#1 Eicosanoids (Pharm) 9/1/06

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Eicosanoids are a diverse group of molecules mainly derived from?

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arachidonic acid

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arachidonic acid is produced from?

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membrane phospholipids

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arachidonic acid is produced by the action of?

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phospholipase A2

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eicosanoids termed?

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autocrine regulators (local hormones)

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eicosanoids include?

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1) prostaglandins
2) thromboxanes
3) leukotrienes

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eicosanoids regulate?

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1) inflammation
2) pain reception
3) blood flow
4) smooth muscle contraction

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eicosanoids are produced in?

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very small amounts, and have short half-lives

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prostaglandins are?

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1) arachidonic acid derivatives
2) contain a cyclopentane ring

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action of prostaglandins?

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1) inflammation
2) reproductive processes
3) digestion

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thromboxanes contain?

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a cyclic ether group

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leukotrienes are?

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noncyclic (linear)

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leukotrienes are known to be components of?

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SRS-A (slow releasing substance of anaphylaxis)

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PG-D2

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1) vosodilation (low [ })
2) vosoconstriction (high [ ])
3) bronchial muscle contraction
4) renin secretion
5) inhibit plt aggregation

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PG-D2 causes only vasoconstriction in the?

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pulmonary circulation

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PG-Es

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1) potent vasodilation
2) < BP
3) > blood flow to heart and kidney
4) inhibit B-lymp proliferation & differentiation to plasma cells
5) inhibit IL-1 & T cell proliferation

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PG-Es

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1) relax bronchial muscle
2) contracts uterine and intestinal smooth muscle
3) > body temp
4) hyperalgesia
5) inhibit gastric secretion
6) > GI mucus secretion

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PG-F2

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1) constrict pulm vessels
2) contracts bronchial muscle
3) contract uterine & GI muscles

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PG-I2 (prostacyclin)

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1) inhibit plt aggregation
2) cause hypotension
3) vasodilation
4) relax uterine tone
5) cytoprotectant

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TX-A2

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1) plt aggregation
2) vasoconstriction
3) bronchoconstriction

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TX-A2 is produced by?

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platelets

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LT-B4

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1) leukocyte chemotaxis
2) hyperalgesia
3) stimulate Bcell proliferation

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LT-C4 & LT-D4

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1) bronchoconstrictors
2) > microvascular permeability, plasma exudation, mucus secretion

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12 HPETE

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function as NTM

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12 HETE

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1) stimulates migration of aortic smooth muscle cells
2) chemotactic factor

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prostaglandins in OB

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1) 1st & 2nd trimester abortion
2) Carboprost (IM)
3) Dinoprostone (intravag)
4) induction of labor
5) control postpertum uterine atony and hemorrhage

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PTG in pediatrics

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1) maintain patency of ductus arteriosus
2) Alprostadil (IV gtt)

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PTG in impotence

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vasodilation with penile injection (Alprostadil)

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PTG in GI

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cytoprotection of the stomach in pts with on NSAIDS
(Misoprostol)

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PG-I2 used to prevent plt aggregation in?

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dialysis machines

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Misoprostol (Cytotec)

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1) synth. oral PG-E1 analog
2) prevent ulcers

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SE of Misoprostol

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1) transient diarrhea
2) C/I in pregnant pts

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Dinoprostone (Cervidil, Prostin E2 suppository, Prepidil gel)

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1) synth. PG-E2 analog
2) terminate pregnancy
3) facilitate labor

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SE of Dinoprostone

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1) vomiting
2) diarrhea
3) transient fever

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Carboprost tromethamine (Hemabate)

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1) synth. derevatives 15-methyl-PG-F2alpha
2) induce abortion
3) control postpartum hemorrhage

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SE of Hemabate

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1) N/V
2) diarrhea
3) transient pyrexia
4) hypotension with large dose

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Alprostadil (Prostin VR pediatric)

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1) naturally occuring form of PG-E1
2) maintain a patent ductus arteriosus

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SE of Alprostadil

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1) apnea (10-12%)
2) fever, flushing, hypotension, bradycardia, Sz, diarrhea, cardiac arrest

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Alprostadil penile injection (Caverject)

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1) naturally occuring form of PG-E1
2) for impotence

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Sildenafil (Viagra)

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1) not a PG preparation
2) increase blood flow in the corpus cavenorsum

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Viagra is contraindicated with?

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organic nitrate vasodilators
(ex) Nitrous = < BP

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Epoprostenol (Folan, Cycloprostin)

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1) PG-F analog
2) prevent plt aggregation in dialysis machine
3) for pulmonary HTN

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Latanaprost (Xalatan)

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1) analog of PG-F2 alpha
2) eye drop, for > IOP

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Montelukast (Singulair)

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1) leukotriene blocker
2) antiasthmatic
3) Zamfirlukast (Accolate)

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Zileuton (ZyFlo)

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1) inhibitor of 5-lipoxygenase
2) for asthma