Pediatric Reactive Airway Disease Medication

Updated: Feb 23, 2016
  • Author: Eric S Chin, MD; Chief Editor: Kirsten A Bechtel, MD  more...
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Medication

Medication Summary

The goals of pharmacotherapy are to reduce morbidity and to prevent complications.

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Beta2-Adrenergic Agonist Agents, Inhaled

Class Summary

These agents relieve reversible bronchospasm by relaxing smooth muscles of the bronchi. Systemic beta-agonists allow systemic delivery of medication to the pulmonary system in medical conditions where bronchoconstriction may inhibit delivery of medication to desired site because of little to no air movement. Oral administration is less effective than inhaled beta-adrenergic agonists, and has therefore fallen into disfavor. Does not appear to alter admission.

Salmeterol is a highly selective, long-acting beta2-adrenergic agonist (LABA) with bronchodilatory activity. Salmeterol's benzene moiety resembles the structure of catecholamines, and occupies the active site of beta2-adrenergic receptor, while the long, lipophilic side chain of salmeterol, binds to the so-called exosite near the beta2-receptors. The binding at the exosite allows the active portion of the molecule to remain at the receptor site and continually engage and disengage with the receptor, therefore providing a long duration of action. This agent stimulates intracellular adenyl cyclase to catalyze the conversion of adenosine triphosphate to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels result in relaxation of bronchiolar smooth muscle, bronchodilation, and increased bronchial airflow.  LABA may not decrease the episodes of asthma exacerbations and may even lead to increased hospitalizations.  [22]

Salmeterol (Serevent Diskus)

Long-acting beta2-agonist. Not for emergent use since onset is 30 min or more. By relaxing the smooth muscles of the bronchioles in conditions associated with bronchitis, emphysema, asthma, or bronchiectasis, can relieve bronchospasms. Effect may also facilitate expectoration.

Adverse effects are more likely to occur when administered at high or more frequent doses than recommended. Available as a dry powder for inhalation in 50 mcg blister packs.

Albuterol (Ventolin HFA, Proventil HFA)

Beta-agonist for bronchospasm refractory to epinephrine. Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on cardiac muscle contractility. May decrease mediator release from mast cells and basophils and inhibit airway microvascular leakage. MDI delivers 90 mcg/actuation.

Continuous therapy may reduce need for mechanical ventilation.

Levalbuterol (Xopenex)

Used for treatment or prevention of bronchospasm. A selective beta2-agonist agent. Albuterol is a racemic mixture, while levalbuterol contains only the active R-enantiomer of albuterol. The S-enantiomer does not bind to beta2-receptors but may be responsible for some adverse effects of racemic albuterol, including bronchial hyperreactivity and reduced pulmonary function during prolonged use.

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Anticholinergic Agents

Class Summary

These agents decrease muscle tone in the small and large pulmonary airways.

Tiotropium (Spiriva HandiHaler, Spiriva Respimat)

long-acting, 24-hour, anticholinergic bronchodilator

Indicated for long-term, once-daily, maintenance treatment of asthma in patients aged ≥12 yr

Spiriva Respimat: 2.5 mcg (2 actuations; 1.25 mcg/actuation) inhaled PO qDay

Ipratropium (Atrovent)

A quaternary ammonium anticholinergic bronchodilator acting at muscarinic receptors of the parasympathetic nervous system. Chemically related to atropine. Has antisecretory properties and, when applied locally, inhibits secretions from serous and seromucous glands lining the nasal mucosa.

Synergistic with beta2-agonists. Each actuation delivers 17 mcg. Solution for nebulization available as 0.02% (500 mcg/vial).

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Beta2-Adrenergic Agonist Agents, Injection

Class Summary

These agents act to decrease the muscle tone in the small and large pulmonary airways.

Epinephrine (Adrenalin)

Elicits alpha-agonist effects that include increased peripheral vascular resistance, reversed peripheral vasodilatation, systemic hypotension, and vascular permeability. Beta2-agonist effects include bronchodilatation, chronotropic cardiac activity, and positive inotropic effects.

Terbutaline (Brethine)

Acts directly on beta2-receptors to relax bronchial smooth muscle, relieving bronchospasm and reducing airway resistance.

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Methylxanthines

Class Summary

These agents provide bronchodilation at the cellular level. The exact mechanism is unknown (eg, alteration of intracellular calcium, inhibition of phosphodiesterase, and/or antagonism of prostaglandins). Routine addition to beta-agonist provides benefit in ED management. May be of benefit in impending respiratory failure.

Theophylline, 85% (Aminophylline)

Potentiates exogenous catecholamines, stimulates endogenous catecholamine release and diaphragmatic muscular relaxation, which, in turn, stimulates bronchodilation.

For bronchodilation, near toxic (>20 mg/dL) levels are usually required.

No role in acute asthma exacerbation.

Considered in children who are responding poorly on maximal therapy.

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Magnesium Salt

Class Summary

These agents decrease acetylcholine release at the neuromuscular junction and may decrease resting tone of smooth muscle.

Magnesium sulfate

Thought to produce bronchodilation through counteraction of calcium-mediated smooth muscle constriction.

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Gas Mixture

Class Summary

This agent is a blend of oxygen and helium that is less dense than air.

Helium and oxygen (Heliox)

Reduces airway resistance in bronchi with turbulent flow because of low density. Decreases the work of breathing, hence, delaying the onset of respiratory muscle fatigue, allowing other therapies to work.

Available in mixtures of 80:20 (helium:oxygen), 70:30, and 60:40.

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General Anesthetic

Class Summary

Nonbarbiturate anesthetic/analgesic agent. An induction agent for airway management in patients with status asthmaticus and has a brief bronchodilatory effect.

Ketamine (Ketalar)

Acts on the cortex and limbic system, decreasing bronchospasm.

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Mast Cell Stabilizers

Class Summary

These agents inhibit degranulation of sensitized mast cells following exposure to specific antigens.

Cromolyn (Intal)

Inhibits histamine release and slow-reacting substance of anaphylaxis from mast cell. MDI delivers 800 mcg/actuation. Solution for nebulization available as 20 mg/2 mL

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Leukotriene Inhibitors

Class Summary

These agents inhibit the synthesis of leukotriene.

Zileuton (Zyflo)

Effective in aspirin-induced, cold air, and exercise-induced asthma. Not for use in acute episodes of asthma. Prophylactic use only.

Hepatic transaminase levels should be evaluated before initiation. Contraindicated in patients with active liver disease.

Zafirlukast (Accolate)

Cysteinyl leukotriene-receptor antagonist. Inhibits aspirin-induced, cold air, and exercise-induced asthma.

Not for use in acute episodes of asthma.

Montelukast (Singulair)

Cysteinyl leukotriene-receptor antagonist. Inhibits aspirin-induced, cold air, and exercise-induced asthma. Not for use in acute episodes of asthma.

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Corticosteroid

Class Summary

These agents have anti-inflammatory properties and cause profound and varied metabolic effects. They modify the body's immune response to diverse stimuli. Oral prednisone should never be substituted for an inhaled corticosteroid in children with a severe acute asthma exacerbation.

Frequent use of inhaled corticosteroid therapy is associated with less ED visits and less hospitalizations. Current research has not proven any long-term adverse effects with children receiving long-term inhaled corticosteroid.

Dexamethasone (Decadron)

Has many pharmacologic benefits but significant adverse effects. Stabilizes cell and lysosomal membranes, increases surfactant synthesis, increases serum vitamin A concentration, inhibits prostaglandin and proinflammatory cytokines (eg, TNF-alpha, IL-6, IL-2, and IFN-gamma). The inhibition of chemotactic factors and factors that increase capillary permeability inhibits recruitment of inflammatory cells into affected areas. Suppresses lymphocyte proliferation through direct cytolysis and inhibits mitosis. Breaks down granulocyte aggregates, and improves pulmonary microcirculation. Has multiple glucocorticoid and mineralocorticoid effects.

Readily absorbed via the GI tract and metabolized in the liver. Inactive metabolites are excreted via the kidneys. Lacks salt-retaining property of hydrocortisone.

Patients can be switched from an IV to PO regimen in a 1:1 ratio.

Prednisolone (Orapred, Prelone, Pediapred)

Glucocorticosteroid that occurs naturally and synthetically. Used for both acute and chronic asthma. May decrease inflammation by reversing increased capillary permeability and suppressing PMN activity.

Loading or initial dose should be taken all at once in the am; may suppress natural cortisone production; hence, requires tapering the dose upon discontinuation.

As soon as the dose for relief is found, a maintenance dose may be established until the nonsteroidal drugs are effective; must always use a decreasing dose to avoid serious renal suppression.

In seasonal allergy a "booster" of prednisone may speed resolution of symptoms. Quite effective in "exhaustion" stage of seasonal allergy.

Prednisone (Sterapred)

May decrease inflammation by reversing increased capillary permeability and suppressing PMN activity.

Methylprednisolone (Medrol, Solu-Medrol)

For treatment of inflammatory and allergic reactions. By reversing increased capillary permeability and suppressing PMN activity, may decrease inflammation. Allows reduction of ongoing airway inflammation. May increase responsiveness to beta2-agonists by increasing the number of beta2-adrenergic receptors. Prophylactic inhaled steroids in those diagnosed with asthma may impede airway remodeling, bronchial hyperreactivity, and future airway damage.

Systemic adverse effects rarely occur with inhaled corticosteroids. Systemic response time is the same in IV and PO.

Steroid use is recommended if minimal improvement occurs after first beta2-agonist treatment, the patient was recently discontinued from steroids, the patient reports a history of asthma symptoms for a few days before presentation, or URI-associated symptoms are present.

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H2 Receptor Antagonists

Class Summary

The combination of H1 and H2 antagonists may be useful in anaphylaxis not responding to H1 antagonists alone.

Cimetidine (Tagamet)

If no response to H1 antagonist alone, coadministration with this H2 antagonist treats itching and flushing in anaphylaxis, pruritus, urticaria, and contact dermatitis.

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Monoclonal Antibody

Class Summary

May be considered in patients with severe asthma caused by allergens and unresponsive to other treatments.

Omalizumab (Xolair)

Recombinant, DNA-derived, humanized IgG monoclonal antibody that binds selectively to human IgE on surface of mast cells and basophils. Reduces mediator release, which promotes allergic response. Indicated for moderate-to-severe persistent asthma in patients who react to perennial allergens in whom symptoms are not controlled by inhaled corticosteroids.

Mepolizumab (Nucala)

Mepolizumab is a humanized IgG1 kappa monoclonal antibody specific for interleukin-5 (IL-5). Mepolizumab binds to IL-5, and therefore stops IL-5 from binding to its receptor on the surface of eosinophils. It is indicated for add-on maintenance treatment of patients with severe asthma aged ≥12 y, and with an eosinophilic phenotype.

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Combination Inhaled Steroids/Long-Acting Beta2-Agonists

Class Summary

The use of combination therapy with a long-acting beta2 agonist plus an inhaled corticosteroid as initial preventer treatment in children who are not already taking inhaled corticosteroids, is not supported by clinical trials.  [23]

Budesonide/formoterol (Symbicort)

Available as an MDI in 2 strengths; each actuation delivers formoterol 4.5-mcg with either 80-mcg or 160-mcg of budesonide.

Mometasone inhaled/formoterol (Dulera)

Available in 2 strengths; each actuation delivers mometasone/formoterol 100 mcg/5 mcg or 200 mcg/5 mcg.

Salmeterol/fluticasone inhaled (Advair HFA, Advair Diskus)

Two delivery mechanisms are available (ie, powder for inhalation [Diskus], metered-dose inhaler [MDI]). Diskus is available as a combination of salmeterol 50 mcg with fluticasone 100 mcg, 250 mcg, or 500 mcg. The MDI is available as 21 mcg salmeterol with fluticasone 45 mcg, 115 mcg, or 230 mcg.

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Corticosteroids

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Corticosteroids, Inhalants

Class Summary

Inhibits bronchoconstriction mechanisms, produces direct smooth muscle relaxation, may decrease number and activity of inflammatory cells, in turn decreasing airway hyperresponsiveness. Has extremely potent vasoconstrictive and anti-inflammatory activity. Alters level of inflammation in airways by inhibiting multiple types of inflammatory cells and decreasing production of cytokines and other mediators. Decreases inflammation by suppressing migration of polymorphonuclear leukocytes and reversing capillary permeability.

Budesonide inhaled (Pulmicort Flexhaler, Pulmicort Respules)

Available as powder for inhalation in 90 mcg/actuation (actuation delivers ~80 mcg) or 180 mcg/actuation (actuation delivers ~160 mcg). Also available as suspension for nebulized inhalation in 0.25-mg/2 mL, 0.5-mg/2 mL, and 1-mg/2 mL. Indicated for maintenance treatment of asthma and prophylactic therapy.

Ciclesonide inhaled (Alvesco)

Aged 12 y and older

Receiving bronchodilators or inhaled corticosteroids: 80 mcg inhaled PO twice daily initially; may increase to 160 mcg twice daily Receiving Oral Corticosteroids: 80 mcg inhaled twice daily initially; may increase to 320 mcg twice daily

Beclomethasone, inhaled (Qvar)

<5 years: Safety and efficacy not established

5-12 years: 40 mcg inhaled PO BID for patients with/without prior history of inhaled corticosteroid use; do not exceed 80 mcg inhaled BID

>12 years

No prior history of inhaled corticosteroid use: 40-80 mcg inhaled PO BID; do not exceed 320 mcg BID Prior history of inhaled corticosteroid use: 40-160 mcg inhaled PO BID; do not exceed 320 mcg BID

Fluticasone inhaled (Flovent Diskus, Flovent HFA)

Inhaled aerosol

<4 years: Safety and efficacy not established 4-12 years: 88 mcg (2 actuations of 44 mcg) PO q12hr >12 years (prior inhaled corticosteroid use): 88-220 mcg PO q12hr; not to exceed 440 mcg q12hr >12 years (prior PO corticosteroid use): 440 mcg PO q12hr; not to exceed 880 mcg q12hr

Inhaled powder

<4 years: Safety and efficacy not established 4-12 years: 50-100 mcg PO q12hr >12 years (prior bronchodilator use): 100 mcg PO q12hr; not to exceed 500 mcg q12hr >12 years (prior inhaled corticosteroid use): 100-250 mcg PO q12hr; not to exceed 500 mcg q12hr >12 years (prior PO corticosteroid use): 500-1000 mcg PO q12hr; not to exceed 1000 mcg q12hr

Budesonide inhaled (Pulmicort Respules, Pulmicort Flexhaler)

Nebulized suspension

<1 years: Safety and efficacy not established 1-8 years (prior therapy with bronchodilators alone): 0.5 mg once daily or divided q12hr; not to exceed 0.5 mg/day 1-8 years (prior therapy with inhaled corticosteroids): 0.5 mg once daily or divided q12hr; not to exceed 1 mg/day 1-8 years (prior therapy with PO corticosteroids): 1 mg once daily or divided q12hr; not to exceed 1 mg/day Symptomatic children not responding to nonsteroidal therapy: May be initiated at 0.25 mg q12hr

Inhaled powder

<6 years: Safety and efficacy not established >6 years: 180 mcg PO q12hr; in some patients, may be initiated at 360 mcg q12hr; not to exceed 360 mcg q12hr

Mometasone inhaled (Asmanex HFA, Asmanex Twisthaler)

Asmanex Twisthaler

<4 years: Safety and efficacy not established 4-11 years: 110 mcg PO inhaled once daily in evening; not to exceed 110 mcg/day ≥12 years (received bronchodilators alone or inhaled corticosteroids): 220 mcg PO inhaled once daily in evening; may increase to 220 mcg q12hr if needed ≥12 years (received PO corticosteroids): 440 mcg PO inhaled q12hr; not to exceed 880 mcg/day

Asmanex HFA

<12 years: Safety and efficacy not established ≥12 years: 2 inhalations PO q12hr (ie, 200-400 mcg q12hr); starting dose based on prior asthma therapy -Received inhaled medium-dose corticosteroids: 200 mcg inhaled PO q12hr (as 2 actuations of 100 mcg/actuation) -Received inhaled high-dose corticosteroids: 400 mcg inhaled PO q12hr (as 2 actuations of 200 mcg/actuation) -Received oral corticosteroids: 400 mcg inhaled PO q12hr (as 2 actuations of 200 mcg/actuation)

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