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PHARMACOLOGY I > L4-5: Pharmacodynamics > Flashcards

L4-5: Pharmacodynamics Flashcards

1
Q

the duration of drug action is directly related to …..?

A

the time that the drug is bound to receptor

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2
Q

As the drug is _________ its action will be terminated

A

cleared from the bloodstream

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3
Q

drugs like corticosteroids act on _________ and alter the expression of specific ______

A

nuclear receptors, genes

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4
Q

MAO inhibitors, omeprazole, aspirin and DFP all ________ bind to and inhibit enzymes, causing their effects to last much longer than the free drug

A

irreversibly

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5
Q

how do drugs interact w/ ligand gated channels

A
  • receptor is linked to an ion channel
  • binding of NT or drug opens channel
  • influx of ion depolarized (Na, Ca) or hyperpolarizes (Cl-) the cell
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6
Q

what type of receptors does Acetylcholine, GABA, Benzodiazepines and Glutamate have

A

ligand gated ion channels

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7
Q

the nicotinic ACh receptor is ________, it depolarizes the cell

A

excitatory

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8
Q

the GABA receptor is_______, it hyperpolarizes the cell

A

inhibitory

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9
Q

G-proteins stimulate binding and hydrolysis of _____ to _____ in response to binding of agonist to the receptor

A

GTP –> GDP
stimulation of G proteins amplifies the response caused by the bidning of the agonist

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10
Q

corticosteroids, mineralcorticoids, sex steroids, vit D and thyroid hormone are all waht types of receptors

A

intracellular

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11
Q

explain how corticosteroids are an exception to the rule that for most drugs - the duraction of action is directly related to the time the drug is bound to the receptor

A

corticosteroids act on nuclear receptors and alter gene expression. Altered gene expression can result for weeks even after the drug has been cleared from the body

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12
Q

explain how MAO inhibitors, omeprazole, aspirin and DFP are an exception to the rule that for most drugs - the duraction of action is directly related to the time the drug is bound to the receptor

A

these drugs irreversibly bind to and inhibit enzymes, their effects persist much longer than the free drug in plasma

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13
Q

the enzymes: tyrosine kinase, serine kinase and guanylyl cyalse are all enzymes that bind to ___________ regulated transmembrane proteins

A

allosterically regulated

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14
Q

allosterically regulated transmembrane proteins are polypeptides with a ________ binding domain and a ________ enzyme domain

A

extracellular hormone binding domain
cytoplasmic enzyme domain

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15
Q

ligand binding to allosterically regulated transmembrane proteins causes receptors to associate, stimulating _________

A

tyrosine kinase

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16
Q

the stimulation of tyrosine kinase in allosterically regulated transmembrane proteins results in the _______ of receptors and other downstream proteins

A

phosphorylation

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17
Q

Acetylcholine, GABA, benzodiazepines and Glutamate all have what type of ion channels

A

ligand gated

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18
Q

insulin, epidermal growth factor and platelet derived growth factor all have what type of receptors

A

protein tyrosine kinase

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19
Q

what is the receptor for ACh

A

nicotinic, Na

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20
Q

what is the receptor for GABA

A

GABA A, Cl-

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21
Q

what is the receptor for Benzodiazepines?

A

GABA A, Cl-

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22
Q

what are the ions associated with a glutamate receptor

A

Ca, Na

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23
Q

G proteins stimulate binding and hydrolysis of _____ to _____ in response to binding of agonist to receptor

A

GTP to GDP

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24
Q

stimulation of G proteins _______ the response to binding of agonist to the receptor

A

amplifies

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25
Q

receptors linked to G_ Stimulate the formation of cAMP

A

Gs

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26
Q

receptors linked to G_ inhibit formation of cAMP

A

Gi

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27
Q

what convertys ATP to cAMP
what breaks cAMP down to 5’AMP

A

adenylyl cylase
**PDE **breaks it down

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28
Q

cAMP binds to intracellular _______ which facilitates ______ of various proteins

A

protein kinase A
phosphorylation

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29
Q

Gq activates….

A

membrane phospholipase C

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30
Q

what happens after Gq activates membrane phospholipase C

A

hydrolysis of PIP2 into IP3 and DAG

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31
Q

what is the role of IP3 in polyphosphoinositide signaling

A

releases Ca from intracellular stores

32
Q

what is the role of DAG in polyphosphoinositide signaling

A

stimulates protein kinase C

33
Q

Gq stimulates the formation of what

A

IP3 and DAG from PIP2

34
Q

drug response is directly related to the number of…

A

receptors occupied

35
Q

when is drug and receptor response at its maximum

A

when all available receptor sites are occupied or bound to the drug

36
Q

once all receptors are bound with drug, is there any effect of further addition of the drug

A

no additional response

37
Q

quantal dose response curves relate the _______ of a drug to the _______ with which a designated response will occur within a population

A

dosages
frequency

38
Q

what is the therapeutic ratio

A

LD50/ED50

39
Q

is a drug with a large or small therapeutic window ‘safer’

A

larger theraeutic window

40
Q

______ measures the binding of drug to receptor

A

affinity

41
Q

what is the concentration needed to produce half max binding called

A

Kd

42
Q

what is the degree of biological response produced by the bidning of a particular drug to a receptor

A

efficacy

not related to potency

43
Q

intrinsic activity is the ability of a drug to ….. and is synonymous with efficacy

A

initiate a response

44
Q

agonists have _____ and ______ activity

A

affinity and intrinsic

45
Q

antagonists have affinity but no _______ activity

A

intrinsic

46
Q

partial agonists (or antagonists) have affinity but lower ____ activity

A

intrinsic

47
Q

a _______ binds to the receptor and initiates a response, causes a max shift of receptors to the activated state

A

agonist

ex: morphine

48
Q

a ______ binds to the receptor but does NOT initiate a response

A

antagonist
blocks response to an agonist

ex: Naloxone

49
Q

binds to the receptor and causes a response that is less that what would be produced by full agonist

A

partial agonist

ex: Buprenophine

50
Q

_______ antagonists bind to receptor and compete w/ agonist

A

competitive

51
Q

______ antagonists take receptors out of play

A

non competitive

52
Q

______ antagonists produce opposing physiological effects

A

functional (physiological)

53
Q

_______ antagonists have no intrinsic activity (no efficacy)

A

competitive

54
Q

if agonist concentration is high enough, the effect of the __________ antagonist can be overcome

A

competitive

55
Q

do competitive antagonists affect max response produced by agonist

A

NO

56
Q

competitive antagonists shift the dose response curve to the ______

A

right

57
Q

what is the effect of competitive antagonists on affinity

A

decrease it
(decreased Kd or EC50)

58
Q

what type of antagonism is this

A

competitive

59
Q

what is the effect of non-competitive antagonists on maximum response

A

decrease it

60
Q

what type of antagonism is this

A

non competitive

61
Q

what type of antagonism is this:
Epi reverses drop in bp caused by histamine in anaphylaxis

A

functional / physiological

62
Q

type of antagonist that neutralizes a drug chemically

A

chemical antagonism

63
Q

what type of antagonism is this:
herapin being neutralized by protamine

A

chemical

64
Q

if ______ agonists are combined with full agonists, they will compete for the recetpor but produce a ________ response

A

partial
smaller

65
Q

what type of agonist is this

A

partial

66
Q

tolerance is the…

A

chronic administration of many drugs

67
Q

what are the 2 types of tolerance

A

pharmacokinetic
pharmacodynamic

68
Q

type of tolerance where the drug induces its own metabolism and may also increase metabolism of another drug

ex: barbiturates

A

pharmacokinetic tolerance
Metabolic

69
Q

type of tolerance caused by the down or up regulation of a drug; includes beta receptor agonsits or antagonists

ex: opioids

A

pharmacodynamic tolerance
changes in the target tissue that makes them less sensitive to a given drug [ ]

70
Q

T/F:drugs are at most ‘selective’, and rarely ‘specific’

A

T

71
Q

what is dose dependent toxicity

A

an adverse reaction is mediated by the same receptor effector mechanism

ex: excessive sedation by sedative agent…overextension of the therapeutic effect

72
Q

what are some examples of dose dependent toxicities

A
  • excessive hypotension
  • arrhythmias
  • hypoglycemia
  • hemorrhage
73
Q

aminoglycosides cause what toxicity

A

reanl and ototoxicity

74
Q

acetaminophen causes what toxicity

A

hepatotoxicity

75
Q

chloramphenicol causes what type of toxicity

A

aplastic anemia

76
Q

tetracycline causes what kind of toxicity

A

retardation of bone growth

77
Q
A

PHARMACOLOGY I (21 decks)

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