Pharm Chapter 42- Eicosanoids Flashcards

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
Q

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

A

Autacoids

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26
Q

What is the common precursor to the majority of eicosanoids

A

Arachidonic acid

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27
Q

What is the precursor for arachidonic acid

A

Linoleic acid

28
Q

What enzyme facilitates the rate limiting step of eicosanoid formation

A

Phospholipase A2

29
Q

What does the Cyclooxygenase pathway lead to the formation of

A

Prostaglandins, prostacylin, thromboxane

30
Q

What does the lipoxygenase pathway lead to the formation of

A

Leukotrienes and lipoxins

31
Q

What is the tissue location for COX1 and COX2

A

COX1 is ubiquitous expression; COX1 is in inflamed and activated tissues

32
Q

What tissues expression PGD2

A

Mast cells, neurons

33
Q

What tissues expression PGE2

A

Many tissues, including macrophages and mast cells

34
Q

What tissues express PGF2alpha

A

Vascular smooth muscle, uterine smooth muscle

35
Q

What are the functions of PGD2

A

Bronchoconstriction (asthma), sleep control functions, Alzheimer’s

36
Q

What are the functions of PGE2

A

Potentiation of responses to painful stimuli, vasodilation, bronchoconstriction, cytoprotective, inflammatory cell activation, fever, mucous production, possibly erectile function

37
Q

What are the functions of PGF2alpha

A

Vascular tone, reproductive physiology, bronchoconstriction

38
Q

What series of prostaglandins is the most biologically prevalent

A

PG2

39
Q

What is the chief eicosanoid product of platelets

A

TXA2

40
Q

What is the primary eicosanoid product of the vascular endothelium

A

PGI2

41
Q

What is the physiological antagonist to TXA2

A

PGI2

42
Q

What are the immediate products of lipoxygenase reactions

A

HPETEs

43
Q

What is the direct precursor to LTA4

A

5-HPETE

44
Q

What is the precursor to all bioactive leukotrienes

A

LTA4

45
Q

What helps 5-LOX translocate to the nuclear membrane

A

FLAP

46
Q

Where is LTA4 converted to LTB4

A

In neutrophils and erythrocytes

47
Q

Where does LTA4 conversion to LTC4 occur

A

Mast cells, basophils, eosinophils, and macrophages

48
Q

What lipoxygenase is most present in the brain

A

12-LOX

49
Q

What are the 2 GPCRs that LTB4 acts via

A

BLT1 and BLT2

50
Q

What do LTC4 and LTD4 cause

A

Vasoconstriction, bronchospasm, and increased vascular permeability

51
Q

What are the actions of resolvin E1

A

Regulates neutrophil infiltration, DC. Function and IL-21 production. Promotes resolution, reduces colitis, and protects from osteoclasts-mediated bone destruction

52
Q

What is the function of resolvin E2

A

Regulates neutrophil infiltration

53
Q

What are the functions of protectin D1

A

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
Q

What is the function of maresin 1

A

Regulates neutrophil infiltration and promotes resolution

55
Q

What eicosanoids are involved with pain and hyperalgesia

A

PGE2, PGI2, LTB4

56
Q

What eicosanoids are involved with local heat and systemic fever

A

PGE2, PGI2, and LXA4

57
Q

What eicosanoids areinvolved in increased vascular permeability

A

LTC4, LTD4, LTE4

58
Q

What eicosanoids are involved in chemotaxis leukocyte adhesion

A

LTB4, HETE, LXA4, LXB4

59
Q

What does PGE2 inhibit the function of (what cells)

A

B and T lymphocytes and NK cells

60
Q

What eicosanoids attract eosinophils to asthmatic pathways

A

LTD4 and LTE4

61
Q

What do human colorectal adenomas and carcinomas express an abundant amount of

A

COX2

62
Q

What does inhibition of phospholipase A2 prevent

A

The release of arachidonic acid from cellular phospholipids (rate limiting step)

63
Q

Describe reye’’s syndrome

A

Condition characterized. By hepatic encephalopathy and liver steatosis in young children

64
Q

What is ridogrel a receptor antagonist to

A

TXA2

65
Q

What do dazoxiben and pirmagrel inhibit

A

Thromboxane synthase

66
Q

What synthesis does adenosine inhibit

A

LTB4