptor
higher
the magnitude of a drug’s effect is proportional to
the degree of its interaction with (binding to) a receptor
what is EC50
concentration of drug that gives half max response
what factor decides if EC50 = Kd
depends on coupling of receptor occupancy and response to a drug
drug selectivity is
property of a drug determined by its affinities at various binding sites
-measure by comparing affinites of drug to diff receptors or by comparing ED50 for different effects of drug
intrinsic activity
ability of drug to change a receptor fnct and produce physiological response upon its binding to a receptor
agonist do or do not have intrinsic activity?
do
do inverse agonist have intrinsic activity
yes and it is related to the inhibition of receptor function
irreversibly bind to and occlude the agonist site on the receptor by forming covalent bonds
irreversible antagonist
noncompetitive antagonist and receptor inactivation
recereceptor inactivation is not surmountable
what are the 2 types of non-competitive antagonists
irreversible and allosteric
drug potency
describes amt of drug required to produce specific pharmacological effect
drugs with higher affinities for a receptor (lower kd) are more potent
efficacy
describes max pharmacological effect that a drug can produce
related to total number of receptors available to bind drug (Bmax)
higher Bmax = higher efficacy
the lower the ED50 the ___ the potency of a drug
higher
what response is represented by mean value within a population or single subject
graded response
quantal response
all or none, yes or no binary response
-does the response occur or not
in how many
non-cumulative quantal dose response curve
number or % of individuals responding at a dose of a drug only at that dose
cumulative quantal dose response curve
number or % of individuals responding at a dose of a drug and at all doses lower than that dose
therapeutic index
TD50 (median toxic dose)/ED50 (median effective dose)
higher TI = safer the drug
therapeutic window
range of doses of a drug or of its concentration in a bodily system that provides safe and effective therapy
