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Pharm Chapter46

Integrative Inflammation Pharmacology: Asthma

QuestionAnswer
Anticholinergics Ipratropium, Tiotropium
MOA ipratropium, tiotropium Antagonists at muscarinic receptors on airway smooth muscle and glands, leading to decreased bronchoconstriction and mucus secretion
Clinical applications ipratropium, tiotropium asthma, COPD
Adverse effects ipratropium, tiotropium dry mouth, constipation
Clinical applications epinephrine asthma, anaphylaxis, cardiac arrest
Adverse effects epinephrine cardiac arrhythmias, hypertensive crisis, pulmonary edema, tachycardia, palpitations, sweating, nervousness
Epinephrine selective or nonselective? Nonselective binds to alpha(causes hypertension) , beta-1(causes cardiac stimulation, and beta-2 adrenergic receptors
Clinical applications isoproterenol Asthma (Stimulates both beta-1 and beta-2 receptors and therefore causes both bronchodilation and cardiac stimulation)
Adverse effects isoproterenol tachyarrhytmia, tremor
Clinical applications isoetharine, metaproterenol, terbutaline, albuterol, levalbuterol, pirbuterol, bitolterol asthma (these are selective agonists at beta-2 receptors, cause fewer cardiac effects)
Clinical applications formoterol, salmeterol asthma (long acting beta-2 agonists; salmeterol not used for acute asthma attacks due to slow onset of action)
Methylxanthines Theophylline, Aminophylline
MOA theophylline, aminophylline nonselective phosphodiesterase inhibitors that prevent the degradation of cAMP; also act as adenosine receptor antagonists. The combined effect is smooth muscle relaxation and bronchodilation
Clinical applications theophylline, aminophylline asthma (inhibition of PDE III and V in smooth muscle results in bronchodilation, inhibtion of PDE IV in T cels and eosinophils causes an immunomodulatory and anti-inflammatory effect)
Adverse effects theophylline, aminophylline Both- ventricular arrhythmia, seizure, tachyarrhythmias, vomiting, insomnia, tremor, restlessness; theophylline- tachycardia and psychomotor agitation, @supratheraputic doses: gastric acid secretion and diuresis, @even higher doses: brain damage
Inhaled corticosteroids Beclomethasone, triamcinolone, fluticasone, budesonide, flunisolide, mometasone, ciclesonide
MOA inhaled corticosteroids Inhibit COX-2 action and prostaglandin biosynthesis by inducing lipocortins, activating endogenous anti-inflammatory pathways; inibition of IL-4 and IL-5
Clinical applications inhaled corticosteroids Asthma
Adverse effects inhaled corticosteroids osteopenia and osteoporosis, oropharyngeal candidiasis
MOA cromolyn, nedocromil inhibit chloride ion transport, which in turn affects calcium gating to prevent granule release, possibly decreasing mast cel response to inflammatory stimule
Clinical applications cromolyn, nedocromil Asthma, mast cell disorder (useful in patients with exercise-induced asthma, more effective in children and young adults)
MOA zileuton inhibits 5-lipoxygenase, thereby decreasing synthesis of leukotrienes
MOA montelukast and zafirlukast Leukotriene receptor antagonists
Clinical application zileuton, montelukast and zafirlukast asthma, allergic rhinitis
Adverse effects zileuton, montelukast, zafirlukast Churg-Strauss syndrome Zileuton - Hepatic toxicity (Monitor LFTs)
MOA omalizumab antibody against the high-affinity IgE-receptor (FceRI)-binding domain on human IgE. Prevents IgE from binding to FceRI on mast cells and APCs; also, decreases the quantity of cirulating IgE; all leads to decrease in allergic response in asthma.
Clinical application omalizumab asthma
Adverse effects omalizumab extremely rare anaphylactic reactions
Created by: 7958184
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