Agonists, Partial Agonists, Antagonists & Inverse Agonists Flashcards Preview

Apex 4 - 2 Pharmacodynamics (5) > Agonists, Partial Agonists, Antagonists & Inverse Agonists > Flashcards

Flashcards in Agonists, Partial Agonists, Antagonists & Inverse Agonists Deck (57)
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1

Click the curve that represents an antagonist.

Study on!!!

2

A drug that binds to a receptor follows the law of:

Mass action

3

A drug that binds to a receptor follows the law of mass action. There is a rate constant for drug -----.
 

Binding

4

A drug that binds to a receptor follows the law of mass action. There is a rate constant for drug binding and a rate constant for ----- from the receptor

Dissociation

5

[Drug] + {Receptor] =?

[Drug] + {Receptor] = [Drug-Receptor Coomplex]

6

7

Drugs may be classified based on their degree of efficacy

True

8

Drugs may be classified based on their degree of efficacy. Remember that efficacy is measured by the ----- of the dose-response curve.

height of the y-axis

9

A ----- binds to a receptor and turns on a specific cellular response

Full Agonist

10

A Full Agonist mimics an ----- ligand

Endogenous ligand

11

A Full Agonist instructs the receptor to produce its ----- response

Maximal response

12

Different Full agonist drugs may produce the same clinical effect, but each may require a different dose to do so. This is a difference in -----.

Potency

13

Continuous administration of an agonist may cause ----- regulation of the target  receptors

Down-regulation

14

Examples: ----- is a full agonist at the beta receptor

Norepinephrine

15

Other examples of full agonists:

Dopamine

Propofol

Alfentanil

16

A ----- binds to a receptor, but it is only capable of partially turning on a cellular response

Partial Agonist

17

A Partial Agonist is ----- efficacious than a full agonist

"less"

18

A partial agonist is also called an -----

Agonist-antagonist

19

Partial Agonist can block the effects of an agonist by ----- for binding sites

"competing"

20

Partial Agonist can block the effects of an agonist by competing for binding sites. For example, giving a partial opioid agonist to an opioid-addicted patient can precipitate -----.

Withdrawal

21

Example: ----- is a Partial Agonist that provides pain relief, but there is a ceiling to its efficacy

Nalbuphine

22

The ----- sits in the receptor and prevents an agonist from binding to it.

Antagonist

23

The Antagonist does not tell the cell to do anything

True

24

By definition, the Antagonist does not have efficacy

True

25

Continuous administration of an Antagonist may cause ----- regulation of the target receptors

Up-regulation

26

Competitive antagonism is

A. reversible

B. not reversible

Reversible

27

If a patient receives a competitive antagonist, the dose-response curve for the agonist shifts to the -----.

Right

28

----- the concentration of the agonist can overcome competitive antagonism

"Increasing"

29

Increasing the concentration of the agonist can overcome competitive antagonism. This allows the agonist can achieve the same -----

Efficacy

30

Increasing the concentration of the agonist can overcome competitive antagonism (the agonist can achieve the same efficacy), but it requires ----- to achieve the desired clinical effect.

More drug molecules