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Pharmacology

       Drugs used to treat:
            Asthma
        Rhinitis & Cough
Topics
• Bronchodilators         •   Decongestants
• Methylxanthines         •   Antihistamines
• Anticholinergics        •   Antitussives
• Anti-inflammatory       •   Expectorants &
  Agents                      mucolytics
• Leukotriene
  Antagonists
• Mast cell stabilizers
Asthma
• Inflammatory response to allergen
• Antibody binds with & ruptures mast cells
  – Releases histamine, prostaglandins,
    leukotrienes
• Two primary issues
  – Bronchoconstriction
  – Inflammation (mucous production)
Approaches to Treatment
• Relax bronchial smooth muscle
   – ß2 agonists
   – methylxanthines
   – anticholinergics
• Inhibit release of mediators
   – Glucocorticoids
   – Mast cell stabilizers
• Block affects of mediators
   – Leukotriene antagonists
Bronchodilators
ß2 agonists        albuterol (Proventil®),
                   metaproterenol (Alupent®)
                   terbutaline (Breathair®)
Nonselective       epinephrine (Adrenalin®)
Methylxanthines    theophylline (TheoDur®)
                   aminophyllin, (Aminophylline®)
Anticholinergics   ipratropium bromide (Atrovent®)
Antiinflammatory Agents
Glucocorticoids
                          inhaled beclomethasone (Beclovent®)
                                 flucticasone (Flovent®)
                            oral prednisolone (Deltasone®)


                       injected methylprednisolone (Solu-Medrol®)
                                 dexamethasone (Decadron®)
Mast cell Stabilizer             cromolyn (Nasalcrom®, Intal®)


Leukotriene Antagonists          zafirlukast (Accolate®)
                                 zileuton (Zyflo®)
Colds and Allergies
• Nasal Inflammation
  – Vasodilation & engorgement
• Itching, redness, rhinorrhea
  – Mast/basophil degranulation
Nasal Decongestants
∀ ⇓ congestion via            • phenylephrine (Neo-
  vasodilation                  Synephrine®)
• Alpha1 stimulation          • pseudoephedrine
   – Topical administration     (Sudafed®, Actifed®)
                              • A moment of silence
                                for:
                                 – phenylpropanolamine
                                   (AlkaSeltzer Cold®,
                                   Contact®, Allerest®)
Antihistamines
• H1 receptors               • Other histamine
   – Vasodilation              receptors
   – Increased capillary       – Sedation
     permeability
   – Bronchoconstriction
• H2 receptors
   – Increase gastric acid
     secretion (Zantac®),
     etc)
Antihistamine Agents
• First generation       • Second generation
   – Sedation               – No sedation
• chlorpheniramine          – blood-brain barrier
  (Chlor-Trimeton®)      • Sniff, sniff:
• diphenhydramine           – terfenadine (Seldane®)
  (Benadry®)             • fexofenadine
• clemastine (Tavist®)     (Allegra®)
• promethazine           • cetirizine (Zyrtec®)
  (Phergan®)             • loratadine (Claritin®)
Cough Suppressants
• Antitussives                  • Expectorants
   – Decrease cough reflex        – guaifenesin may work
   – Opioids                      – others are doubtful
      • codeine & hydrocodone   • Mucolytics
   – Non-opioids                  – Decreases viscocity
      • dextromethorphan
                                  – acetlycysteine
      • benzonatate
        (Tessalon®)                 (Mucomyst®)
                                  – hypertonic saline

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Respiratoy drugs

  • 1. Pharmacology Drugs used to treat: Asthma Rhinitis & Cough
  • 2. Topics • Bronchodilators • Decongestants • Methylxanthines • Antihistamines • Anticholinergics • Antitussives • Anti-inflammatory • Expectorants & Agents mucolytics • Leukotriene Antagonists • Mast cell stabilizers
  • 3. Asthma • Inflammatory response to allergen • Antibody binds with & ruptures mast cells – Releases histamine, prostaglandins, leukotrienes • Two primary issues – Bronchoconstriction – Inflammation (mucous production)
  • 4. Approaches to Treatment • Relax bronchial smooth muscle – ß2 agonists – methylxanthines – anticholinergics • Inhibit release of mediators – Glucocorticoids – Mast cell stabilizers • Block affects of mediators – Leukotriene antagonists
  • 5. Bronchodilators ß2 agonists albuterol (Proventil®), metaproterenol (Alupent®) terbutaline (Breathair®) Nonselective epinephrine (Adrenalin®) Methylxanthines theophylline (TheoDur®) aminophyllin, (Aminophylline®) Anticholinergics ipratropium bromide (Atrovent®)
  • 6. Antiinflammatory Agents Glucocorticoids inhaled beclomethasone (Beclovent®) flucticasone (Flovent®) oral prednisolone (Deltasone®) injected methylprednisolone (Solu-Medrol®) dexamethasone (Decadron®) Mast cell Stabilizer cromolyn (Nasalcrom®, Intal®) Leukotriene Antagonists zafirlukast (Accolate®) zileuton (Zyflo®)
  • 7. Colds and Allergies • Nasal Inflammation – Vasodilation & engorgement • Itching, redness, rhinorrhea – Mast/basophil degranulation
  • 8. Nasal Decongestants ∀ ⇓ congestion via • phenylephrine (Neo- vasodilation Synephrine®) • Alpha1 stimulation • pseudoephedrine – Topical administration (Sudafed®, Actifed®) • A moment of silence for: – phenylpropanolamine (AlkaSeltzer Cold®, Contact®, Allerest®)
  • 9. Antihistamines • H1 receptors • Other histamine – Vasodilation receptors – Increased capillary – Sedation permeability – Bronchoconstriction • H2 receptors – Increase gastric acid secretion (Zantac®), etc)
  • 10. Antihistamine Agents • First generation • Second generation – Sedation – No sedation • chlorpheniramine – blood-brain barrier (Chlor-Trimeton®) • Sniff, sniff: • diphenhydramine – terfenadine (Seldane®) (Benadry®) • fexofenadine • clemastine (Tavist®) (Allegra®) • promethazine • cetirizine (Zyrtec®) (Phergan®) • loratadine (Claritin®)
  • 11. Cough Suppressants • Antitussives • Expectorants – Decrease cough reflex – guaifenesin may work – Opioids – others are doubtful • codeine & hydrocodone • Mucolytics – Non-opioids – Decreases viscocity • dextromethorphan – acetlycysteine • benzonatate (Tessalon®) (Mucomyst®) – hypertonic saline