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pharmacology block 1 > lecture 4 > Flashcards

lecture 4 Flashcards

1
Q

efficacy

A

the ability of a drug to initiate and cellular effect

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2
Q

agonist

A

has affinity and efficacy, can be full or partial

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3
Q

antagonist

A

has affinity but no efficacy, can be non-competitive (irreversible) or competitive (reversible)

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4
Q

type of drugs that use intracellular receptors (4)

A

steroid hormones, thyroid hormone, vit d, vit a

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5
Q

drugs that use tyrosine kinase receptors (2)

A

insulin and EGF

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6
Q

MOA of JAK-STAT receptors

A

binding to receptor activates janus-kinase enzymes that go on to phosphorylate STAT molecules

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7
Q

drugs that bind to JAK-STAT receptors (3)

A

interferon, GH, EPO

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8
Q

3 basic components of G-protein coupled receptors

A

cell surface receptor
G protein
2nd messenger

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9
Q

Gas

A

activates adenylate cyclase to increase cAMP

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10
Q

Gi

A

inhibits adenylate cyclase to decrease cAMP

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11
Q

Gaq

A

activates PLC to increase IP3/DAG = increased Ca

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12
Q

Gt

A

activate cGMP diesterase to decrease cGMP

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13
Q

example of agonist that is an enzyme activator

A

nitroglycerin

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14
Q

example of a nuclear receptor antagonist

A

tamoxifen

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15
Q

example of non-receptor mediated enzyme action

A

streptokinase for thrombolysis

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16
Q

example of non-receptor mediated physical reactions

A

osmotic laxatives

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17
Q

example of non-receptor mediated chemical reactions

A

antacids

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18
Q

define potency

A

concentration of a drug needed to produce a particular effect

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19
Q

median effective dose

A

dose of drug needed to produce 50% max response

20
Q

median lethal dose

A

dose causing death in 50% of users

21
Q

therapeutic index equation

A

TI = LD50/ED50

22
Q

interpretation of TI

A

higher TI = safe drugs

23
Q

graded dose-respone curve

A

tracks percent of maximum response vs. dose

24
Q

quantal dose-response curve

A

tracks percent of subjects with response (all or nothing) vs. dose

25
Q

what receptors are affected with normal doses of caffeine?

A

adenosine receptors

26
Q

what are the effects of very high doses of caffeine?

A

inhibit GABA receptors, inhibit phosphodiesterase and cause release of Ca

27
Q

describe the development of the 3 types of tolerance

A

acute tolerance- tachyphylaxis (oxymetazoline)
pharmacodynamic tolerance - dec synthesis of receptors (morphine)
pharmacokinetic tolerance - increased synthesis of metabolic enzymes (carbamazepine)

28
Q

differences between the 2 isomers of warfarin

A

S-warfarin: 5x more active, metabolized by 2C9

R-warfarin: less active, metabolized by 1A2 and 3A4

29
Q

pharmacogenetics

A

study of genetic basis for variation in drug response

30
Q

pharmacogenomics

A

use of tools to assess multigenic determinants of drug response

31
Q

variant genes for CYP450 enzymes are characterized by:

A

little to no enzymatic activity

32
Q

ultrarapid metabolizer

A

multiple copies of wild type

33
Q

extensive metabolizer

A

homozygous for wild type

34
Q

intermediate metabolizer

A

heterozygous

35
Q

poor metabolizer

A

homozygous for variant

36
Q

for which CYP450 enzymes do these variations occur? (4)

A

1A2, 2C9, 2C19, 2D6

37
Q

7-10 % of whites are poor metabolizers for:

A

2D6

38
Q

18-23% of asians are poor metabolizers for:

A

2C19

39
Q

what drug is less effective in poor 2C19 metabolizers? why?

A

plavix, because it is a pro-drug and requires activation by 2C19 enzymes

40
Q

4 types of adverse reactions

A

1-hypersensitvity
2-toxic
3- ideosyncratic
4-alteration of biological or metabolic systems

41
Q

hypersensitivity reactions are ___ of dose

A

independent

42
Q

toxic reactions are ___ of dose

A

dependent

43
Q

ideosyncratic reactions are:

A

genetically based and hard to predict

44
Q

2 types of synergism

A

potentiation and summation

45
Q

define potentiation

A

effect of A and B together is greater than their summative effects

pharmacology block 1 (5 decks)

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