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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
receptors linked to G_ Stimulate the formation of cAMP
G**s**
26
receptors linked to G_ inhibit formation of cAMP
G**i**
27
what convertys ATP to cAMP what breaks cAMP down to 5'AMP
**adenylyl cylase** **PDE **breaks it down
28
cAMP binds to intracellular _______ which facilitates ______ of various proteins
**protein kinase A** phosphorylation
29
Gq activates....
membrane phospholipase C
30
what happens after Gq activates membrane phospholipase C
hydrolysis of PIP2 into IP3 and DAG
31
what is the role of IP3 in polyphosphoinositide signaling
releases Ca from intracellular stores
32
what is the role of DAG in polyphosphoinositide signaling
stimulates protein kinase C
33
Gq stimulates the formation of what
IP3 and DAG from PIP2
34
drug response is directly related to the number of...
receptors occupied
35
when is drug and receptor response at its maximum
when all available receptor sites are occupied or bound to the drug
36
once all receptors are bound with drug, is there any effect of further addition of the drug
no additional response
37
quantal dose response curves relate the _______ of a drug to the _______ with which a designated response will occur within a population
dosages frequency
38
what is the therapeutic ratio
LD50/ED50
39
is a drug with a large or small therapeutic window 'safer'
larger theraeutic window
40
______ measures the binding of drug to receptor
affinity
41
what is the concentration needed to produce half max binding called
Kd
42
what is the degree of biological response produced by the bidning of a particular drug to a receptor
efficacy | not related to potency
43
intrinsic activity is the ability of a drug to ..... and is synonymous with efficacy
initiate a response
44
agonists have _____ and ______ activity
affinity and intrinsic
45
antagonists have affinity but no _______ activity
intrinsic
46
partial agonists (or antagonists) have affinity but lower ____ activity
intrinsic
47
a _______ binds to the receptor and initiates a response, causes a max shift of receptors to the activated state
agonist | ex: morphine
48
a ______ binds to the receptor but does NOT initiate a response
antagonist blocks response to an agonist | ex: Naloxone
49
binds to the receptor and causes a response that is less that what would be produced by full agonist
partial agonist | ex: Buprenophine
50
_______ antagonists bind to receptor and compete w/ agonist
competitive
51
______ antagonists take receptors out of play
non competitive
52
______ antagonists produce opposing physiological effects
functional (physiological)
53
_______ antagonists have no intrinsic activity (no efficacy)
competitive
54
if agonist concentration is high enough, the effect of the __________ antagonist can be overcome
competitive
55
do competitive antagonists affect max response produced by agonist
NO
56
competitive antagonists shift the dose response curve to the ______
right
57
what is the effect of competitive antagonists on affinity
decrease it (decreased Kd or EC50)
58
what type of antagonism is this
competitive
59
what is the effect of non-competitive antagonists on maximum response
decrease it
60
what type of antagonism is this
non competitive
61
what type of antagonism is this: Epi reverses drop in bp caused by histamine in anaphylaxis
functional / physiological
62
type of antagonist that neutralizes a drug chemically
chemical antagonism
63
what type of antagonism is this: herapin being neutralized by protamine
chemical
64
if ______ agonists are combined with full agonists, they will compete for the recetpor but produce a ________ response
partial smaller
65
what type of agonist is this
partial
66
tolerance is the...
chronic administration of many drugs
67
what are the 2 types of tolerance
pharmacokinetic pharmacodynamic
68
type of tolerance where the drug induces its own metabolism and may also increase metabolism of another drug ex: barbiturates
pharmacokinetic tolerance *Metabolic*
69
type of tolerance caused by the down or up regulation of a drug; includes beta receptor agonsits or antagonists ex: opioids
pharmacodynamic tolerance *changes in the target tissue that makes them **less sensitive** to a given drug [ ]*
70
T/F:drugs are at most 'selective', and rarely 'specific'
T
71
what is dose dependent toxicity
an adverse reaction is mediated by the same receptor effector mechanism ex: excessive sedation by sedative agent...**overextension of the therapeutic effect**
72
what are some examples of dose dependent toxicities
* excessive hypotension * arrhythmias * hypoglycemia * hemorrhage
73
aminoglycosides cause what toxicity
reanl and ototoxicity
74
acetaminophen causes what toxicity
hepatotoxicity
75
chloramphenicol causes what type of toxicity
aplastic anemia
76
tetracycline causes what kind of toxicity
retardation of bone growth
77

PHARMACOLOGY I (21 decks)

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