Eicosinoids

  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
    Aspirin
    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
    Acetaminophen
    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
    Zileuton
  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
    -Hydrocortisone
    -Dexamethasone
    -Prednisone
    -Beclomethasone
    -Flucticasone
    -Triamcinolone
    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
Author
jknell
ID
113492
Card Set
Eicosinoids
Description
Eicosanoids and Eicosanoid Antagonists
Updated