NSAID 2 Flashcards
1
Q
what does analgesic mean
A
stops pain
2
Q
what does antipyretic mean
A
stops fever
3
Q
what does of aspirin is the only effective antiplatelet NSAID
A
low dose
4
Q
what do prostaglandins do to mucous secretion
A
secretion is promoted
5
Q
what do prostaglandins do to peptic ulcers
A
prevent
6
Q
what do prostaglandins do to uterine
A
causes contrations
7
Q
are prostaglandins vasoconstrictors or vasodilatiors
A
usually vasodilation but some are vasoconstrictors
8
Q
what kind of blood flow are prostaglandins important for
A
regulation of renal blood flow
9
Q
what do prostaglandins do to fever and where does this occur
A
promote it by actions in the hypothalamus
10
Q
what do prostaglandins do to inflammation
A
cause it
11
Q
why may prostaglandins be given to induce labour
A
because it promotes uterine contraction
12
Q
what are 6 things that prostaglandins cause
A
- inflammation
- gastric mucous secretion
- uterine contraction
- vasoconstrict + dilate
- renal blood flow
- fever (hypothalamus)
13
Q
what is misoprostol
A
synthetic PGE1
14
Q
what is the role of misoprotol
A
induce labour and treat peptide ulcers
15
Q
how do glucocorticoids work
A
induce lipocortin which inhibits phospholipase A2
16
Q
what is a problem with corticosteroids / glucocorticoids (1 word)
A
toxicity
17
Q
what kind of syndrome do glucocorticoids cause the appearance of
A
cushing’s syndrome
18
Q
what are a few signs of cushing’s syndrome
A
-abnormal fat deposition, hair growth, acne, developmental disorders. breakdown of protein to glucose, muscle wasting. peptic ulcers, hypokalemia, immunosuppression
19
Q
what does glucocorticoids do to fat deposition
A
makes it abnormal
20
Q
what does glucocorticoids do to hair growth
A
increase
21
Q
what does glucocorticoids do to skin
A
acne
22
Q
what does glucocorticoids do to development
A
may cause development disorders
23
Q
what does glucocorticoids do to protein
A
breaks it down into glucose
24
Q
what does glucocorticoids do to muscle
A
causes wasting
25
what does glucocorticoids do to would healing
impairs it
26
what does glucocorticoids do to stomach
causes peptic ulcers
27
what does glucocorticoids do to blood K+ levels
hypokalemia
28
what does glucocorticoids do to immune system
suppress
29
what are 3 things that NSAIDS do
analgesia
antipyretic
anti-inflammatory
30
what are 4 things that NSAIDs are used for
mild - moderate pain
fever
arthritis + other inflammatory disorders
grout + hyperuricemia
31
what is myalgia
muscle pain
32
what is arthralgia
bone pain
33
what is hyperuricemia
lots of urea in blood
34
what are 2 ways that NSAIDS reduce pain
they act at the site of origin of pain and interfere with the perception of pain by CNS
35
what is the mechanism of action of NSAIDS
inhibit fatty acid cyclo-oxygenase (COX)
36
what do NSAIDS do to prostaglandins
inhibit their synthesis
37
what do NSAIDS do to thromboxanes
inhibit their synthesis
38
what do NSAIDS do to prostacyclin
inhibit their synthesis
39
what are 3 things that NSAIDS inhibit the synthesis of
prostaglandins
thromboxanes
prostacyclin
40
how do NSAIDS cause the antipyretic effects
inhibition of prostaglandin E2 biosynthesis in the preoptic region of the hypothalamus
41
what do NSAIDS do to GI
ulceration and intolerance
42
what do NSAIDS do to to platelet aggregation
block (but not COX2 selective NSAIDS)
43
which NSAIDS dont block platelet aggregation
COX2
44
what do NSAIDS do to uterine motility
inhibit
45
what do NSAIDS do to renal function
inhibit prostaglandin-mediated renal function
46
what do NSAIDS do to blood pressure
may cause hypertension
47
what kind of reactions can happen with NSAIDS
hypersensitivity
48
what are 6 common untoward effects of all NSAIDS
- GI ulcers
- block platelet aggregation
- inhibit uterine motility
- inhibit prostaglanding mediated renal function
- hypersensitivity reactions
- may cause hypertension
49
what kind of compounds are All NSAIDS
organic acids
50
where do NSAIDS bind
arachidonic acid site on COX 1 or 2
51
which is the standard NSAID with which all others are compared
aspirin
52
what is the mechanism of action of aspirin
inhibition of both COX isoforms (1 and 2)
53
what does aspirin do to inflammation
interferes with adhesion and migration of granulocytes, leukocytes and macrophages to the site of inflammation
54
can aspirin be used for rheumatoid arthritis, which dose
yes at high doses
55
does aspirin affect fevers
yes it is antipyretic
56
what does aspirin do to body temperature (normal temp and fever temp)
reduces elevated temp without affecting normal temp
57
how does aspirin stop fever
reduces prostaglandin release in hypothalamus
58
what are 2 autonomic effects of aspirin as an anti-pyretic
vasodilation and sweating
59
how does aspirin do the analgesic effect
peripheral action at site of injury and perhaps within CNS
60
what compound is involved in platelet aggregation
thromboxane A2
61
why can't platelets just make more COX when inhibited by apsirin
because it has no nucleus
62
what is special about COX inhibition by aspirin
it is irreversible
63
how does aspirin do its antiplatelet effect
blocks synthesis of thromboxane A2 in platelets
64
how does aspirin effect the heart and how
reduces risk of myocardial infarction and transient ischemic episodes by stopping blot formation in coronary vessels
65
what does aspirin do to bleeding time
doubles
66
what does high doses of aspirin do and how
overcomes beneficial anti-platelet effect by stopping prostacyclin synthesis and thereby increasing chance of vasoconstriction
67
what does prostacyclin do to platelet aggregation
helps stop it
68
what is inhibited with high doses vs low dose of aspirin (general)
low: thromboxane (bad guy)
high: prostacyclin (good guy that stops aggregation
69
what are 3 main undesirable effects of aspirin
- gastric irritation and bleeding
- salicylism
- renal and hepatic effects
70
what does aspirin do to gastric
irritate, bleed
71
how does aspirin cause GI irritation and bleeding
inhibition of production of protecting prostaglandins which normally enhance mucous secretion
72
what dose causes salicylism from aspirin
high doses
73
what are 4 things that happen in salicylism
vomiting, tinnitus, deafness, vertigo
74
what can aspirin do to renal and hepatic system
rare but cause hepatic damage or reduction of renal function
75
whos renal and hepatic system is most effected by aspirin and why
in heart failure because prostaglandin mechanisms become important in renal function
76
who gets reyes syndrome
kids with viral infections who are treated with aspirin
77
what is reye's syndrome associated with (what happens)
encephalopathy and hepatitis
78
what does salicylate poisoning produce
uncoupling of oxidative phosphorylation
79
what is uncoupling of oxidative phosphorylation
electron transport and generation of pH gradient across mitochondrion inner membrane still occurs but ATP is not made
80
what happens to body temp in salicylate poisoning and why
hyperthermia : e transport is exothermic, ATP production is endothermic
81
is e transport exo or endo thermic
exothermic
82
is ATP production exo or endo thermic
endothermic
83
what happens to O2 consumption in salicylate poisoning
increased
84
what happens to CO2 production in salicylate poisoning
increased
85
how does aspirin cause the uncoupling
they mess up the H gradient (reduces it) so that they diffuse back in and dont make ATP
86
what does aspirin do to H gradient
| what does it cause
reduces it
| less ATP can be made
87
why are most NSAIDS other than aspirin not used for antiplatelet
because they dont block COX irreversibly so they would need high doses (compared to aspirin)
88
compare diclofenac and aspirin in terms of side effects
really similar, diclofenac is not much better
89
what is sulindac
a prodrug that needs to be converted into an active metabolite to work
90
what is the duration of action of sulindac
long
91
where is sulindac absorbed
intestine
92
where is sulindac excreted
bile
93
what is the potency of ibuprofen compared to aspirin
more potent
94
does ibuprofen do analgesia
yes
95
what is the analgesia effects of ibuprofen compared to aspirin
does it at a lower dose than aspirin
96
what is the GI effects of ibuprofen compared to aspirin
less because ibuprofen more potent and needs a smaller dose
97
what does ibuprofen do to blood pressure
hypertension
98
how does ibuprofen cause hypertension
stops PGE1 synthesis in kidney and/or altering balance of thromboxane (vasoconstrictor) / prostacyclin (vasodilator) synthesis
99
is thromboxane a vasodilator or constrictor
vasoconstrictor
100
is prostacyclin a vasodilator or constrictor
vasodilator
101
what is naproxen
a non selective COX inhibitor
102
what is naproxen typically used for
osteoarthritis
103
what is unique about naproxen
it is the only NSAID that is a single isomer (others are racemates)
104
what is the duration of action of naproxen
12h hours - long time
105
what are the side effects of naproxen like
less cardio effects than COX 2 inhibitors
106
how does indomethacin work
inhibits COX and phospholipase A2
107
what does indomethacin do (immune)
impedes migration and proliferation of immune cells
108
what are conditions that indomethacin is used for
```
extreme things (really strong)
rheumatic conditions (gout, ankylosing spondylitis) patent ductus arteriosus
```
109
how strong is indomethacin
very
110
what are the side effects of indomethacin
lots because its so strong
111
what are some side effects of indomethacin
GI upset, pancreatitis, headache, dizziness, confusion, thrombocytopenia, aplastic anemia
112
what is ductus arteiosis
a short circuit vessel in fetal circulation that bypasses the lugns
113
why is ductus arteiosis used
because the fetus doesny need to send blood to lungs
114
what drug do you use to treat ductus arteiosis that persists after birth
indomethacin
115
what maintains ductus arteiosis in fetus
cyclo-oxygenase products
116
what is the role of COX 1 (2 main + one side role)
generating prostaglandins (which produce mucous in stomach) and cause platelet aggregation
117
what is the role of COX 2 (3)
inflammation pain and fever
118
which COX is consititutive
COX1
119
which COX is inducible
COX2
120
do COX2 inhibitors (selective) cause platelet effects
no
121
do COX2 inhibitors (selective) cause gastric irritation
no
122
do COX1 inhibitors (selective) cause anti-platelet
yes
123
do COX1 inhibitors (selective) cause gastric irritation
yes
124
what are 3 drugs that are COX 2 selective
meloxicam
etodolac
celecoxib
125
what is the mechanism of action of meloxicam
COX 2 selective
126
what is the mechanism of action of etodolac
COX 2 selective
127
how much more selective is celecoxib for the different COX forms
10X more for COX2 than COX1
128
what is celecoxib often used for
rheumatoid arthritis and osteoartritis
129
does celecoxib cause GI upset
no
130
what are some cardiovascular effects of celecoxib
possibly hypertension
131
why does celecoxib cause hypertension
due to altered ratio of thromboxane (constrict) to prostacyclin (dilate)
132
what are 4 types of prostaglandin receptors
EP1 EP2 EP3 EP4
133
what does EP1 do
potentiation of responses to painful stimulus
134
what does EP2 do
vasodilation, bronchoconstriction
135
what does EP4 do
vasodilation, bronchoconstriction
136
what does EP3 do
gastric mucous secretion
137
which prostaglandins receptor have the same function and what do they do
EP2 and EP4
| vasodilation, bronchoconstriction
138
what is the interest in trying to do along with a prostaglandin receptor antagonist (what are they trying to avoid when designing prostaglandins antagonists)
not disturbing balance between thromboxanes and prostacyclin that use different receptors
139
what do drugs want to do to prostaglandins receptors
antagonize
140
is acetaminophen an NSAID
no
141
what does acetaminophen do
analgesia, antipyretic
142
does acetaminophen do pain
analgesia
143
does acetaminophen do fever
antipyretic
144
does acetaminophen do inflammation
nothing
145
does acetaminophen do platelets
nothing
146
what does acetaminophen do GI
doesnt cause bleeding
147
does acetaminophen affect COX1
no
148
does acetaminophen affect COX2
no
149
which COX does acetaminophen affect
COX 3
150
what are 2 uses of tylenol / acetaminophen
mild pain, fever in children (no reye's sendrom)
151
is tylenol good for arthritis
no not alone
152
what are 5 effects of tylenol / acetaminophen
dizziness, excitement, disorientation, hepatic damage, renal damage
153
what does tylenol do to hepatic system + symptoms
cause damage : nausea vomiting diarrhea abdominal pain
154
how much tylenol is fatal
15g
155
can renal damage from tylenol happen with hepatic damage
yes
156
can renal damage from tylenol happen without hepatic damage
yes
