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Pharm Block 9 > Drug-receptor Interactions > Flashcards

Drug-receptor Interactions Flashcards

1
Q

Drug or ligand which binds to the same site as the endogenous ligand and produces the same signal

A

Agonist

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2
Q

Drug or ligand whihc binds to a different site than the endogenous agonist without producing a signal itself; this type of agonist enhances the response of endogenous agonists allosterically

A

Allosteric agonist

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3
Q

Drug which produces a lower response when at full receptor occupancy than do full agonists. By themselves, they evoke a response, but in the presence of an agonist, they act to competitively inhibit full agonist binding to the receptor

A

Partial agonist

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4
Q

Drug that binds to the receptor or components of the effector system used by the endogenous ligand and inhibits the action of the agonist; they initiate no effect on themselves

A

Antagonists

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5
Q

Typical of drugs that bind reversibly to the receptor, inhibition can be overcome by increasing the concentration of the agonist, ultimately achieving the same maximal effect

A

Competitive antagonist

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6
Q

Typical of drugs that bind irreversibly or allosterically to the receptor; this is a drug that prevents the agonist at any concentration from producing a maximum effect on a give recepto

A

Non-competitive antagonist

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7
Q

Agonist receptor

A

Same

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8
Q

Allosteric agonist receptor

A

Different site on the same receptor

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9
Q

Partial agonist receptor

A

Same

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10
Q

Antagonist receptor

A

Same

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11
Q

Agonist signal

A

Same

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12
Q

Allosteric agonist siglan

A

None by itself

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13
Q

Partial agonist signal

A

Same

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14
Q

Antagonists signal

A

None, just block

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15
Q

Agonist response

A

Same

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16
Q

Response of allosteric agonist

A

Greater than ag

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17
Q

Partial agonist response

A

Less than ag

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18
Q

Antagonists response

A

Less than Ag

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19
Q

Which drug-receptor interaction binds to a different spot than the agonist

A

Allosteric agonist. Binds to a different spot on the same receptor

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20
Q

Which two drug-receptor interactions have the same signal by themselves as the agonist

A

Agonist

Partial agonist

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21
Q

Which drug-receptor interactions have no signal by themselves

A

Allosteric a agonist

Antagonist

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22
Q

Which two drug-receptor interactions have a lesser response than the agonist

A

Partial agonist

Antagonist

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23
Q

Which drug-receptor interaction has a greater affect than agonist alone

A

Allosteric agonist

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24
Q

Which drug-receptor interaction has the same response when in the presence of an agonist

A

Agonist

25
Q

When looking at a graph plotting % max effect against log [agonsit], which type of drug-receptor interaction will not reach 100% max effect?

A

Partial agonist

26
Q

What can a partial agonist sometimes look like

A

An antagonist

27
Q

What does a %max effect vs log[A] curve look like when a competitive antagonist is added

A

It does not reduce the max effect, can give more agonists to overcome. Each curve should look the same on the graph

28
Q

What does a non competitive antagonist look like on the % max effect vs log [A] graph

A

The more antagonists that are added, the less steep the curve will get.

The most common type is irreversible. No binding sites for agonists to bind to and make up for.

29
Q

Enahances activity of agonists

A

Allosteric agonist

30
Q

Potentiates the agonist

A

Allosteric agonist

31
Q

What does it mean when there is a left shift on the % max effect vs log [A] curve

A

Potentiation by an allosteric agonist

Shifts curve in opposite direction as competitive antagonists

32
Q

Which direction will the curve shift in competitive antagonism

A

Right

33
Q

Which direction will the curve shift in noncompettive antagonism?

A

Down

34
Q

What happens to drug response when the dose increases

A

Generally as the dose increases, the response increases proportionally, however, as the dose increase the response increment diminishes until a dose is reached where no further increase in response can be achieved

35
Q

Example of dose-response relationships

A

Beta blocker to slow the heart down

  • 10mg, decrease HR by 10BPM
  • 20mg, decrease HR by 20 bpm
  • 40mg decrease HR by 30
  • 80mg decrease HR by 30

The most you want to give of this drug is 40mg

36
Q

What is the equation for looking at dose-response relationships and the max effect (efficacy)

A

E= (Emax x C)/(C+EC50)

Emax is the max response
EC50 is the cxn that produces 50% of the max effect

37
Q

What is the equation for looking at dose-response relationships in terms of receptor binding

A

B=Bmax x C/(C+Kd)

Bmax=total number of receptor sites
Kd=cxn of free drug at which 1/2 max binding is observed

38
Q

When the graph reads “drug effect” on the y axis, what value are we looking at half way up the curve?

A

EC50

39
Q

When we are looking at a graph with the y axis reads as “receptor bound drug”, what value are we getting half way up the curve

A

Kd

40
Q

When reading EC50, do you take the number off the Y axis or the X axis?

A

X

41
Q

When reading the Emax, do you read from the Y or the X axis

A

Y

42
Q

When reading Bmax, do you read from the Y or the X axis

A

Y

43
Q

When reading Kd, do you read from the Y or the X axis

A

X

44
Q

When can EC50 and Kd be identical

A

When bind half the receptors, you get half max response

45
Q

Refers to the concentration required to produce 50% of that drugs maximal response, refers to EC50

A

Potency

46
Q

Reflects the upper limit of the dose response relation on the response axis (max effect), associated with Emax

A

Efficacy

47
Q

Which is more important when choosing a drug, potency or efficacy

A

Efficacy. Care more about fixing the headache than how much drug you have to take.

48
Q

Between Emax and Kd, which is proabaky more important

A

Emax, efficacy is more important

49
Q

When looking at a response curve, how do you know the efficacy of a drug

A

By reading the Emax. If there is a partial agonist, the Emax will be lower

50
Q

What axis is associated with efficacy on the response curve

A

Y

51
Q

What axis is associated with potency on the response curve

A

X

52
Q

The curve that is the furthest _______ will be the most potent drug (on response graph)

A

Left

53
Q

The clinical effectiveness of a drug depends not on its __________ but on its ________ and its ability to reach relevant receptors

A

Potency (EC50)

Maximal efficacy

54
Q

When talking about therapeutic index on a graph, is a safer drug closer together or are the curves farther apart?

A

Father apart

55
Q

2 drugs, 1 receptors

A

Pharmacological antagonism

56
Q

Drugs may bind to and antagonize action of drug. 2 drugs, 0 receptors

A

Chemical antagonism

57
Q

Antagonist produces a physiological action that is opposite of agonsit and by a separate mechanism. 2 receptors, 2 drugs, the two receptors oppose each other

A

Physilogic antagonism

58
Q

Movement of a drug from the site of administration into the blood

A

Absoprtion

59
Q

Once in the blood, the drug moves to various parts of the body

A

Distribution

Pharm Block 9 (7 decks)

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