pharmacodynamics dose-effect relationships

Question 1

dose-effect relationships allow the ability to predict the effects of changing the dose of a drug and facilitate comparisons between medications for the same ???

Answer 1

indication

Question 2

The magnitude of the response to a drug at ??? is proportional to the number of receptors occupied

Answer 2

equilibrium

Question 3

Equilibrium constant for association (K):
Rate of ??? reaction: k +1 [A][R]

Answer 3

Forward

Question 4

Equilibrium constant for association (K): Rate of ??? reaction: k -1 [A-R]

Answer 4

Reverse

Question 5

Equilibrium constant for association (K): Definition of chemical ???:
k +1 [A][R] = k -1 [A-R]

Answer 5

equilibrium

Question 6

Equilibrium constant for ??? (KA):
𝐾𝐴 = 𝑘−1 / 𝑘+1 = 𝐴 [𝑅] / [𝐴𝑅]

Answer 6

dissociation

Question 7

TRUE or FALSE: KA gives affinity of a drug for a receptor. Hence, the lower the KA, the higher the affinity of the drug for the receptor

Answer 7

TRUE

Question 8

receptor ??? occupancy model:
(𝑝𝐴) = [𝐴] / [𝐴] + 𝐾A

Answer 8

fractional

Question 9

a semi-log scale plot of the relationship between free agonist [A] and fractional occupancy (pA) is sigmoidal or hyperbolic?

Answer 9

sigmoidal

Question 10

Response =
??? Response x 𝑝𝐴 =
𝑀𝑎𝑥 𝑅𝑒𝑠𝑝𝑜𝑛𝑠𝑒 x 𝐴 / [𝐴] + 𝐾𝐴

Answer 10

Maximal response

Question 11

TRUE or FALSE: The relationship between agonist [A] and response (effect), KA is equivalent to the [A] that gives ½ maximum response ONLY in this model, where Response is proportional to ???

Answer 11

pA.
NOTE: In reality, response is often not directly proportional to fractional occupancy

Question 12

TRUE or FALSE:
½ maximal response:
Response = ½ Maximal Response when [A]free = KA

Answer 12

TRUE

Question 13

EC50 refers to the concentration of drug that causes ??? response

Answer 13

½ Maximal Response

Question 14

EC50 corresponds to the KA of Drug only if there is a ??? relationship between pA and the tissue response

Answer 14

linear

Question 15

The term ??? refers to the EC50 of a drug.
i.e. EC50 = Effective Concentration of agonist that produces 50% response

Answer 15

potency

Question 16

The relationship between agonist [A] and response (effect)
Response =
𝑚𝑎𝑥 𝑟𝑒𝑠𝑝𝑜𝑛𝑠𝑒 x [𝐴]𝑓𝑟𝑒𝑒 / [𝐴]𝑓𝑟𝑒𝑒 + 𝐸𝐶50