Eicosanoids

Question 1

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

Answer 1

Eicosanoids

Question 2

Eicosanoid examples

Answer 2

Prostaglandin
Thromboxane
Prostacyclin
Leukotriene
Lipoxin

Question 3

Eicosanoid Biomedical Importance

Answer 3

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

Question 4

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

Answer 4

Nonsteroidal anti-inflammatory drugs

Question 5

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

Answer 5

Steroidal anti-inflammatory drugs

Question 6

NSAIDs block prostaglandin production via

Answer 6

Cyclooxygenase inhibition

Question 7

Steroids block prostaglandin release by inhibiting

Answer 7

phospholipase A2 activity to interfere with mobilization of arachidonic acid

Question 8

Acts on the SMOOTH MUSCLE

Used to induce parturition and for the termination of unwanted pregnancy

Answer 8

PGE2

PGF2

Question 9

Membrane phospholipid is converted into arachidonate via

Answer 9

Phospholipase A2

Question 10

Phospholipase A2 that converts membrane phospholipids to arachidonate is stimulated by

Answer 10

various stimuli 
angiotensin II
bradykinin
epinephrine
thrombin

Question 11

Arachidonate is further converted into either

Answer 11

Lipoxygenase

Cyclooxygenase

Question 12

Lipoxygenase

Answer 12

Leukotrienes

Lipoxins

Question 13

Cyclooxygenase

Answer 13

Prostaglandins

Thromboxanes

Question 14

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

Answer 14

self-catalyzed destruction

Question 15

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

Answer 15

15-hydroxyprostaglandin dehydrogenase

Question 16

Constitutively expressed
Inhibited by NSAIDs

Blocking this cyclooxygenase isoform results in
gastritis
GI bleeding

Answer 16

COX-1

Question 17

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

Answer 17

COX-2

Question 18

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

Do not cause gastric irritation and bleeding

Answer 18

COX-2

Question 19

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

Answer 19

Prostacyclin PGI2

Question 20

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

Answer 20

Thromboxane A2

Question 21

Drug that inhibits TXA2

Answer 21

Aspirin

Question 22

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

Answer 22

PGE2

Question 23

PGE1 analog used to induce labor

Answer 23

Misoprostol

Question 24

Produced in leukocytes
platelets
mast cells
heart and lung vascular tissues

Answer 24

Leukotriene A4 LTA4

Question 25

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

Answer 25

LTC4 -> LTD4 -> LTE4

Question 26

Arachidonjc acid is converted into

Answer 26

15-lipoxygenase

Question 27

15-lipoxygenase is converted into

Answer 27

15-HPETE

Question 28

15-HPETE is converted into

Answer 28

5-lipoxygenase

Question 29

5-lipoxygenase is converted into

Answer 29

Lipoxins

Question 30

Family of unconjugated tetraenes also arising in leukocytes Exhibit vasoactive and immunoregulatory function

Answer 30

Lipoxins (LXA4)

Question 31

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

Answer 31

Arachidonic acid: 5-LOX -> 5 HPETE -> Leukotrienes COX -> TXA, Prostacyclin (PGI2), Prostaglandin (PGE, PGF)

Question 32

In prostate glands

Answer 32

Prostaglandin

Question 33

On thrombocytes

Answer 33

Thromboxane

Question 34

In leukocytes

Answer 34

Leucotrienes

Question 35

PGH2 or Cycloendoperoxidases from COX

Answer 35

PGI TXA2 PGE PGF2a

Question 36

Acts on endothelium Antiplatelet aggregation Vasodilation

Answer 36

PGI

Question 37

Smooth muscle contraction | Vasodilation

Answer 37

PGE2

Question 38

Released by platelet Platelet aggregation Vasoconstriction

Answer 38

TxA2

Question 39

Smooth muscle contraction | Vasoconstriction

Answer 39

PGF2a

Question 40

Inflammation Bronchoconstriction Vasoconstriction Capillary permability

Answer 40

Leukotrienes

Question 41

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

Answer 41

Slow-reacting Substance of Anaphylaxis SRS-A

Question 42

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

Answer 42

PGE1 | Alprostadil

Question 43

Cause contraction of the uterus | Approved for use to soften the cervix at term before induction of labor with oxytocin

Answer 43

Dinoprostone | PGE2

Question 44

Cause contraction of uterus Used as abortifacients in the second trimester of pregnancy Produce more GI effects than oxytocin

Answer 44

PGE2 | PGF2a

Question 45

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

Answer 45

Misoprostol

Question 46

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

Answer 46

PGE1

Question 47

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

Answer 47

PGI2

Question 48

PGF2a derivative used extensively for the topical treatment of glaucoma Reduce intraocular pressure, apparently by increasing outflow of aqueous humor

Answer 48

Latanoprost Bimatoprost Travoprost Unoprostone

Question 49

Selective inhibitor of lipoxygenase inhibiting leukotrienes

Answer 49

Zileuton

Question 50

Inhibitor at CysLT1 receptor of LTD4 and LTE4 receptor

Answer 50

Montelukast | Zafirlukast

Question 51

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

Answer 51

Leukotrienes

Question 52

Chemotactic factor in inflammation | Local release

Answer 52

LTB4

Question 53

Activates TP alpha beta receptors Causes platelet aggregation Vasoconstriction

Answer 53

TXA2

Question 54

Parenteral or inhalation form of PGI2 analog for pulmonary hypertension

Answer 54

Treprostinil

Question 55

Reversibly inhibits COX-1 and COX-2 | Reduces synthesis of prostaglandin

Answer 55

Ibuprofen Indomethacin Naproxen

Question 56

Irreversibly inhibits COX-1 and COX-2 | Reduces synthesis of prostaglandins

Answer 56

Aspirin

Question 57

Reversibly inhibits phospholipase A2 | Reduces synthesis of COX, LOX enzymes

Answer 57

Corticosteroids

Question 58

Injectable COX

Answer 58

Parecoxib Prodrug of Valdecoxib

Question 59

FDA banned because it increases HTN

Answer 59

Etoricoxib | Arcoxia

Question 60

Banned because of CV effects

Answer 60

Rofecoxib