Pharmacodynamics Flashcards

1
Q

What is the relationship between the drug dose and plasma concentration?

A

pharmacokinetics

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2
Q

What is the relationship between the effect site concentration and clinical effect?

A

pharmacodynamics

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3
Q

What theory unities kinetics and dynamics by examining plasma concentration and effect site concentration?

A

pharmacobiophasics

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4
Q

What affects pharmokinetics?

A

absorption, distribution, metabolism, and elimination

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5
Q

Vd, half lives, metabolism, enzyme induction and inhibition, clearance, steady state, context sensitive half life, degree of ionization, protein binding, ion trapping are all part of what pharmacology theory?

A

pharmacokinetics

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6
Q

Rate constants between the plasma and effect site make up what theory?

A

pharmacobiophysics

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7
Q

Potency, efficacy, dose response curve slope, agonist, antagonist, partial agonist, inverse agonist, ED50, LD50, therapeutic index and stereochemistry all make up what theory?

A

pharmacodynamics

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8
Q

What the body does to the drug?

A

pharmacokinetics

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9
Q

What the drug does to the body?

A

pharmacodynamics

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10
Q

What does slope on a dose response curve tell us?

A

how many receptors need to be occupied to elicit a clinical effect

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11
Q

What does a steep dose response curve tell us?

A

most receptors need to be occupied to create a response

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12
Q

What medications have a steep dose response curve?

A

inhaled anesthetics and NMB

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13
Q

What is potency on a dose response curve?

A

the dose required to achieve a clinical effect

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14
Q

What affects drug potency?

A

absorption, distribution, metabolism, elimination, and receptor affinity

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15
Q

What are two measures of potency?

A

ED50 and LD50

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16
Q

What does a left shift on the dose response curve indicate?

A

increased affinity for receptor-> increased potency, lower dose required for a clinical effect

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17
Q

What does a right shift on the dose response curve indicate?

A

decreased affinity for the receptor -> decreased potency, higher dose required for a clinical response

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18
Q

What is efficacy on a dose response curve?

A

a measure of the intrinsic ability of a drug to elicit a given clinical effect

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19
Q

What does the height on a dose response curve indicate?

A

efficacy

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20
Q

Once a drugs efficacy is reached what can occur if more drug is administered?

A

toxic levels, not additional effects

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21
Q

What type of agonist binds to a receptor and turns on a specific response?

A

full agonist

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22
Q

What does a full agonist tell the receptor to do?

A

produce its maximal response

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23
Q

Continuous administration of a full agonist causes up/down regulation of target receptors?

A

down regulation

24
Q

What type of agonist binds to a receptor but is only capable of partially turning on a cellular response?

A

partial agonist

25
Q

What is another name for a partial agonist?

A

agonist-antagonist

26
Q

What does a partial agonist do at receptor sites?

A

competes for receptor sites and blocks the agonist

26
Q

What kind of drug sits in the receptor and prevents the agonist from binding?

A

antagonist

27
Q

Does an antagonist have efficacy?

A

no

28
Q

Continuous infusion of an antagonist causes up/down regulation of target receptors?

A

up regulation

29
Q

What type of antagonist is reversible? Non reversible?

A

competitive antagonism is reversible

non-competitive antagonism is not reversible

30
Q

How does a competitive antagonist shift the dose response curve? What does this mean?

A

Right. increasing concentration of the agonist can overcome the antagonist, but it less potent.

31
Q

What is an example of a competitive antagonist?

A

Rocuronium and Ach receptors

32
Q

Describe non-competitive antagonism.

A

The drug binds to the receptor and does not unbind. New receptors must be made.

33
Q

How does a non-competitive antagonist shift the dose response curve?

A

down. like a partial agonist

34
Q

What is an example of a non-competitive antagonist

A

aspirin

35
Q

What is an inverse agonist?

A

binds to the receptor and causes the opposite effect as agonist. Negative efficacy

36
Q
Match the following. 
1+1=2.                  potentiation
1+1=3                   addition
1+0=3                  antagonism
1+1=0                   synergism
A

1+1=2 addition
1+1=3 synergism
1+0=3 potentiation
1+1=0 antagonism

37
Q

What term describes two drugs given at the same time?

A

addition

38
Q

What term describes two drugs given produce greater effect together?

A

synergism

39
Q

What term describes when one drug is enhanced by another with no effect on its own?

A

potentiation

40
Q

What term describes when one drug cancels the other?

A

antagonism

41
Q

What is ED50?

A

the dose produces the expected clinical response in 50% of the population.

42
Q

What is ED50 a measure of?

A

potentcy

43
Q

What is LD50?

A

the dose that produced death in 50% of the population

44
Q

What is therapeutic index and how is it calculated?

A

measure of drug safety. LD50/ED50

45
Q

Drug A has a therapeutic index of 10, Drug B has a therapeutic index of 50. Which drug is safer?

A

drug B

46
Q

What is chirality?

A

molecules with a center of 3 dimensional asymmetry. Carbon bound to 4 different atoms.

47
Q

What is enantiomerism?

A

chiral molecules that are non-superimposable mirror images of each other.

48
Q

How to dextrorotatory and levorotatory molecules rotate?

A

dextrorotatory: clockwise
levorotatory: counter-clockwise

49
Q

What drugs are enantiomers in clinical practice?

(Kids Today May Illegally Drink My Parents Beer Maybe Monday If Kept

A

ketamine, thiopental, methohexital, isoflurane, desflurane, mepivicaine, prilocaine, bupivicaine, morphine, methadone, ibuprofen, ketorolac

50
Q

What are racemic mixtures?

A

two enantiomers in equal amounts

51
Q

What are examples of racemic mixtures in practice?

A

levobupivicaine, ketamine

52
Q

What is special about ketamine?

A

it is a enantiomer and racemic mixture

53
Q

Label as antagonist, partial agonist, inverse agonist, full agonist

A
54
Q

What is the dose required to achieve a given clinical effect? Depicted on the x-axis

A

Potency

55
Q

What is the intrinsic ability of a drug to elicit a given clinical effect? Depicted on the y-axis?

A

efficacy