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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)
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Dinoprostone (PGE2)
Mechanism: stimluates EP1 and/or EP3 receptors causing SM contraction
Indications: midtrimester abortion, cervical ripening
Adverse Effects: nausea, diarrhea, hypotension, fever
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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
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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
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Epoprostenol/Troprostinil/Iloprost (PGI2)
Mechanism: stimulates IP receptors on vascular SM causing vasodilation
Indications: pulmonary hypertension
Adverse Effects: nausea, diarrhea, headache
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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
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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)
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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
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tNSAIDS
Acetaminophen
Mechanism: inhibits COX causing antipyretic, analgesic effects
Indications: mild to severe pain, fever, osteoarthritis
Adverse Effects: hepatotoxicity
Other: minimal anti inflammatory effects
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Selective COX-2 inhibitors
Celecoxib (celebrex)
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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)
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Lipoxygenase Inhibitors
Zileuton
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Zileuton
Mechansim: inhibits 5-LOX
Indications: asthma
Adverse Effects: Hepatotoxicity
Other: prophylactic ONLY
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LT recepter antagonists
- 'lukasts'
- Zafirlukast
- Montelukast (singulair)
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Zafirlukast
Montelukast (Singulair)
Mechansim: block CysLT1 receptors
Indications: Asthma, allergic rhinitis
Other: prophylactic use ONLY
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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
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