1, Molecules and Receptors Flashcards
what is PHARMACODYNAMICS the STUDY OF
what a DRUG DOES TO the BODY
- BIOCHEMICAL and PHYSIOLOGICAL EFFECTS
& MECHANISMS of drug ACTION,
& the relationship between drug CONCENTRATION and EFFECT
at basic equilibrium, AGONIST-RECEPTOR COMPLEX CONC. [AR] is PROPORTIONAL to..
CONC. AGONIST (drug) [A]
and CONC. RECEPTOR [R]
[AR] =
[AR] = K affinity [A][R]
(affinity constant for A, ability of receptor to bind agonist)
K affinity =
[AR] / [A][R]
[A][R] =
[A] [R] = Ka [AR]
KA is DISSOCIATION CONSTANT for agonist
K a =
(dissociation constant)
[A] [R] / [AR]
what does HIGH AFFINITY mean for K a (dissociation constant)
LOW KA
KA = [A][R] / [AR]
high affinity means high [AR]
Y is the proportion of receptors occupied and 1 means all receptors are bound
what is the equation for Y
y=
y = 1
/ 1 + Ka/[A]
when does Ka = [A]
when y=0.5
a DOSE RESPONSE CURVE for an AGONIST is a … curve
HYPERBOLIC CURVE
(increases and curves off)
a LOG-DOSE RESPONSE CURVE for an AGONIST is a … curve
SIGMOIDAL CURVE
(s shape)
what can be measured directly from a LOG-CONCENTRATION RESPONSE CURVE
EC50
- CONC at 50% RESPONSE