Pharmacodynamics DSA - 8/2 Konorev

Question 1

List the non-covalent bonds in order from strongest to weakest

Answer 1

Ionic
Hydrogen
Hydrophobic interactions
Van der Waals

Question 2

How is a concentration-effect curve normally graphed?

What shape do you get?

Answer 2

Logarithm

Sigmoidal

Question 3

What type of plot will give you a hyperbolic curve?

Answer 3

Arithmetic

Question 4

What parameters describe the interaction of a drug with its receptor?

Answer 4

Affinity
Selectivity
Intrinsic activity

Question 5

A low Kd means what about the affinity of the drug for the receptor?

Answer 5

High affinity

Question 6

Do agonists or antagonists have intrinsic activity?

What do they change?

Answer 6

Agonists

Receptor function to produce a physiological response

Question 7

What decreases receptor signaling and the response at receptors with a significant level of constitutive receptor activity?

Answer 7

Inverse agonists

Question 8

Is Emax lower or higher in partial agonists compared to full?

Answer 8

Lower

Question 9

What are the 3 types of antagonists?

Answer 9

Pharmacological
Chemical
Physiologic

Question 10

What type of antagonism occurs between endogenous pathways regulated by different receptors?

Answer 10

Physiologic

Question 11

If the Agonist Emax decreases but EC50 does not change, what interaction is occurring?

Answer 11

Noncompetitive antagonism

Question 12

If the Agonist EC50 increases but the Emax does not change, what interaction is occurring?

Answer 12

Competitive antagonism

Question 13

What is the best way to control adverse side effects?

Answer 13

Avoid systemic administration

Question 14

What is efficacy related to?

Drugs with what have a higher efficacy?

Answer 14

Total # of receptors available to bind a drug (Bmax)

Higher Bmax

Question 15

What represents drug potency?

High or low means more potent?

Answer 15

ED50

Low

Question 16

What describes the efficacy of a drug?

High or low is more efficacious?

Answer 16

Emax

High

Question 17

How do you measure drug safety?

Answer 17

Therapeutic Index (TI)

Question 18

TI equation?

Safer drug has high or low TI?

Answer 18

TD50 / ED50

High

Question 19

What questions do graded response curves answer?

Represents what?

Answer 19

How much

Mean value within a population or a single subject

Question 20

What question does a quantal response curve answer?

Used to examine what?

Answer 20

Does the response occur or not and how many

Frequency of a response in a large population

Question 21

What is lower in partial agonists compared to full agonists?

Answer 21

Emax, produces sub-max pharmacological effect at full receptor capacity

Question 22

What kind of interaction occurs when an antagonist makes the other drug unavailable?

Answer 22

Chemical antagonism (does not interact with the receptor)

Question 23

What does the following describe: antagonism (action at the same receptor as endogenous ligands or agonist drugs)

Answer 23

Pharmacologic (receptor)

Question 24

What phase II enzyme polymorphism results in increased irinotecan toxicity?

Answer 24

UGT1A1

Question 25

SNP of ADRB1 (beta1 adrenoreceptor) results in what?

Answer 25

Increased efficacy of metoprolol

Question 26

Potency primarily relates to what?

Efficacy?

Answer 26

Drug dose

Total # of receptors (Maximum effect)

Question 27

Is the Kd higher or lower for a more potent drug?

What else does this mean?

Answer 27

Lower

Higher affinity for a receptor

Question 28

What can be determined from plotting frequency distribution of subjects against drug dose?

Answer 28

Median effective dose

Question 29

What provides information about the variability in sensitivity to a drug w/in a population?

Answer 29

Quantal dose-response curve

Question 30

What describes how readily and tightly that drugs bind to their receptor?

Answer 30

Affinity

Question 31

What is equation for Kd?

Answer 31

Kd = [L][R] / [LR]

Question 32

What will decrease receptor signaling, decrease response at receptors with a significant level of constitutive receptor activity?

Answer 32

Inverse agonist

Question 33

What is present with inverse agonists?

What fx?

Answer 33

Intrinsic activity

Inhibition of receptor function

Question 34

What shape is the non cumulative frequency quantal dose response curve?

What can you find from it?

Answer 34

Bell shape

Median effective dose