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Biochemistry > Eicosanoids > Flashcards

Eicosanoids Flashcards

1
Q

Hormone-like compounds that are derived from 20-carbon atom eicosanoic acids such as arachidonic acid and timnodonic acid

A

Eicosanoids

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2
Q

Eicosanoid examples

A 
Prostaglandin
Thromboxane
Prostacyclin
Leukotriene
Lipoxin
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3
Q

Eicosanoid Biomedical Importance

A 
Modulating the vascular tone, platelet
Platelet aggregation
Gastric secretion
Salt and water balance
Mediating pain and inflammatory responses
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4
Q

Drugs that act to reduce inflammation and provide pain relief by blocking the production of prostaglandins through inhibition of cyclooxygenase

A

Nonsteroidal anti-inflammatory drugs

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5
Q

Blocks prostaglandin release by inhibiting phospholipase A2 activity so as to interfere with mobilization of arachidonic acid

A

Steroidal anti-inflammatory drugs

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6
Q

NSAIDs block prostaglandin production via

A

Cyclooxygenase inhibition

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7
Q

Steroids block prostaglandin release by inhibiting

A

phospholipase A2 activity to interfere with mobilization of arachidonic acid

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8
Q

Acts on the SMOOTH MUSCLE

Used to induce parturition and for the termination of unwanted pregnancy

A

PGE2

PGF2

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9
Q

Membrane phospholipid is converted into arachidonate via

A

Phospholipase A2

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10
Q

Phospholipase A2 that converts membrane phospholipids to arachidonate is stimulated by

A 
various stimuli 
angiotensin II
bradykinin
epinephrine
thrombin
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11
Q

Arachidonate is further converted into either

A

Lipoxygenase

Cyclooxygenase

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12
Q

Lipoxygenase

A

Leukotrienes

Lipoxins

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13
Q

Cyclooxygenase

A

Prostaglandins

Thromboxanes

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14
Q

Cyclooxygenase hww a remarkable property of switching off prostaglandin formation by its

A

self-catalyzed destruction

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15
Q

Self-catalyzed destruction of cox is due to the action of

A

15-hydroxyprostaglandin dehydrogenase

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16
Q

Constitutively expressed
Inhibited by NSAIDs

Blocking this cyclooxygenase isoform results in
gastritis
GI bleeding

A

COX-1

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17
Q

Made only in response to inflammatory mediators such as cytokines
Inhibited by NSAID

A

COX-2

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18
Q

Block COX-2 and are called COX-2 specific inhibitors

Do not cause gastric irritation and bleeding

A

COX-2

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19
Q

Produced by endothelial cells of blood vessels
Causes vasodilation
Inhibits platelet aggregation
Increases formation of cAMP

A

Prostacyclin PGI2

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20
Q 
Produced primarily by platelets
Promotes platelet aggregation
Decreases formation of cAMP
Causes vasoconstriction
Mobilizes intracellular calcium
Stimulates concentration of smooth muscle
A

Thromboxane A2

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21
Q

Drug that inhibits TXA2

A

Aspirin

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22
Q

Produced by most tissues especially the kidney
Causes arteriolar vasodilation
Increases capillary permeability
Evokes chemokinesis of T cells
Enhances pain caused by histamine and bradykinin
Relaxes smooth muscle
Used to induce labor

A

PGE2

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23
Q

PGE1 analog used to induce labor

A

Misoprostol

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24
Q

Produced in leukocytes
platelets
mast cells
heart and lung vascular tissues

A

Leukotriene A4 LTA4

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25
Q 
Contraction of snooth muscle
Bronchoconstriction
Vasoconstriction
Increased vascular permeability
Components of slow-reacting substance of anaphylaxis (SRS-A)
A

LTC4 -> LTD4 -> LTE4

26
Q

Arachidonjc acid is converted into

A

15-lipoxygenase

27
Q

15-lipoxygenase is converted into

A

15-HPETE

28
Q

15-HPETE is converted into

A

5-lipoxygenase

29
Q

5-lipoxygenase is converted into

A

Lipoxins

30
Q

Family of unconjugated tetraenes also arising in leukocytes

Exhibit vasoactive and immunoregulatory function

A

Lipoxins (LXA4)

31
Q

A 20 - carbon Omega 6 Fatty Acid with 4 double bonds

A

Arachidonic acid:

5-LOX -> 5 HPETE -> Leukotrienes

COX -> TXA, Prostacyclin (PGI2), Prostaglandin (PGE, PGF)

32
Q

In prostate glands

A

Prostaglandin

33
Q

On thrombocytes

A

Thromboxane

34
Q

In leukocytes

A

Leucotrienes

35
Q

PGH2 or Cycloendoperoxidases from COX

A

PGI
TXA2
PGE
PGF2a

36
Q

Acts on endothelium
Antiplatelet aggregation
Vasodilation

A

PGI

37
Q

Smooth muscle contraction

Vasodilation

A

PGE2

38
Q

Released by platelet
Platelet aggregation
Vasoconstriction

A

TxA2

39
Q

Smooth muscle contraction

Vasoconstriction

A

PGF2a

40
Q

Inflammation
Bronchoconstriction
Vasoconstriction
Capillary permability

A

Leukotrienes

41
Q

Material originally identified by bioassay from tissues of animals in anaphylactic shock; now recognized as a mixture of leukotrienes, especially LTC4 and LTD4

A

Slow-reacting Substance of Anaphylaxis SRS-A

42
Q

Used in the treatment of impotence by injection into cavernosa of a urethral suppository

A

PGE1

Alprostadil

43
Q

Cause contraction of the uterus

Approved for use to soften the cervix at term before induction of labor with oxytocin

A

Dinoprostone

PGE2

44
Q

Cause contraction of uterus
Used as abortifacients in the second trimester of pregnancy

Produce more GI effects than oxytocin

A

PGE2

PGF2a

45
Q

The PGE1 analog used with progesterone antagonist Mifepristone (RU 486) as an extremely effective and safe abortifacient combination

Approved for the prevention of peptic ulcers in patients who must take high doses of NSAIDs for arthritis and who have a history of ulcer associated with this use

May cause diarrhea

A

Misoprostol

46
Q

Given as an infusion to maintain patency of the ductus arteriosus in infants with transposition of the great vessels until surgical correction can be undertaken

A

PGE1

47
Q

Approved for use as epoprostenol in severe pulmonary hypertension and to prevent platelet aggregation in dialysis machines

A

PGI2

48
Q

PGF2a derivative used extensively for the topical treatment of glaucoma

Reduce intraocular pressure, apparently by increasing outflow of aqueous humor

A

Latanoprost

Bimatoprost
Travoprost
Unoprostone

49
Q

Selective inhibitor of lipoxygenase inhibiting leukotrienes

A

Zileuton

50
Q

Inhibitor at CysLT1 receptor of LTD4 and LTE4 receptor

A

Montelukast

Zafirlukast

51
Q

When COX is blocked, this is produced in increased amounts by diversion of prostaglandin precursors into the lipoxygenase pathway

A

Leukotrienes

52
Q

Chemotactic factor in inflammation

Local release

A

LTB4

53
Q

Activates TP alpha beta receptors
Causes platelet aggregation
Vasoconstriction

A

TXA2

54
Q

Parenteral or inhalation form of PGI2 analog for pulmonary hypertension

A

Treprostinil

55
Q

Reversibly inhibits COX-1 and COX-2

Reduces synthesis of prostaglandin

A

Ibuprofen
Indomethacin
Naproxen

56
Q

Irreversibly inhibits COX-1 and COX-2

Reduces synthesis of prostaglandins

A

Aspirin

57
Q

Reversibly inhibits phospholipase A2

Reduces synthesis of COX, LOX enzymes

A

Corticosteroids

58
Q

Injectable COX

A

Parecoxib

Prodrug of Valdecoxib

59
Q

FDA banned because it increases HTN

A

Etoricoxib

Arcoxia

60
Q

Banned because of CV effects

A

Rofecoxib

Biochemistry (32 decks)

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