Eicosanoids

Question 1

Clinical analog of Prostacyclin (PGI2) (2)

Answer 1

Epoprostenol, Iloprost

Question 2

Clincal analog of PGE2 (3)

Answer 2

Misoprostol
Alprostadil
Dinoprostone

Question 3

Clinical analog of PGF2a

Answer 3

Latanoprost

Question 4

Name leukotriene receptor antagonist

Answer 4

Montelukast, Zafirlukast,

Question 5

Name a lioxygenase inhibitor

Answer 5

Zileuton

Question 6

What is omacor/lovaza

Answer 6

Omega-3 Fatty Acids

Question 7

2 classes o f eicosanoids

Answer 7

1. Prostaglandins

2. Leukotrienes

Question 8

Eicosanoids are derived from/rate limiting step/enzye

Answer 8

Arachidonic Acid by Phospholipase A2

Question 9

Main sourse of arachidonic acid

Answer 9

Dietary linoleic acid

Question 10

Which enzyme is responsible for the production of prostaglandins

Answer 10

Cyclo-oxygenases

Question 11

Which enzyme is responsible for the production of leukotrienes

Answer 11

Lipoxygenases

Question 12

Half life for eicosanoids

Answer 12

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

Question 13

Which receptor do prostaglandins activate

Answer 13

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

Question 14

Which prostglandins cause resp. smooth muscle to relax

Answer 14

PGE2, PGI2 = relax respiratory sm

Question 15

Which prostglandins cause resp. smooth muscle to contract

Answer 15

PGF2a

Question 16

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

Answer 16

PGE2, PGF2a

Question 17

Which prostaglanin causes circular muscle to relax

Answer 17

PGE2

Question 18

Which prostglandins cause vascular constriction in smooth muscle

Answer 18

-TXA2, PGF2a

Question 19

Which prostglandins cause vascular dilitation in smooth muscle

Answer 19

PGI2, PGE2

Question 20

Which prostaglandins cause uterine constriction

Answer 20

-PGE2, PGF2a, TXA2 = contract

Question 21

Which prostaglandins cause uterine dilatation

Answer 21

PGI2

Question 22

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

Answer 22

PGE2

Question 23

In asthma are the PGs or leukotirens more importat

Answer 23

eukotrienes are major mediators of asthma

Question 24

Which leukotrienes most important in asthma

Answer 24

LTC4, LTD4 pathologic for asthma

Bronchoconstriction, inc mucus secretion, increased vasc permeability

Question 25

Which prostglandin is major mediator of pain and fever

Answer 25

PGE2

Question 26

Which prostglanins mediate dysenorrhea

Answer 26

PGE2 and PGF2

Question 27

Which prostgladins regluate intraocular eye pressure

Answer 27

PGF2

Question 28

How to corticosteriods exert their effect

Answer 28

Corticosteriods reduce the activity of PLA2 and synthesis of COX2

Question 29

How does asprin exert its effect

Answer 29

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

Question 30

Whay are COX2 inhibitors associates with adverse cardiac effects

Answer 30

Inhibit PGI2 vasodilatory effects and get uninhibited COx1/TXA2 vasoconstrictio

Question 31

Which cell type ainly produces leukocytes

Answer 31

Leukotrienes

Question 32

Second messanger for leukotriene receptors

Answer 32

IP3 with a subsequent increase in [Ca2+]

Question 33

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

Answer 33

LTC4 and LTD4 ALso active in asthma

Question 34

Mechanism for asprine induced hypersensitivity asthma

Answer 34

Know that aspirin induced hypersensitivity asthma may be | exacerbated by diverting arachidonic acid to leukotrienes (LTC4 and LTD4)

Question 35

5 lipoxygebase inhibitor

Answer 35

Zileuton

Question 36

Leukotriene receptor antagonist

Answer 36

Zarfirlukast | Montelukast

Question 37

Misoprostol (Cytotex) - Use - Side Effect - Contraindications - BBW

Answer 37

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

Question 38

What is used to keep PDA open

Answer 38

PGE2

Question 39

What is used to close PDA

Answer 39

Ibuprofen | Indomethacin

Question 40

Iloprost (Ilomedin) - Use - Mechanism

Answer 40

FDA approved for pulmonary hypertension A stable second generation analog of prostacyclin

Question 41

Alprostadil - Mechanism - Side Effect

Answer 41

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%)

Question 42

Zileuton - Drug class - Mechanism - Indications

Answer 42

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. (

Question 43

Montelukast - Drug class - Mechanism

Answer 43

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)

Question 44

Dexamethason - Class - Mechanism of action - Indication

Answer 44

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..