03: Dose Response Relationship 3 Flashcards Preview

D2: 609 Pharm and Pain Control > 03: Dose Response Relationship 3 > Flashcards

Flashcards in 03: Dose Response Relationship 3 Deck (31):
1

In a graded drug response, how does dose relate to effect?

Dose is related to the INTENSITY of the effect

2

In a quantal drug response, how does the dose relate to the effect?

Dose is related to the FREQUENCY of the effect

3

How is a drug's quantal effect studied? (Single Biological Unit/Population Studies)

Population Studies

4

Is a graded drug response measured on a continuous scale or in an "all or none" pharmacological effect?

Continuous Scale

5

What does the term Potency mean in respect to drugs?

The amount of drug needed to produce a given effect

6

What quality of the drug molecule has the largest influence on its potency?

Its affinity for the target receptor

7

Is potency of great concern to clinicians?

Not really because the potency can be controlled through the dosage

8

How is potency expressed?

EC50 (uM)

ED50 (mg/kg)

9

This term describes the maximal effect that can be produced by a drug

Efficacy

10

Which molecules have the lower maximal effect? Partial Agonists or Full Agonists?

Partial agonists

11

What property of the drug has the largest influence on its efficacy?

The receptor-effector system

12

What is more important clinically, the drugs potency or its efficacy?

Efficacy

13

What is the difference between a Full Agonist and a Partial Agonist in terms of their ability to induce a conformational change in their target receptors?

A partial agonist can only induce some degree of receptor activation; but not enough to induce a maximal response

The full agonist leads to a conformational change that results in full activation of the receptor response

14

What does the shape of the D-R curve describe?

The drug binding to its receptors

15

What does the steepness of the curve indicate?

The useful dosage range

16

What aspect of the drug is the slope of the curve related to?

The toxicity

17

Are D-R curves with steep slopes more or less toxic?

More, because you get to the max with a smaller dose

18

Change in efficacy with or without changing the ED50

Non-competitive Antagonist

19

Change in ED50 without a change in Efficacy

Competitive Antagonist

20

How are toxicity of drugs compared?

By their ED50

21

The question, how many people got sick out of a group of 100 taking a drug? Would be an example of.....(Quantal/Graded)

Quantal

22

When can partial agonists be useful?

When you don't want to induce a maximal effect

23

Agonist that locks a receptor in an inactive state but produces the opposite of the "real" agonist's effect.

Inverse Agonist

24

Are antagonists and inverse agonists the same thing?

No. Antagonists just lock up the receptor, they do not produce an effect

25

What will the antagonist "block" from the receptor besides the agonist

Inverse agonists for that receptor as well

26

What is the difference between a competitive antagonist and a non competitive antagonist

Competitive agonists bind in the same site on the receptor

27

How can the effect of an antagonist be overcome?

Increasing the concentration of the agonist

28

What produces a shift to the right (delta ED50/affinity/potency) without changing the Emax/Efficacy

Competitive antagonists

29

With the introduction of a competitive antagonist, does the absolute affinity of the receptor change?

No, but you need to increase the dose of the agonist in order to get the same response; and therefore the relative affinity has been shifted to the right

30

What will depress the Emax and shift the entire curve to the right?

Non-competitive antagonist

31

The effect of what type of antagonist could be considered "taking receptors out of the pool"

Non-competitive antagonists