EICOSANOIDS PART II

increase the rate of longitudinal contraction in the gut and decrease transit time.

Response of PGF2 in gastro-intestinal tract

Cytoprotectant-inhibit acid and pepsinogen secretion in the stomach

Response of PGE2 in gastro-intestinal tract

PGE2 & PGI2: Inhibit platelet aggregation

TXA2: Induce platelet aggregati

Inhibit platelet aggregation and Induce platelet aggregation

Differentiates them on the Site of action of eicosanoids

5-HPETE: Stimulate release

PGD2 & PGI2: Inhibits release

Stimulate release

Inhibits release

Differentiates them on the Site of action of eicosanoids

Increase body temperature

Response of PGE2 in CNS fever

PGD2: Induces natural sleep

PGE2: Wakefulness

Induces natural sleep

Wakefulness

Differentiates them on the Site of action of eicosanoids

Derivatives can lower intraocular pressure

Response of PGE and PGF in Eyes

Carboprost

PGF2 analogue - induces labor at second trimester

Carboprost and Mifepristone (RU486)

With this drug combined it will cost the therapeutic abortion to induce labor

Epoprostenol (Flolan)

Iloprost (Ventavis)

Treprostinil (Remodulin)

PGI2 analogue and Management of Pulmonary hypertension

Alprostadil (Caverject)

Misoprostol (Cytotec)

PGE1 analogue

Alprostadil (Caverject)

Management of erectile dysfunction and used in patient with patent ductus arteriosus

Intracavernosal injection (the base of the penis) or urethral suppository

Alprostadil (Caverject) is based on what route of administration

Dinosprostone (Previdil, Cervidil)

PGE2 analogue

Latonoprost (Xalatan)

PGF2A analogue

Misoprostol (Cytotec)

Used as cytoprotectant

⏤ approved for use in patients taking high doses of nonsteroidal anti-inflammatory drugs (NSAIDs) to reduce gastric ulceration.

Uterine contraction (Abortificient)

Misoprostol A/E

Dinoprostone (Prepidil, Cervidil)

Used for abortion and cervical ripening

combined with mifepristone (RU486) to induce first-trimester abortion.

Latanoprost (Xalatan)

Used in the management of glaucoma

irreversible brown pigmentation of the iris and eyelashes

Latanoprost (A/E)

Corticosteroids; Inhibiting the Phospholipase A2

5-LOX inhibitor: Zileuton (Zyflo)

Leukotriene antagonist: Montelukast, Zafirlukast

Thromboxane synthesis inhibitor: Dazoxiben

NSAID: Non-selective COX inhibitor

COX-2: Coxib

Eicosanoids syntehsis of Inhibitors

Peptic ulcer disease

Most common side effect of NSAID:

Increase platelet aggregation (led to heart attack and stroke)

Most common side effect of COX-2 inhibitors

Linoleic acid

Eicosapentaenoic and Docosahexanoic acid

Changing the phospholipid composition of cell membranes by replacing arachidonic acid with the dietary fatty acids

Linoleic acid

Found in corn, safflower, and sunflower oils

Eicosapentanoic and Docosahexanoic acid

called omega-3 fatty acids

from cold-water fish

reduction in the incidence of myocardial infarction and sudden cardiac death

protect against experimentally induced arrhythmogenesis, platelet aggregation, vasomotor spasm, and dyslipidemias.

Dietary use of the dietary fatty acid.