Pharmacology Final

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Author:
Rx2013
ID:
80757
Filename:
Pharmacology Final
Updated:
2011-04-19 20:53:05
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Respiratory Pharmacology
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Description:
Respiratory Pharmacology
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  1. Asthma has dramatically risen worldwide over the past decades, particularly in
    developed countries
  2. Not all people with asthma have
    allergies
  3. Asthma is most likely caused by
    • genetics
    • biologic triggers
    • infections
    • diet
    • hormonal changes
    • allergens
  4. 3 major characteristics of asthma
    • airway inflammation
    • airway obstruction
    • hyperresponsiveness of airways
  5. Severe persistant asthma
    Days with sx, nights with sx, FEV1, PEF
    • continual
    • frequent
    • <60%
    • >30%
  6. Moderate Persistant Asthma
    Days with sx, nights with sx, FEV1, PEF
    • Daily
    • >1x/week
    • 60-80%
    • >30%
  7. Mild persistent Asthma
    Days with sx, nights with sx, FEV1, PEF
    • >2x/week less than 1x/day
    • >2x/month
    • >80%
    • 20-30%
  8. Mild Intermittent Asthma
    Days with sx, nights with sx, FEV1, PEF
    • <2x/week
    • <2x/month
    • >80%
    • <20%
  9. Controller medications
    • corticosteroids
    • long acting beta agonists
    • leukotriene receptor modifiers
    • methylxanthines
    • immunomodulators: Anti-IgE
    • cromolyn and nedocrimil
  10. Quick relief medications
    • short acting beta agonists
    • systemic corticosteroids
    • anticholinergic agents
  11. Inhaled Beta 2-agonist
    • treatment of choice for mild asthma and acute exacerbations
    • smooth muscle relaxation
    • can prevent and reverse exercise induced bronchospasm
    • more effective on an "as needed" basis
  12. Beta 2-agonist onset of action and duration of action
    • onset = 10-15 min
    • max duration 4-6 hours
  13. Regular use (more than ___ canister(s) per month) is assocaited with diminished control of asthma.
    more than 1 canister per month
  14. Beta 2 Agonists relieve symptoms but do not control
    inflammation
  15. Side effects of Beta 2 Agonists
    • action on systemic B2 receptors result in increased HR, BP and EKG.
    • Tremor
    • Hypokalemia and hypomagnesemia with frequent use, especially in pts on thiazides
    • Hyperglycemia
  16. Metabolism and elimination of beta 2 agonists
    • metabolized by sulfotransferases
    • 80-100% eliminated through renal excretion
    • 20% eliminated in feces
  17. Methylxanthine (theophylline) mechanisms of action
    • decrease phosphodiesterase
    • increase cAMP
    • non-specific adenosine antagonist
  18. Theophylline is a ____ drug and ____ is essential.
    • low therapeutic index
    • monitoring blood levels
  19. Absorption and metabolism of theophylline
    • rapidly absorbed
    • distributed into fat free tissues
    • metabolized by the liver
    • short T1/2
  20. Conditions effecting Theophylline metabolism
    • fever
    • CHF
    • hepatic insufficiency
    • alcohol
    • neonates and adults >60 have decreased clearance
    • smokers and hyperthyroidism increased clearance
  21. Drugs that decrease clearance of theophylline
    • ticlopidine
    • erythromycin
    • disulfiram
  22. Drugs that increase clearance of theophylline
    • rifampin
    • phenytoin
    • phenobarbital
  23. Decreases absorption of theophylline
    food
  24. Theophylline level >20mcg/ml will cause
    • vomiting
    • arrhythmia
    • intractable seizures
  25. Cell types inhibited by inhaled corticosteroids
    • mast cells
    • eosinophils
    • basophils
    • neutrophils
    • macrophages
  26. Preferred drug of treatment for persistent asthma
    inhaled corticosteroids
  27. Mechanism of action for inhaled corticosteroids
    act locally in the lungs to inhibit cytokine production
  28. absorption and metabolism of inhaled corticosteroids
    • incomplete absorption
    • metabolized in the gut and liver
  29. ADEs with inhaled corticosteroids
    • hoarsness
    • thrush
    • thinning of skin and increased bruising
    • growth velocity slowed
    • cataracts
    • osteopenia in post menopausal pregnancy
  30. Leukotriene pathway
    • Arachidonic acid + 5-Lipoxygenase activating protein => Leukotriene A4.
    • LA4 + LC4 synthase => LC4
    • LC4 exits the cell and binds CysLT1 receptor
  31. Binding CysLT1 receptor results in
    • smooth muscle constriciton
    • eosinophil migration
    • edema
  32. Cys LT1 blockers
    • montelukast
    • pranlukast
    • zafirlukast
  33. 5-Lipoxygenase inhibitor
    Zileuton
  34. Leukotrine receptor antagonists (monteleukast and zafirlukast)
    • no known drug interactions
    • tablets
    • safe
    • once or twice daily dosing
    • not as predictable as inhaled corticosteroids
  35. Lipoxygenase inhibitor (ziluetin)
    • metablized by CYP2C9
    • Dosed 2-4x/day
    • drug drug interactions with warfarin, macrolides and theophylline
  36. Omalizumab
    • anti-IgE
    • only works in patients allergic to pollen or other seasonal identified causes

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