Overview Therapeutic strategies for treating asthma include: decreasing inflammation increasing sympathetic tone There are 7 families of drugs that are commonly used: corticosteroids β-agonists muscarinic antagonists methylxanthines cromolyn antileukotrienes omalizumab Corticosteroids Inhaled corticosteroids are first line therapy for chronic asthma Examples mometasone fluticasone budesonide beclomethasone triamcinolone flunisolide Mechanism inhibiting the synthesis of virtually all cytokines upregulating expression of beta-adrenergic receptors inactivating NF-κB NF-κB is the transcription factor that induces the production of TNF-α and other inflammatory agents Toxicity oral candidiasis use spacers or post-inhalation mouth rinse to prevent β2-agonists Drugs short acting -- used for breakthrough symptoms and during acute exacerbation albuterol known internationally as salbutamol levalbuterol Others used much less commonly terbutaline metaproterenol (β2, minor β1) isoproterenol (nonselective) tachycardia may lead to cardiac death long acting -- used for maintenance in combination with inhaled corticosteroid (never without) salmeterol tremors, arrhythmia formoterol Mechanism β2 receptors are activated on bronchial smooth muscle to achieve bronchodilation stimulation of adenylate cyclase leading to closing of calcium channels and ultimately the relaxation of smooth muscles Methylxanthines Drugs theophylline (rarely used) Mechanism inhibition of phosphodiesterase leading to decreased cAMP hydrolysis causes bronchodilation metabolized by P-450 blocks actions of adenosine Toxicity seizures narrow therapeutic index nausea/vomiting arrhythmia Muscarinic antagonists Drugs ipratropium tiotropium Mechanism competitive inhibition of muscarinic receptors prevents bronchoconstriction Also used for COPD Cromolyn Prophylaxis only! ineffective during an acute asthma attack Mechanism prevents release of mediators from mast cells Toxicity rare Antileukotrienes Drugs zileuton 5-lipoxygenase pathway inhibitor blocks conversion of arachidonic acid to leukotrienes zafirlukast, montelukast blocks leukotriene receptors particularly effective in aspirin-induced asthma Omalizumab Clinical use severe uncontrolled asthma with elevated IgE symptoms and activity refractory to standard therapies and oral glucocorticoids Mechanism anti-IgE antibody inhibits action of IgE with inflammatory cells asthma can be caused by uncontrollably high IgE response
QUESTIONS 1 of 12 1 2 3 4 5 6 7 8 9 10 11 12 Previous Next Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK (M1.PL.15.106) An 8-year-old female is given omalizumab for the treatment of bronchial asthma. Omalizumab treats asthma through which mechanism? Tested Concept QID: 100909 Type & Select Correct Answer 1 Inhibition of IgE binding to mast cells 84% (57/68) 2 Binding to nuclear receptors 4% (3/68) 3 Inhibition of leukotriene binding to receptor 7% (5/68) 4 Inhibition of phosphodiesterase breakdown of cAMP 3% (2/68) 5 Mediating type IV hypersensitivity reaction 1% (1/68) M 1 Question Complexity D Question Importance Select Answer to see Preferred Response SUBMIT RESPONSE 1 Review tested concept Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK (M1.PL.14.33) In patients with chronic obstructive pulmonary disease, stimulation of muscarinic acetylcholine receptors results in an increase in mucus secretion, smooth muscle contraction and bronchoconstriction. The end result is an increase in airway resistance. Which of the following pharmacologic agents interferes directly with this pathway? Tested Concept QID: 100836 Type & Select Correct Answer 1 Epinephrine 2% (1/58) 2 Theophylline 2% (1/58) 3 Ipratropium 88% (51/58) 4 Albuterol 9% (5/58) 5 Metoprolol 0% (0/58) M 1 Question Complexity E Question Importance Select Answer to see Preferred Response SUBMIT RESPONSE 3 Review tested concept Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK (M1.PL.14.41) A 7-year-old boy is brought to your office with complaints of wheezing and dyspnea. Laboratory work reveals eosinophilia and positive skin tests for allergens. Which of the following types of drugs would be an effective treatment in this patient? Tested Concept QID: 100844 Type & Select Correct Answer 1 Beta-2 antagonist 16% (27/167) 2 Histone deacetylase inhibitor 7% (12/167) 3 VEGF inhibitor 5% (8/167) 4 Muscarinic antagonist 71% (119/167) 5 Anticoagulant 0% (0/167) M 3 Question Complexity E Question Importance Select Answer to see Preferred Response SUBMIT RESPONSE 4 Review tested concept (M1.PL.13.126) A new drug is designed to treat asthma by inhibiting bronchoconstriction. Experimental assays show that treated animals had markedly reduced acetylcholine binding to muscarinic receptors relative to untreated controls. The drug is most similar to which of the following: Tested Concept QID: 100929 Type & Select Correct Answer 1 Theophylline 8% (5/64) 2 Cromolyn 0% (0/64) 3 Zafirlukast 5% (3/64) 4 Prednisone 2% (1/64) 5 Ipratropium 84% (54/64) M 3 Question Complexity E Question Importance Select Answer to see Preferred Response SUBMIT RESPONSE 5 Review tested concept Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK (M1.PL.13.91) A 12-year-old female presents to her pediatrician with an asthma exacerbation. Upon physical examination, the physician notes the finding shown in Figure A. This presentation is a common side effect of which of the following pharmacologic agents used in the treatment of asthma? Tested Concept QID: 100894 FIGURES: A Type & Select Correct Answer 1 Salmeterol 3% (2/73) 2 Albuterol 5% (4/73) 3 Inhaled beclomethasone 84% (61/73) 4 Ipratropium 3% (2/73) 5 Theophylline 4% (3/73) M 3 Question Complexity E Question Importance Select Answer to see Preferred Response SUBMIT RESPONSE 3 Review tested concept Sorry, this question is for PEAK Premium Subscribers only Upgrade to PEAK