Pharm- HEENT; MCS, ophthalmic,aptamers

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merazar15
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221246
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Pharm- HEENT; MCS, ophthalmic,aptamers
Updated:
2013-05-26 19:17:03
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Pharm HEENT
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Mast cell stabilizers, ophthalmic prostaglandins, aptamers
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  1. Mast cell stabilizers:
    inhibit allergic responses by preventing degranulation of mast cells
  2. Mast cell stabilizer drugs:
    • Cromolyn (Gastrocrom)
    • Cromolyn (NasalCrom)- nasal
    • Cromolyn (Crolom)
    • (Intal) Cromolyn -inhaled- brand DC’d
    • (Alocril) Nedocromil- ophthalmic
    • (Alomide) Lodoxamide- ophthalmic
  3. MOA of mast cell stabilizers
    • allergen leads to degranulation of mast cells
    • degranulation leads to release of proinflam factors (histamine, leukotrienes, &       cytokines)
    • work by preventing degranulation
  4. Indication of mast cell stabilizers:
    • Conditions with an allergic component
    • -Asthma* (not useful in acute attacks)
    • -rhinitis
    • -conjunctivitis
    • Mastocytosis
  5. SE    
    Cromolyn (nasal)-    
    Cromolyn (ophthalmic)-
    • Cromolyn (nasal)- sneezing, burning, nose bleeds, bad taste
    • Cromolyn (ophthalmic)- eye irritation; burning, dry, watery, itchy eyes
  6. Indication for Ophthalmic prostaglandins:
    • Glaucoma
    • eyelash hypotrichosis
  7. Ophthalmic prostaglandin drugs:
    • Latanoprost (Xalatan)
    • Travoprost (Travatan) (Travatan Z)
    • Bimatoprost (Lumigan) (Latisse)
    • Tafluprost (Zioptan)
  8. Strategies to reduce IOP:
    • Decrease production & secretion of aqueous humor
    • Facilitate drainage of aqueous humor
  9. Glaucoma characterized by increased IOP can lead to:
    Blindness, if left untreated
  10. Drainage occurs via:
    • Schlemm’s  canal (80-90%)
    • Uveoscleral route (10-20%)
  11. Prostaglandins bind to receptors on the ciliary muscle & reduce IOP by:
    by increasing aqueous humor outflow through the uveoscleral route
  12. Kinetics of ophthalmic prostaglandins:
    administered topically
  13. SE
    • foreign body sensation
    • burning
    • blurred vision
    • hyperpigmentation of iris & eyelids
    • dry eyes
    • excessive tearing
    • photophobia
    • hyperemia
    • macular edema
    • punctate epithelial keratitis
  14. other pharm for glaucoma:
    • BB: Timolol, Betaxolol, Metipranolol
    • Alpha agonists: Brimonidine
    • Parasympathomimetics: Carbachol, Pilocarpine
    • Carbonic anhydrase inhibitors: Dorzolamide, Brinzolamide
  15. Aptamers:
    • DNA or RNA molecules that bind to target molecules
    • (These molecules have many potential uses in medicine)
  16. Indication for aptamers
    Age related Macular degeneration
  17. What is Age related Macular degeneration?
    • an incurable eye dz
    • an overgrowth of blood vessels in the macula; these blood vessels function              poorly & may leak, leading to impaired vision & eventually degeneration of the macula & blindness·
    • VEGF bolsters new blood  vessel growth & increases vessel permeability
  18. Aptamer drugs:
    Pegaptanib (Macugen):  1st aptamer approved for human use. Binds to VEGF (vascular endothelial growth factor) a protein

    Ranibizumab (Lucentis)
  19. MOA of Aptamers:
    By binding to VEGF, pegaptanib inhibits proliferation of blood vessels and reduces blood vessel leakage
  20. Kinetics of Aptamers:
    • Injected directly into the eye vitreous
    • Slowly reaches systemic circulation after injection
  21. SE of Aptamers:
    • mostly due to injection
    • Increased IOP (injecting a volume of fluid into an enclosed space)
    • Floaters (air bubbles from injection)
    • Infection of eye (endophthalmitis)
  22. CI of Aptamers:
    Ocular infection

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