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29 Cards in this Set
- Front
- Back
Patient's responsibility in control of asthma.
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ADHERENCE
-medication must be taken as directed to be effective |
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Asthma
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Chronic inflammatory disorder of the airways
(Nuetrophils, Eosinophils, Lymphocytes infiltation) Epithelial cell injury and mass cell activation |
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Mechanisms of Allergy in Asthma
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Allergen exposure, lympocyte IL-4 production signals b cells to product IgE, activate mass cells, mass cells degranulation release mediators (Histamine, LTs, PGs, bradykinin), leads to inflammation in late phase.
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Early Allergic Reaction
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Decease FEV1 in minutes (lasts 1.5-2 hours)
Acute airway obstruction. |
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Late Allergic Reaction
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Another decrease in FEV1 about 2-8 h after exposure
Cytokines released from mast cells Lasts days to weeks. |
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MOA of Beta2 agonists
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Bind receptor, active adenylate cyclase increasing cAMP. Actives protein kinases affecting myosin light chain kinase and Ca++ dependent K+ channels... Bronchodilation
May also enhance mucociliary clearance, reduce mucosal edema, decrease mediator release, weak antiinflammatory NO effect on late response or on airway hyperresponsiveness. |
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Beta2 agonists
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Albuterol (onset within 5 min) last 3-6 hours
Salmeterol (onset 10-15 min) last 12 hours. Formoterol (onset 2-3 min) last 12 hours. All inhaled. |
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SABA Indications
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Best agent for exercise-induced asthma
Treatment of choice for mild intermittent asthma and acute exacerbation of asthma with systemic steroids COPD maintenace and exacerbations (often combined with anticholinergic agents) |
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LOBA Indications
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(Salmeterol, Formoterol)
Maintenace treatment of asthma, COPD, and EIA. Never use as monotherapy (add to ICS theapy) |
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B2 Agoinists Adverse effects
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CNS
Nervousness, irritability, insomnia Skeletal muscle tremor – ß2 manifestation Tolerance develops Heart – ß1 manifestation Palpitations, tachycardia, arrhythmias Paradoxical bronchospasm Regular or too frequent dosing |
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Parasympathetic effect on bronchioles
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Parasympathetic stimulation of muscarinic receptors – airway mostly M3 receptor
Increased cholinergic tone Increased bronial smooth muscle tone and mucus secretion |
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Anticholinergics for Asthma
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Ipratropium (Atrovent)
Tiotropium -once daily doing (Atrovent 4x/day) Combination albuterol/ipratropium. |
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Anticholinergics Indications
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FDA-approved for COPD
-may be better than B2 agonists. Non-FDA approved for asthma |
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Methylxanthines
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Theophyllin (caffeine, theobromine are natural alkaloids)
Low therapeutic index |
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Methylxanthine effects
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Pulmonary – theophylline > caffeine
Nonspecific phosphodiesterase inhibitor that increases intracellular cAMP Airway smooth muscle relaxation – Bronchodilation CNS effect – caffeine > theophylline Increased alertness, reduced fatigue Respiratory stimulant Nervousness, insomnia Cardiovascular effect Positive inotropic & chronotropic GI effects Increased gastric acid secretion Decreased LES pressure Renal effect – Weak diuretic Increased GFR Decreased tubular Na+ reabsorption Tolerance develops Improvement of diaphragmatic contractility May be important in COPD patients |
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Theophylline Why not used
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Less effective than B2 agonists
Metabolized by CYP450. Significant does-related side effects. >30 mcg/mL CNS stimulation & seizures |
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Anti-Inflammatory Agents for Asthma
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Corticosteroids
Mass cell stabilizers Leukotriene modifiers |
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Effects of corticosteroids in asthma
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Block late-phase reation
Reduce mucus secretion Increases B receptors |
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Corticosteroids for Asthma
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Fluticason (Flovent)
Triamcinole |
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Combination drugs for Asthma
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Fluticasone/Salmeterol (Advair) 1 inhal q12h
Budesonide/Formoterol (Symbicort) 2 inhal q12h. |
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Cromolyn
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Mast Cell Inhibitors
Not used very often mild potency anti-inflammatory agent, NOT a bronchodilator. |
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Leukotrienes Overview
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CYSTEINYL LTs – LT C4, D4 & E4
Formerly known as slow reacting substance of anaphylaxis (SRS-A) Very potent bronchoconstrictors & inflammatory mediators 1000 x > bronchospasm potency as histamine ACTIONS OF LTS Contract airway smooth muscle Increase vascular permeability (edema) Increase mucus secretions Decrease mucociliary clearance Recruit & activate eosinophils and basophils into airway Proliferation of smooth muscle |
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Zileuton
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5-lipooxygenase inhibitor
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Montelukast and Zafirlukast
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Cysteinyl LT receptor antagonists)
Montelukast (Singulair) Alternative, not preferred, treatment. Modest improvement in lung function as monotherapy. |
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Omalizumab
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Monoclonal Ab that binds IgE
-decrease free IgE in serum Allergy should be established by skin or blood test. Consider for severe persistent asthma (very expensive) |
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Asthma Classification
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COPD
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4th leading cause of death in US
Pharmacotherapy has not improved mortality, but does reduce symptoms and complications Smoking cessation and O2 most helpful to improve mortality. |
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Therapy for COPD
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Smoking cessation
Bronchodilator therapy Inhaled are preferred Methylxanthines Corticosteroids Treatment of Alpha-1 antitrypsin deficiency Influenza and pneumonia vaccination Oxygen supplementation Pulmonary rehabilitation Lung volume reduction surgery |
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COPD Management
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