Third Flashcards
1
Q
Inflammatory compounds are all derived from_____________ which is broken down by _____________
A
membrane phospholipids
phospholipase
2
Q
Phospholipase breaks down phospholipids to produce _____________
A
arachidonic acid
3
Q
Arachidonic acid can enter two cycles…what are they?
A
lipoxygenase
cyclo-oxygenase
4
Q
Leukotrienes are derived from what pathway?
A
lipoxygenase
5
Q
Prostaglandins are derived from what pathway?
A
cyclo-oxygenase
6
Q
Thomboxane are derived from what pathway?
A
cyclo-oxygenase
7
Q
Prostacyclin are derived from what pathway?
A
cyclo-oxygenase
8
Q
Prostacyclins counteract the action of _____________
A
thromboxanes
9
Q
LTB4 is involved in ___________
A
chemotaxis
hyperalgesia
10
Q
LCT4, LTD4, LTE4 are involved in _______________
A
bronchoconstriction
edema
*produced in asthma
11
Q
Zafirlukast, montelukast block activity of which leukotrienes?
A
LCT4, LTD4, LTE 4
12
Q
Acetaminophen is _______________ an NSAID
A
NOT
*tylenole ?
13
Q
Is aspirin an NSAID?
A
yep
14
Q
Is acetaminophen an NSAID?
A
nope
15
Q
MOA of NSAIDs
A
blocks cyclo-oxygenase pathway
*cox 1 and cox 2
16
Q
What are the selective COX2 inhibitors?
A
celecoxib
rofecoxib
17
Q
Why would you prefer selective cox2 inhibitors over common nsaids?
A
COX1 remains intact, allowing for the production of gastric cytoprotection
18
Q
COX1 pathway is known as the ___________ pathway
A
constitutive physiologically active (always on) -gastric protection
19
Q
COX2 pathway is known as the ____________pathway
A
inducible
20
Q
Why would the COX2 pathway be turned on?
A
it kickstarts the inflammatory process, including pain
makes you mores sensitive to pain
21
Q
What turns of COX2 pathway?
A
glucocorticoids
NSAIDs
growth factors, gut peptides
COX 2 inhibitors
22
Q
_____________is located predominantly located in the vascular endothelium
A
prostacyclin
PGI2
23
Q
TxA2 is found ________________
A
in the platelets
24
Q
What are the main effects of PGI2?
A
vasodilation
inhibition of platelet aggregation
25
What are the main effects of TxA2?
platelet aggregation
| vasoconstriction
26
PGE2 causes________________
inhibitirion of gastric acid secretion
contraction of uterus
contraction of GI smooth muscles
27
PGF2-a main effects are ________________
contraction of bronchi
| contraction of myometrium in uterus
28
The cyclooxygenase (COX) is found ____________________________
bound to the endoplasmatic reticulum
29
__________ acts in physiological conditions
COX1
30
___________ is induced by inflammatory cells by pathological stimulus
COX2
31
____________ is located only in the brain
COX3
32
Which COX provides gastric protection?
COX1
33
What are the nonselective NSAIDs?
```
salicylates
pehnylacetates
ndolacetates
enolates
fenamates
propionates
butylpyrazo----- ugh
```
34
Phenylacetates:______________
diclofenac
35
indolacetates:__________________
indomethacin, sulindac
36
Enolates:____________________
piroxicam..... I dont think we need to know these.
37
___________connected with influence of thermoregulatoy centre in the hypothalamus
antipyresis
| *benefit of NSAID
38
_________________mainly anti-exudative effect
anti-inflammatory
| *benefit of NSAID
39
_______________ in very low daily doses
anti-thrombotic action
| *benefit of NSAID
40
__________ of ductus arteriosus
Closure
| *benefit of NSAID-specifically INDOMETHACIN
41
Which NSAID can be used to close the ductus arteriosus?
indomethacin
42
Toxicities of NSAIDs
```
gastric mucosal damage
bleeding
limitation of renal blood flow
delay/prolongation of labor
asthma and anaphylactoid reactions
```
43
__________ arises from the inhibition of platelet function (TxA2 synthesis)
bleeding
44
Limitation of renal blood flow results in what?
Na and water retention
45
Asthma and anaphylactoid reactions associated with NSAIDS are connected with __________ inhibition
PGF2-a
46
How NSAIDs cause mucosal injury
ion trapping - direct toxicity from NSAID use
47
Aspirin when metabolized is split into what 2 compounds?
acetic acid
| salicylate
48
What can salicylate conjugate with?
glucuronic acid
| glycine
49
When salicylates are oxidized they become __________
gentisic acid
50
Aspirin resets the ___________________
hypothalmic? thermastat
51
dont need to know slide 25-31
nope
52
___________ increases GI toxicity of NSAIDs
alcohol
53
Aspirin in high dose reduces renal tubular excretion of _____________
urate
| *is harmful to the tubules-causes damage
54
What are the uses of Aspirin?
analgesic
antipyretic
acute rheumatic fever
rheumatoid arthritis
55
____________ is the DOC for acute rheumatic fever
aspirin
56
What two drugs are safer than aspirin in the treatment of a fever?
paracetamol
metamizole
*these are preferred over aspirin
57
When treating RA with aspirin, when should the medication be given?
after meal
58
Aspirin in children with a viral infection can result in what?
Reyes syndrome
59
What is reyes syndrome
Aspirin in children w/viral infection
| hepatic encephalopathy seen in children
60
Aspirin should not be given to children under the age of ________
15
61
What is a possible AE of being on chronic aspirin?
blood thinning
| *higher risk of hemorrhagic stroke
62
NSAIDs + cyclosporines
increase nephrotoxicity
63
NSAIDs+ ACEi or BB
decrease antihypertensive effect
64
NSAIDs + sulfonylureas
increased risk of hypoglycemia
65
NSAIDs+ GCS
increase risk of GI bleeding
66
NSAIDs+alcohol
increase of GI bleeding
67
Ibuprofen (advil) is a derivative of ______________
phenylpropionic acid
68
What is the effect of oral ibuprofen in lower doses?
analgesic but not inflammatory effect
69
A liquid form of __________ provides prompt relief in post surgical dental pain
ibuprofen
70
Aspirin is ______ potent than ibuprofen
less
71
In addition to indomethacin, what other NSAID is effective in closing the ductus arteriosus?
ibuprofen
72
In comparison to indomethacin, ibuprofen ________ urine output less and causes ________ fluid retention
decreases urine output
| less fluid retention
73
________________ is a propionic acid derivative
ketoprofen
74
____________ inhibits both COX (non-selectively) and lipoxygenase
ketoprofen
75
Ketoprofen has a dual effect on ________ and __________
prostaglandins
leukotrienes
* is no better than any other NSAID
76
_______________ is a non selective cox inhibitor and may also inhibit phospholipase A and C, reduce neutrophil migration and decreases production of T and B cells
indomethacin
77
Give _________ to prolong the life of indomethacin
probenecid
| *inhibits both renal and biliary clearance
78
Indications of indomethacin
juvenile RA, gout, ankylosing spondylitis, postepisiotomy pain
79
There is an ophthalmic preparation of ___________
indomethacin
80
_________ comes in an oral formulation
indomethacin
81
Diclofenac is a ____________ derivative
phenylacetic
82
____________ in a rectal suppository form can be considered and DOC for analgesia and postoperative nausea
diclofenac
83
A combination of diclofenac and ___________ decreases upper GI ulceration
misoprostol (PGE1)
84
___________ is a non-selective COX inhibitor that at high concentrations inhibits polymorphonuclear leukocyte migration, decreases oxygen radical production and inhibits lymphocyte function
piroxican
85
Piroxicam has a ______ half life
long
| *can give only once a day
86
In doses >20 mg/d of piroxicam you have a higher incidence of ______________
peptic ulcer and bleeding
| *this drug has a higher risk than other NSAIDs
87
Selective COX 2 inhibitors
celeboxib
88
Preferential COX 2 inhibitors
meloxicam
| nabumetone
89
What is meloxicam?
preferential cox 2 inhibitor
90
What is nabumetone?
preferential cox 2 inhibitor
91
What is celeboxib?
selective cox 2 inhibitor
92
___________are selective cox 2 inhibitors
coxibs
93
What is the only benefit of coxibs?
ulcerogenic potential is lower
94
Celecoxib is a _____________
sulfonamide
95
Celecoxib may cause _____________
rashes
96
Celecoxib __________ effect platelet aggregation
does not (within normal doses)
97
_____________ is an enolcarboxamide
meloxicam
98
Meloxicam is ___________ selective
preferentially
99
_____________ is associated with fewer GI symptoms and complications than piroxicam, diclofenac and naproxen
meloxicam
100
________ can cause infertility.
coxibs
101
_________ have prothrombotic cardiovascular risk
coxibs
102
Acetaminophen is different than NSAIDs d/t its lack of ________________
anti-inflammatory effects
103
Acetaminophen _______ effect uric acid levels
does not
104
Acetaminophen is preferential to aspirin in patients with ______________ or a history of ________ and_________
hemophilia
peptic ulcers
bronchospasm
105
You have a kid with a viral infection, what do you give him? Aspirin or acetaminophen?
acetaminophen
| *no risk of Reye's syndrome
106
NABQI is detoxicated by _________________
conjugation with glutathione
107
_____________is a highly reactive arylating metabolite of acetaminophen
NABQI
108
Why is NABQI bad?
it binds covalently to proteins in the liver and causes necrosis
109
What can you give in an acute gout situation?
colchicine
diclofenac, indomethacin
naproxen , piroxiam
110
What are the uricostatics?
xanthine oxidase inhibitors
| -allopurinol, febuxxostat
111
What are the uricosurics?
probenecid, benzbromarone
| sulfinpyrazone
112
What are the uricolytics?
uricase, rasburicase
113
Allopurinol + benzbromarone
harpagin
114
_________increase the release of uric acid, preventing buildup, preventing gout
uricosurics
