Pharmacodynamics 2

Question 1

Why is binding not sufficient to produce response?

Answer 1

Need conformational change in the receptor to lead to activting of cellular signlaing

Question 2

Intrinsic ativity

Answer 2

ability of agonist to impart activating stimulus to a receptor

Question 3

Full vs/ partial agonists

Answer 3

Full have higher intrinsic activity

Question 4

As concentration of drug increases

Answer 4

There is dose dependent response until it reaches a maximum

Question 5

How is max effect reached

Answer 5

DOES NOT have to have all receptors occupied to produce maximal response from system

Question 6

Receptor reserve/spare receptors

Answer 6

Excess receptor population

Question 7

If occupancy and response a linear relationship?

Answer 7

No, can have fewer than 50% fo receptors occupied to produce 50% response

Question 8

Why is there a nonlinear response

Answer 8

Amplification of signaling pathways

Question 9

ED50

Answer 9

Dose at which 50% of the maximal effect is observed

Question 10

Potency

Answer 10

Concentration of a drug required to produce a given physiologic effect

Higher receptor affinity means higher potency

Question 11

Potency shift on a log dose graph

Answer 11

Lower potency to the right of the graph

Question 12

Efficacy

Answer 12

Maximal level of response a drug can produce

Efficacy of full agonists higher tha partial

Question 13

Efficacy on graph

Answer 13

Lower means lower max and shifted to the right