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2011-10-31 20:29:43
Eicosanoids Eicosanoid Antagonists

Eicosanoids and Eicosanoid Antagonists
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  1. Eicosanoids and their synthetic derivatives
    • 1. Dinoprostone (PGE2 synthetic)
    • 2. Misoprostol (PGE1 analog)
    • 3. Alprostadil (PGE1 synthetic)
    • 4. Epoprostenol/Treprostinil/Iloprost (PGI2 synthetic)
    • 5. Lubiprostone (PGE1 derivative)
    • 6. Latanoprost/Bimaprost/Travoprost (PGF2a analog/ester prodrug)
  2. Dinoprostone (PGE2)
    Mechanism: stimluates EP1 and/or EP3 receptors causing SM contraction

    Indications: midtrimester abortion, cervical ripening

    Adverse Effects: nausea, diarrhea, hypotension, fever
  3. Misoprostol (PGE1)
    Mechanism: stimulates EP3 receptors causing decreased gastric acid secretion, increased mucous and HCO3- secretion/stimulates EP1 receptors causing SM contraction

    Indications: NSAID-induced ulcer prophylaxis, termination of early pregnancy

    Adverse Effects: nausea, diarrhea, headache
  4. Alprostadil (PGE1)
    Mechanism: stimulates EP2 and/or EP4 receptors causing vasodilation

    Indications: ED, maintenance of patent ductus arteriosus in neonates prior to corrective surgery

    Adverse Effects: local reactions, hypotension, apnea
  5. Epoprostenol/Troprostinil/Iloprost (PGI2)
    Mechanism: stimulates IP receptors on vascular SM causing vasodilation

    Indications: pulmonary hypertension

    Adverse Effects: nausea, diarrhea, headache
  6. Lubiprostone (PGE1 derivatvie)
    Mechanism: stimulate EP4 receptors on GI epithelial cells causing increase in chloride channels and increased fluid and electrolyte secretion

    Indications: chronic constipation, IBS with constipation in women

    Adverse Effects: nausea, diarrhea, headache
  7. Latanoprost/Bimatoprost/Travoprost (PGF2a)
    Mechanism: Stimulate FP receptors causing increased drainage of aqueous humor

    Indications: chronic open-angle glaucoma

    Adverse Effects: darkening/discoloration of the iris, eyelashes and eyelids (permanent)
  8. tNSAIDs
    Ibuprofen(motrin, advil)
    Naproxen (aleve)
    Mechanism: inhibit Cox, causing antipyretic, analgesic and anti-inflammatory effects

    Indications: mild to severe pain, fever, osteoarthritis, RA, dysmenorrhea, migraine, cardioprotection (low dose aspirin)

    Adverse Effects: gastric or intestinal ulcers, increased renal blood flow and filtration in renal problems, stimulates gestation?, hypersensitivity reactions

    Other: aspirin irreversibly binds COX
  9. tNSAIDS
    Mechanism: inhibits COX causing antipyretic, analgesic effects

    Indications: mild to severe pain, fever, osteoarthritis

    Adverse Effects: hepatotoxicity

    Other: minimal anti inflammatory effects
  10. Selective COX-2 inhibitors
    Celecoxib (celebrex)
  11. Celecoxib (celebrex)
    Mechanism: inhibits COX-2 causing antipyretic, analgesic and anti-inflammatory effects

    Indications: moderate to severe pain, osteoarthritis, RA

    Adverse Effects: GI side effects but less than with tNSAIDS

    Other: potential risk of thromboembolic events due to inhibiton of COX2 in endothelial cells (decrease PGI2 synthesis)
  12. Lipoxygenase Inhibitors
  13. Zileuton
    Mechansim: inhibits 5-LOX

    Indications: asthma

    Adverse Effects: Hepatotoxicity

    Other: prophylactic ONLY
  14. LT recepter antagonists
    • 'lukasts'
    • Zafirlukast
    • Montelukast (singulair)
  15. Zafirlukast
    Montelukast (Singulair)
    Mechansim: block CysLT1 receptors

    Indications: Asthma, allergic rhinitis

    Other: prophylactic use ONLY
  16. Corticosteroids
    Mechanism: induces synthesis of annexins (inhibit PLA2, decrease synthesis of eicosanoids), down regulate COX-2 expression, decrease synthesis and relase of cytokines, decrease extravasation of leukocytes

    Indications: asthma, RA, acute inflammatory reactions

    Adverse Effects: susceptibility to infections, osteporosis, diabetes, weight gain

    Other: long term use leads to adrenal suppression so withdrawal must be gradual, inhalation administration for asthma can decrease side effects