Pharm Chapter 42- Eicosanoids Flashcards

(66 cards)

1
Q

What are contraindications for aspirin

A

Aspirin hypersensitivity, aspirin-triggered asthma, children and teenagers with chicken pox or flu-like symptoms, due to risk of Reye’s syndrome

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2
Q

What affect does aspirin have with acetazolamine

A

Increases its concentration, which leads to CNS toxicity

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3
Q

What drug may inhibit the antiplatelet effect of aspirin

A

Ibuprofen

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4
Q

Compare naproxen to aspirin

A

Naproxen has a longer half life, is 20X more potent, and causes fewer Gi adverse effects than aspirin

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5
Q

How long can ketorolac be used

A

3-5 days max post-surgery

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6
Q

What COX-1/COX-2 inhibitor has the greatest selectivity for COX-2

A

Nabumetone

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7
Q

What is the leading cause of hepatic failure

A

Acetaminophen overdose

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8
Q

What are the common adverse effects of acetaminophen

A

Hepatotoxicity, nephrotoxicity (rare), rash, hypothermia

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9
Q

What is the only FDA approved COX-2 inhibitor

A

Celecoxib

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10
Q

What effect does celecoxib have on ACE inhibitors

A

Decreases ACE inhibitor efficacy

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11
Q

What is the clinical application of alprostadil

A

Maintenance of patent ductus arteriosus, ED

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12
Q

What are the contraindications for alprostadil

A

Sickle cell anemia or trait leukemia, myeloma, neonatal respiratory distress syndrome, anatomic deformation (of penis, penile implant, Peyronie’s disease)

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13
Q

What is the major contraindication for misoprostol

A

Pregnancy

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14
Q

What is carboprost used for

A

Abortion in second trimester, postpartum hemorrhage

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15
Q

What are common adverse effects of carboprost

A

Dystopia, pulmonary edema, GI disturbance with prevalent diarrhea, headache, paresthesia, fever, breast tenderness

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16
Q

What are contraindications for carboprost

A

Acute pelvic inflammatory disease. Cardiac, pulmonary, renal or hepatic disease

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17
Q

What is the use of letanoprost, bimatoprost, and Travis roar

A

Ocular hypertension, open-angle glaucoma

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18
Q

What are common side effects of latanoprost, bimatoprost, and travoprost

A

Macular retinal edema, blurred vision, hyperpigmentation of eyelid, iris pigmentation

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19
Q

What is the major use of epoprostenol

A

Pulmonary hypertension

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20
Q

What are the contraindications for epoprostenol

A

Heart failure with severe left ventricular dysfunction. Chronic use in patients developing pulmonary edema

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21
Q

What is the major clinical application of zileuton

A

Asthma

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22
Q

What are common side effects of zileuton

A

Increased liver enzymes, urticaria, abdominal discomfort, dizziness, insomnia

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23
Q

What are contraindications for use of zileuton

A

Active liver disease, elevated liver enzymes

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24
Q

What are the clinical applications for montelukast and zafirlukast

A

Chronic asthma, perennial allergic rhinitis (montelukast), and seasonal allergic rhinitis (montelukast)

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25
What are substances that are rapidly synthesized in response to specific stimuli, act quickly in the immediate environment, and remain active for only a short time before degradation
Autacoids
26
What is the common precursor to the majority of eicosanoids
Arachidonic acid
27
What is the precursor for arachidonic acid
Linoleic acid
28
What enzyme facilitates the rate limiting step of eicosanoid formation
Phospholipase A2
29
What does the Cyclooxygenase pathway lead to the formation of
Prostaglandins, prostacylin, thromboxane
30
What does the lipoxygenase pathway lead to the formation of
Leukotrienes and lipoxins
31
What is the tissue location for COX1 and COX2
COX1 is ubiquitous expression; COX1 is in inflamed and activated tissues
32
What tissues expression PGD2
Mast cells, neurons
33
What tissues expression PGE2
Many tissues, including macrophages and mast cells
34
What tissues express PGF2alpha
Vascular smooth muscle, uterine smooth muscle
35
What are the functions of PGD2
Bronchoconstriction (asthma), sleep control functions, Alzheimer's
36
What are the functions of PGE2
Potentiation of responses to painful stimuli, vasodilation, bronchoconstriction, cytoprotective, inflammatory cell activation, fever, mucous production, possibly erectile function
37
What are the functions of PGF2alpha
Vascular tone, reproductive physiology, bronchoconstriction
38
What series of prostaglandins is the most biologically prevalent
PG2
39
What is the chief eicosanoid product of platelets
TXA2
40
What is the primary eicosanoid product of the vascular endothelium
PGI2
41
What is the physiological antagonist to TXA2
PGI2
42
What are the immediate products of lipoxygenase reactions
HPETEs
43
What is the direct precursor to LTA4
5-HPETE
44
What is the precursor to all bioactive leukotrienes
LTA4
45
What helps 5-LOX translocate to the nuclear membrane
FLAP
46
Where is LTA4 converted to LTB4
In neutrophils and erythrocytes
47
Where does LTA4 conversion to LTC4 occur
Mast cells, basophils, eosinophils, and macrophages
48
What lipoxygenase is most present in the brain
12-LOX
49
What are the 2 GPCRs that LTB4 acts via
BLT1 and BLT2
50
What do LTC4 and LTD4 cause
Vasoconstriction, bronchospasm, and increased vascular permeability
51
What are the actions of resolvin E1
Regulates neutrophil infiltration, DC. Function and IL-21 production. Promotes resolution, reduces colitis, and protects from osteoclasts-mediated bone destruction
52
What is the function of resolvin E2
Regulates neutrophil infiltration
53
What are the functions of protectin D1
Regulates neutrophil and T cell infiltration, regulates TNF and interferon production, promotes resolution, reduces peritonitis and airway inflammation, protects brain from ischemia/reperfusion injury may mitigates kidney ischemia injury
54
What is the function of maresin 1
Regulates neutrophil infiltration and promotes resolution
55
What eicosanoids are involved with pain and hyperalgesia
PGE2, PGI2, LTB4
56
What eicosanoids are involved with local heat and systemic fever
PGE2, PGI2, and LXA4
57
What eicosanoids areinvolved in increased vascular permeability
LTC4, LTD4, LTE4
58
What eicosanoids are involved in chemotaxis leukocyte adhesion
LTB4, HETE, LXA4, LXB4
59
What does PGE2 inhibit the function of (what cells)
B and T lymphocytes and NK cells
60
What eicosanoids attract eosinophils to asthmatic pathways
LTD4 and LTE4
61
What do human colorectal adenomas and carcinomas express an abundant amount of
COX2
62
What does inhibition of phospholipase A2 prevent
The release of arachidonic acid from cellular phospholipids (rate limiting step)
63
Describe reye''s syndrome
Condition characterized. By hepatic encephalopathy and liver steatosis in young children
64
What is ridogrel a receptor antagonist to
TXA2
65
What do dazoxiben and pirmagrel inhibit
Thromboxane synthase
66
What synthesis does adenosine inhibit
LTB4