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Pharmacology. 7. Pharmacodynamic Principles. > Agonists and Antagonists. > Flashcards

Agonists and Antagonists. Flashcards

1
Q

Will a drug that is an agonist of a receptor have an affinity for that receptor?

A

Yes.

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2
Q

What happens when an agonist binds to a receptor?

A

It will elicit a response.

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3
Q

What determines the level of a receptors response following the binding of an agonist?

A

The efficacy of the drug.

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4
Q

Do agonists have affinity or efficacy for their receptors?

A

Both.

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5
Q

Will drugs that are antagonists have affinity for a receptor?

A

Yes.

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6
Q

Will drugs that are antagonists have efficacy for a receptor?

A

No, as they block the receptor and there will be no response.

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7
Q

Do antagonists have affinity or efficacy for their receptors?

A

Only affinity.

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8
Q

What effects will full agonists have on a receptor?

A

The maximum possible effect.

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9
Q

What effects will partial agonists have on a receptor?

A

They elicit a partial response.

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10
Q

Will partial agonists have a higher or lower efficacy than full agonists?

A

A lower efficacy.

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11
Q

Can drug A have a higher affinity than drug B, but a lower efficacy?

A

Yes.

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12
Q

If drug A has a higher affinity than drug B and a lower efficacy, what will be the difference in effect if we give the same dose?

A

We need less of drug A to get a maximum effect, but the maximum effect is not as high as that of drug B.

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13
Q

What effects will antagonists have on receptors?

A

Always no effect.

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14
Q

What is drug potency based on?

A

Its EC-50.

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15
Q

What are equipotent drugs?

A

Drugs that have the same potency.

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16
Q

What is the EC-50 of a drug?

A

50% of the drugs maximum response.

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17
Q

Will drugs with a low EC-50 have a high or low potency?

A

Drugs with a low EC-50 have a high potency.

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18
Q

Can drugs have the same potency, but different efficacies?

A

Yes.

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19
Q

Will high potency full agonists have a high or low EC 50?

A

A low EC-50.

20
Q

Will low potency full agonists have a high or low EC 50?

A

A high EC-50.

21
Q

Do we need less or more of a highly potent drug to achieve the same response as that of a less potent drug?

A

Less.

22
Q

Will weak agonists have strong or weak potency?

A

Weak potency.

23
Q

Will strong agonists have strong or weak potency?

A

High potency.

24
Q

How can we tell that a drug has a higher potency that another drug?

A

The EC-50 will be smaller.

25
Q

Will partial agonists be able to achieve a maximum effect?

A

No, only full agonists can do this.

26
Q

What will competitive agonists compete against to bind to an enzymes active site?

A

The enzymes normal substrate.

27
Q

What happens if an antagonist binds to an enzyme instead of its substrate?

A

It stops the enzyme from working properly.

28
Q

Will an enzymes substrate and its antagonist use the same binding site?

A

Yes.

29
Q

What will make it more likely that an enzyme will bind to its substrate instead of an antagonist?

A

If we increase the concentration of substrate then it is more likely that the enzyme will bind to the substrate.

However, if we increase the concentration of the inhibitor then it is more likely that the enzyme will bind to the inhibitor.

30
Q

How will non-competitive antagonists bind to enzymes?

A

They bind to a location of the enzyme that is not the active site.

31
Q

How will non-competitive antagonists affect enzymes?

A

Binding usually results in a conformational change in the enzyme.

32
Q

What happens after a non-competitive antagonist has bound to an enzyme and caused a conformational change in the enzyme?

A

The enzyme can no longer bind to its substrate and this results in the enzyme being useless.

33
Q

Will non-competitive antagonists do bind to the same site as the enzyme substrate?

A

No.

34
Q

How will increasing the amount of a competitive antagonist affect the graph curve for enzyme activity?

A

If we increase the antagonist for competitive inhibition then we decrease the amount of active enzymes and this means the curve shifts to the right.

35
Q

How will increasing the amount of an agonist affect the graph curve for enzyme activity?

A

It shifts the curve to the left.

36
Q

How will increasing the amount of a non-competitive antagonist affect enzyme activity?

A

The more we increase the antagonist, the greater the effect will be until there are no enzymes functioning.

37
Q

Is it possible to overcome the effects of a non-competitive agonist?

A

No.

38
Q

Inverse agonists have effects on what kind of receptors?

A

Active receptors.

39
Q

What effects will inverse agonists have on receptors?

A

They will keep a receptor active, but they will decrease its response.

40
Q

Will a receptor bound to an inverse agonist be more less active than it would be if it was not bound to any agonist?

A

Less active.

41
Q

What kind of agonists increase the activity of a receptor?

A

Partial and full agonists.

42
Q

What kind of agonists decrease the activity of a receptor?

A

Inverse agonists will decrease it.

43
Q

What about drug binding will lead to a better response?

A

The tighter the ligand binds to a receptor, the better the response will be.

44
Q

Can chiral drugs or enantiomers bind to a receptor?

A

No, only one form of the drug will bind to the receptor while the other will not.

45
Q

How will using an agonist for a long time affect the amount of drug receptors?

A

Prolonged use of agonists can lead to the down regulation of receptors.

46
Q

How will using an antagonist for a long time affect the amount of drug receptors?

A

It leads to up-regulation of receptors.

Pharmacology. 7. Pharmacodynamic Principles. (3 decks)

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