Pulmonary Medications PDF

Pulmonary Drugs for Asthma and Chronic Obstructive Pulmonary Disease Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Overview of Drugs for Asthma and COPD Two main pharmacologic classes Anti-inflammatory agents Glucocorticoids...

Pulmonary Drugs for Asthma and Chronic Obstructive Pulmonary Disease Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Overview of Drugs for Asthma and COPD Two main pharmacologic classes Anti-inflammatory agents Glucocorticoids (prednisone) Bronchodilators Beta2 agonists (albuterol) 2 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Inhalation Drug Therapy Three obvious advantages Therapeutic effects are enhanced Systemic effects are minimized Relief of acute attacks is rapid Three types Metered-dose inhalers (MDIs) Respimats Dry-powder inhalers (DPIs) Nebulizers 3 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs Foundation of asthma therapy Taken daily for long-term control Principal anti-inflammatory drugs are the glucocorticoids (for example, budesonide, fluticasone) 4 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Mechanism of action Considered the most effective antiasthma drugs available Decrease synthesis and release of inflammatory mediators Reduce infiltration and activity of inflammatory cells Decrease edema of the airway mucosa caused by beta2 agonists Usually administered by inhalation, but IV and oral routes are also options Mechanism of action = suppress inflammation Reduce bronchial hyperreactivity and decrease airway mucus production May increase the number of bronchial beta2 receptors and their responsiveness to beta2 agonists 5 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Use Prophylaxis of chronic asthma Dosing must be on a fixed schedule, not as needed (PRN) Not used to abort an ongoing attack because beneficial effects develop slowly 6 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Inhaled use First-line therapy for management of inflammatory component of asthma Most patients with persistent asthma should use these drugs daily Inhaled glucocorticoids are very effective and much safer than systemic glucocorticoids 7 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Oral use For patients with moderate to severe persistent asthma or for management of acute exacerbations of asthma or COPD Potential for toxicity; should be used only when symptoms cannot be controlled with safer medications (inhaled glucocorticoids, inhaled beta 2 agonists) Treatment should be as brief as possible 8 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Adverse effects of inhaled forms Adrenal suppression Oropharyngeal candidiasis Dysphonia Glucocorticoids can slow growth in children and adolescents; however, these drugs do not decrease adult height Promotion of bone loss Increased risk of cataracts Increased risk of glaucoma 9 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Adverse effects of oral forms Short-term therapy Long-term therapy Adrenal suppression Osteoporosis Hyperglycemia Peptic ulcer disease In young patients: Growth suppression 10 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Adrenal suppression Prolonged glucocorticoid use can decrease the ability of the adrenal cortex to produce glucocorticoids of its own Life-threatening at times of severe physiologic stress (for example, surgery, trauma, or systemic infection) High levels of glucocorticoids are required to survive severe stress Adrenal suppression prevents production of endogenous glucocorticoids Patients must be given increased doses of oral or IV glucocorticoids at times of stress Failure to do so can prove fatal 11 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Glucocorticoids Adrenal suppression Discontinuing treatment Must be done slowly Recovery of adrenocortical function takes several months Dosage of exogenous sources must be reduced gradually During this time, patients ‒ including those switched to inhaled glucocorticoids ‒ must be given supplemental oral or IV glucocorticoids at times of severe stress 12 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Leukotriene Modifiers Suppress effects of leukotrienes Leukotrienes: Promote smooth muscle constriction, blood vessel permeability, and inflammatory responses through direct action and recruitment of eosinophils and other inflammatory cells In patients with asthma, leukotriene modifiers can reduce bronchoconstriction and inflammatory responses such as edema and mucus secretion 13 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anti-Inflammatory Drugs: Leukotriene Modifiers Second-line agents Generally well tolerated but can cause adverse neuropsychiatric effects, including depression, suicidal thinking, and suicidal behavior Available agents Zileuton [Zyflo] Zafirlukast [Accolate] Montelukast [Singulair] 14 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Monoclonal Antibody: Omalizumab [Xolair] Mechanism of action Antagonism of immunoglobulin E (IgE), a type of antibody Therapeutic use Patients age 12 years or older with moderate to severe asthma that (1) is allergy related and (2) cannot be controlled with an inhaled glucocorticoid 15 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Monoclonal Antibody: Omalizumab [Xolair] Adverse effects Injection-site reactions Viral infection Upper respiratory infection Sinusitis Headache Pharyngitis Cardiovascular events Malignancy Life-threatening anaphylaxis 16 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Bronchodilators Provide symptomatic relief but do not alter the underlying disease process (inflammation) In almost all cases, patients taking a bronchodilator should also be taking a glucocorticoid for long-term suppression of inflammation Principal bronchodilators are the beta 2-adrenergic agonists 17 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Bronchodilators: Beta2-Adrenergic Agonists Mechanism of action Through activation of beta 2 receptors in the smooth muscle of the lung, these drugs promote bronchodilation, relieving bronchospasm Beta2 agonists have a limited role in suppressing histamine release in the lung and increasing ciliary motility 18 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Bronchodilators: Beta2-Adrenergic Agonists Use in asthma and COPD Inhaled short-acting beta2 agonists (SABAs) Taken PRN to abort an ongoing attack EIB: Taken before exercise to prevent an attack Hospitalized patients undergoing a severe acute attack: Nebulized SABA is the traditional treatment of choice Delivery with an MDI in the outpatient setting may be equally effective 19 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Bronchodilators: Beta2-Adrenergic Agonists Use in asthma and COPD Inhaled long-acting beta2 agonists (LABAs) Long-term control in patients who experience frequent attacks Dosing is on a fixed schedule, not PRN Effective in treating stable COPD When used to treat asthma, must always be combined with a glucocorticoid Use alone in asthma is contraindicated 20 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Bronchodilators: Beta2-Adrenergic Agonists Adverse effects Inhaled preparations Systemic effects: Tachycardia, angina, tremor Oral preparations Excessive dosage: Angina pectoris, tachydysrhythmias Tremor 21 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anticholinergic Drugs: Ipratropium Improves lung function by blocking muscarinic receptors in the bronchi, thereby reducing bronchoconstriction Action and use Administered by inhalation to relieve bronchospasm Therapeutic effects begin within 30 seconds, reach 50% of maximum in 3 minutes, and persist about 6 hours Adverse effects Dry mouth and irritation of the pharynx Glaucoma Cardiovascular events 22 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anticholinergic Drugs: Tiotropium Long-acting, inhaled anticholinergic agent approved for maintenance therapy of bronchospasm associated with COPD Not approved for asthma Relieves bronchospasm by blocking muscarinic receptors in the lung Therapeutic effects begin about 30 minutes after inhalation, peak in 3 hours, and persist about 24 hours With subsequent doses: Bronchodilation continues to improve, reaching a plateau after eight consecutive doses (8 days) 23 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Anticholinergic Drugs: Aclidinium Newest long-acting anticholinergic for management of bronchospasm associated with COPD Relieves bronchospasm by blocking muscarinic receptors in the lung Peak levels have occurred within 10 minutes of drug delivery Intended only for maintenance therapy Not for acute symptom relief 24 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Glucocorticoid/LABA Combinations Available combinations Fluticasone/salmeterol [Advair] Budesonide/formoterol [Symbicort] Mometasone/formoterol [Dulera] Indicated for long-term maintenance in adults and children Not recommended for initial therapy 25 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Management of Asthma Four classes of asthma severity Intermittent Mild persistent Moderate persistent Severe persistent Treatment goals Reducing impairment Reducing risk Stepwise therapy Step chosen for initial therapy is based on pretreatment classification of asthma severity Moving up or down a step is based on ongoing assessment of asthma control 26 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Drugs for Acute Severe Exacerbation This condition requires immediate attention Goals: Relieve airway obstruction and hypoxemia, and normalize lung function as quickly as possible Initial therapy consists of administering: Oxygen ‒ To relieve hypoxemia A systemic glucocorticoid ‒ To reduce airway inflammation A nebulized, high-dose SABA ‒ To relieve airflow obstruction Nebulized ipratropium ‒ To further reduce airflow obstruction 27 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Management of Stable COPD Pharmacologic management Bronchodilators Glucocorticoids Phosphodiesterase-4 inhibitors 28 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Management of COPD Exacerbations Pharmacologic management SABAs (specifically inhaled, either alone or in combination with inhaled anticholinergics) are preferred for bronchodilation during COPD exacerbations Systemic glucocorticoids Antibiotics Supplemental oxygen to maintain an oxygen saturation of 88% to 92% 29 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Drugs for Allergic Rhinitis, Cough, and Colds Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Allergic Rhinitis Inflammatory disorder of the upper airway, lower airway, and eyes Symptoms Sneezing Rhinorrhea Pruritus Nasal congestion For some people: Conjunctivitis, sinusitis, and asthma 31 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Allergic Rhinitis Seasonal and perennial Triggered by airborne allergens Allergens bind to immunoglobulin E (Ig E) on mast cells Triggers release of inflammatory mediators Histamine, leukotrienes, prostaglandins 32 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Classes of Drugs Used for Allergic Rhinitis Glucocorticoids (intranasal) Antihistamines (oral and intranasal) Sympathomimetics (oral and intranasal) 33 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Intranasal Glucocorticoids First choice ‒ most effective for treatment and prevention of rhinitis Mild adverse effects Drying of nasal mucosa or sore throat Epistaxis (nosebleed) Headache Rarely, systemic effects (adrenal suppression and slowing of linear pediatric growth) 34 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Oral Antihistamines For allergic rhinitis Do not reduce nasal congestion Most effective if taken prophylactically Should be taken regularly throughout the allergy season, even when symptoms are absent, to prevent an initial histamine receptor activation Mild adverse effects: Sedation with first generation (much less with second generation) 35 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Sympathomimetics Reduce nasal congestion (do not reduce rhinorrhea, sneezing, or itching) Activate alpha 1-adrenergic receptors on nasal blood vessels Adverse effects Rebound congestion CNS stimulation Cardiovascular effects and stroke Abuse 36 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Sympathomimetics (Oral/Nasal) Factors in topical administration Should not use longer than 5 consecutive days Drops or sprays Comparison: Drops versus sprays Topical agents act more quickly than oral agents and are usually more effective Oral agents act longer than topical preparations Systemic effects occur primarily with oral agents; topical agents usually elicit these responses only when dosage is higher than recommended Rebound congestion is common with prolonged use of topical agents but rare with oral agents 37 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Sympathomimetics (Oral/Nasal) Phenylephrine, ephedrine, pseudoephedrine Antihistamine-sympathomimetic combinations Ipratropium bromide [Atrovent] Montelukast [Singulair] Omalizumab [Xolair] 38 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Drugs for Cough Antitussives Drugs that suppress cough Opioid antitussives Codeine and hydrocodone Nonopioid antitussives Dextromethorphan Diphenhydramine Benzonatate 39 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved. Expectorants Guaifenesin [Mucinex, Humibid] Renders cough more productive by stimulating flow of respiratory tract secretions Higher doses may be effective 40 Copyright © 2016, 2013, 2010 by Saunders, an imprint of Elsevier Inc. All rights reserved.