Eicosanoids Flashcards

1
Q

Clinical analog of Prostacyclin (PGI2) (2)

A

Epoprostenol, Iloprost

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2
Q

Clincal analog of PGE2 (3)

A

Misoprostol
Alprostadil
Dinoprostone

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3
Q

Clinical analog of PGF2a

A

Latanoprost

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4
Q

Name leukotriene receptor antagonist

A

Montelukast, Zafirlukast,

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5
Q

Name a lioxygenase inhibitor

A

Zileuton

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6
Q

What is omacor/lovaza

A

Omega-3 Fatty Acids

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7
Q

2 classes o f eicosanoids

A
  1. Prostaglandins

2. Leukotrienes

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8
Q

Eicosanoids are derived from/rate limiting step/enzye

A

Arachidonic Acid by Phospholipase A2

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9
Q

Main sourse of arachidonic acid

A

Dietary linoleic acid

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10
Q

Which enzyme is responsible for the production of prostaglandins

A

Cyclo-oxygenases

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11
Q

Which enzyme is responsible for the production of leukotrienes

A

Lipoxygenases

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12
Q

Half life for eicosanoids

A
  • Have short half lives (<5 min) and act locally (autocoids)
  • metabolized in tissues and excreted in urine
  • do not circulate in blood
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13
Q

Which receptor do prostaglandins activate

A

G protein recptors
Can raise cAMP leves = smooth muscle reaxation
Activate PLC and raise Ca = smooth muscle contraction

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14
Q

Which prostglandins cause resp. smooth muscle to relax

A

PGE2, PGI2 = relax respiratory sm

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15
Q

Which prostglandins cause resp. smooth muscle to contract

A

PGF2a

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16
Q

Which prostaglandins cause longituidnal muscles in the GI system to contract (diarrhea & vomiting)

A

PGE2, PGF2a

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17
Q

Which prostaglanin causes circular muscle to relax

A

PGE2

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18
Q

Which prostglandins cause vascular constriction in smooth muscle

A

-TXA2, PGF2a

19
Q

Which prostglandins cause vascular dilitation in smooth muscle

A

PGI2, PGE2

20
Q

Which prostaglandins cause uterine constriction

A

-PGE2, PGF2a, TXA2 = contract

21
Q

Which prostaglandins cause uterine dilatation

A

PGI2

22
Q

Which prostglandins are cytoprotective (more mucus) to G.I.

A

PGE2

23
Q

In asthma are the PGs or leukotirens more importat

A

eukotrienes are major mediators of asthma

24
Q

Which leukotrienes most important in asthma

A

LTC4, LTD4 pathologic for asthma

Bronchoconstriction, inc mucus secretion, increased vasc permeability

25
Q

Which prostglandin is major mediator of pain and fever

A

PGE2

26
Q

Which prostglanins mediate dysenorrhea

A

PGE2 and PGF2

27
Q

Which prostgladins regluate intraocular eye pressure

A

PGF2

28
Q

How to corticosteriods exert their effect

A

Corticosteriods reduce the activity of PLA2 and synthesis of COX2

29
Q

How does asprin exert its effect

A

aspirin irreversibly inhibit COXs while all other NSAIDs are reversible inhibitors - prevents vasoconstriction & platelet aggregation

30
Q

Whay are COX2 inhibitors associates with adverse cardiac effects

A

Inhibit PGI2 vasodilatory effects and get uninhibited COx1/TXA2 vasoconstrictio

31
Q

Which cell type ainly produces leukocytes

A

Leukotrienes

32
Q

Second messanger for leukotriene receptors

A

IP3 with a subsequent increase in [Ca2+]

33
Q

What is SRS-A = slow-reacting substance of anaphylaxis.

A

LTC4 and LTD4

ALso active in asthma

34
Q

Mechanism for asprine induced hypersensitivity asthma

A

Know that aspirin induced hypersensitivity asthma may be

exacerbated by diverting arachidonic acid to leukotrienes (LTC4 and LTD4)

35
Q

5 lipoxygebase inhibitor

A

Zileuton

36
Q

Leukotriene receptor antagonist

A

Zarfirlukast

Montelukast

37
Q

Misoprostol (Cytotex)

  • Use
  • Side Effect
  • Contraindications
  • BBW
A

Primarily used for ulcer prevention during long-tem NSAID therapy (FDA approved): increases mucus & bicarbonate secretion

Adverse effects
Diarrhea and occasional abdominal discomfort

Contraindication
Pregnancy due to uterotonic activity

BBW
Abortion & birth defects

38
Q

What is used to keep PDA open

A

PGE2

39
Q

What is used to close PDA

A

Ibuprofen

Indomethacin

40
Q

Iloprost (Ilomedin)

  • Use
  • Mechanism
A

FDA approved for pulmonary hypertension

A stable second generation analog of prostacyclin

41
Q

Alprostadil

  • Mechanism
  • Side Effect
A

PGE1 analog.

Vasodilator

Pharmacokinetics:
Can be injected directly into the cavernosa, used as a topical cream, or placed in the urethra as a minisuppository, from which it diffuses into the cavernosal tissue

Side Effects:
penile pain (29-49% of users)
urethral bleeding (5%)
hypotension within 1 hour of use (3.3%)

42
Q

Zileuton

  • Drug class
  • Mechanism
  • Indications
A

Drug Class:Leukotriene pathway inhibitor

Mechanism of Action:
orally activeinhibitor of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid

Indications:
prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older. (

43
Q

Montelukast

  • Drug class
  • Mechanism
A

Drug Class:Leukotriene Inhibitor
Mechanism of Action:
anLTD4-receptor antagonist
Indications:
for the prophylaxis and chronictreatment of asthmain adults and pediatric patients 6 years of age and older.
It is NOT indicated for use in the reversal of bronchospasm in acute asthma attacks.
Pharmacokinetics:
effective orally,taken once a day(typically in the evening)

44
Q

Dexamethason

  • Class
  • Mechanism of action
  • Indication
A

Drug Class:Glucocorticoid, Anti-Inflammatory

Mechanism of Action:Binds to intracellular glucocorticoid receptors and modulates gene expression.Glucocorticoids dramatically reduce the manifestations of inflammation due to their profound effects on the concentration, distribution, and function of peripheral leukocytes and to their suppressive effects on the inflammatory cytokines and chemokines and on other lipid and glucolipid mediators of inflammation.

Indications:
used for its potent anti-inflammatory effects in disorders of many organ systems.
Examples of indications include:rheumatic disorders, arthritis, lupus erythrematosus, bronchial asthma & ulcerative colitis.
Glucocorticoids cause profound and varied metabolic effects. In addition, they modify the body’s immune responses to diverse stimuli..