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5.11 Drugs acting on the respiratory system
Achievable USMLE/1
5. Pharmacology

Drugs acting on the respiratory system

Drugs used in the treatment of asthma

Drug Mechanism of action Adverse effects
Beta 2 agonists: albuterol, terbutaline, salmeterol, formoterol Relaxation of smooth muscle in the bronchi by stimulating bronchodilating beta 2 receptors, activation of adenylate cyclase, increased cAMP; Salmeterol and formoterol show greater specificity for beta 2 receptors Tremors, tachycardia, tolerance, cramps, salmeterol can increase the risk of severe asthma attacks and death
Corticosteroids (budesonide, beclomethasone, fluticasone, triamcinolone, prednisone, methylprednisone, prednisolone) Anti Inflammatory, reduce secretions and mucosal inflammation, decrease the severity and frequency of asthma attacks Oral candidiasis, cough, adrenal suppression, osteoporosis, growth suppression, peptic ulcers, myopathy, hypertension, Cushing’s syndrome
Methylxanthines (theophylline) Inhibits phosphodiesterase hence prevents the breakdown of cAMP, increases cAMP and cGMPlevels, bronchodilation, decreased release of inflammatory mediators from mast cells; adenosine receptor antagonist Narrow therapeutic index, tachycardia, arrhythmias, sudden death, CNS excitation, nervousness, insomnia, tremors, seizures, gastric upset
Cromolyn, nedocromil Inhibit release of inflammatory mediators from mast cells, suppression of leukocyte chemotaxis; Used to prevent asthma, prevent exercise and allergen induced bronchoconstriction Cough, unpleasant taste, dermatitis, myositis, generally well tolerated
Zileuton It inhibits the enzyme 5 lipoxygenase that is used in the synthesis of leukotrienes Headache, nausea, gastric upset, myalgia, Churg Strauss syndrome
Leukotriene modifiers (montelukast, zafirlukast) Antagonize the action of leukotriene on the airways by blocking leukotriene receptors; Effective in aspirin induced asthma also Headache, nausea, gastric upset, myalgia, Churg Strauss syndrome, elevation of liver enzymes
Muscarinic antagonists (ipratropium, tiotropium) Block muscarinic receptors in the airways, decrease bronchoconstriction and mucosal secretion Anticholinergic effects especially in elderly, cough, dry mouth, throat irritation, urinary retention, tachycardia, delirium, blurred vision
Monoclonal antibodies (omalizumab) It is a humanized recombinant monoclonal antibody to IgE that blocks the binding of IgE to mast cells, preventing degranulation Injection site reactions, risk of malignancies, rarely anaphylaxis, high cost
Stepwise therapy of asthma
Stepwise therapy of asthma

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