TEST 2 Dose-Response Relationship Flashcards

1
Q

Define dose:

A

The amount of drug administered

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2
Q

Define response?

A

A change in biological activity.

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3
Q

Define Dose-response relationships?

A

The relationship between the amount of a drug administered and the observed change in a biological function.

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4
Q

What are the two response theories?

A

Occupation and Rate Theory

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5
Q

Describe Occupation Theory?

A

The magnitude of a response is proportional to the number of receptors occupied by a drug.

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6
Q

Describe Rate theory?

A

The magnitude of a response is proportional to the rate of formation of the D-R complex.

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7
Q

Define the Dissociation constant mathematically.

A

KD=K2/K1

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8
Q

Define Intrinsic Activity?

A

The ability of a drug to induce a biological response.

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9
Q

Define Efficacy?

A

Maximal effect produced by a drug

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10
Q

Define Potency?

A

Determined by the dose needed to produce a particular effect of given intensity

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11
Q

Define Agonist?

A

A drug which possesses affinity and intrinsic activity.

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12
Q

Define Partial Agonist?

A

An agonist with lower efficacy than a full agonist

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13
Q

Define Antagonist?

A

A drug which possesses affinity but little or no intrinsic activity.

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14
Q

Define Specificity?

A

Ability of a drug to exert its effect through a single mechanism of action

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15
Q

Define Selectivity?

A

Ability of a drug to induce one effect in preference to another effect.

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16
Q

What type of graph does an Competitive antagonist create?

A

Logarithmic curve

17
Q

What effect does a competitive antagonist have on the agonist effect graph.

A

Moves the curve to the left.

18
Q

What type of graph does an Non-competitive antagonist create?

A

Logarithmic curves

19
Q

What effect does a competitive antagonist have on the agonist effect graph?

A

Lowers peak % maximal effect

20
Q

What effect on the agonist do different antagonists have on a double reciprocal plot.

A
  • Non-competitive antagonist:
    • x-intercept doesn’t change
    • y-intercept moves up.
  • Competitive antagonist
    • x-intercept moves right.
    • y-intercept doesn’t move.
21
Q

Define Median Effective Dose (ED50)

A

Dose required to produce specific therapeutic effect in 50% of test subjects.

22
Q

Define Lethal Dose (LD50)?

A

Dose required to produce death in 50% of test subjects.

23
Q

Define Median Toxic Dose (TD50)?

A

Dose required to produce a toxic effect in 50% of test subjects.

24
Q

Define Therapeutic ratio or index?

A

The LD50/ED50 ratio for a drug. The larger the ratio, the safer the drug.

25
Q

Define Certain Safety Factor?

A
  • The LD1/ED99 ratio for a drug.
    • If the ratio is:
      • <1, the two curves overlap
      • >1, little or no overlap.
26
Q

Define Standard safety margin?

A

(LD1-ED99)/ED99 X 100 =

Represents the percent that the ED99 must be increased to be lethal in 1% of the test subjects.

27
Q

What are the three decreased response relationships?

A

Tolerance, Tachyphylaxis, Resistance

28
Q

What are the three increased response relationships?

A

Additive effects, synergism, potentiation.

29
Q

Define Tolerance:

A

A decrease in efficacy with repeated drug administration.

30
Q

Define Tachyphylaxis

A

An acute form of tolerance due to rapid, repeated administration of a drug.

31
Q

Define Resistance:

A

A decreased or complete lack of responsiveness to drugs that normally inhibit or cause cell death.

32
Q

Define Additive effects:

A

The combination of two drugs induces an effect equal to the sum of the effects of the two drugs when administered individually.

33
Q

Define Synergism:

A

The combination of two drugs induces an effect which is greater than the sum of the effects of the two drugs when administered individually.

34
Q

Define Potentiation:

A

Administration of a drug with little or no efficacy enhances the biological shift to the left of the dose-response curve for the antagonist.