Pediatric Asthma Medication

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    Pediatric Asthma Medication

    Author: Girish D Sharma, MD, FCCP, FAAP; Chief Editor: Michael R Bye, MD more...

    Updated: Nov 25, 2013

    Medication Summary

    Pharmacologic management includes the use of control agents such as inhaled corticosteroids, inhaled cromolyn

    or nedocromil, long-acting bronchodilators, theophylline, leukotriene modifiers, and more recent strategies such as

    the use of anti-immunoglobulin E (IgE) antibodies (omalizumab). Relief medications include short-acting

    bronchodilators, systemic corticosteroids, and ipratropium

    Bronchodilators, Beta2-Agonists

    Class Summary

    These agents are used to treat bronchospasm in acute asthmatic episodes, and used to prevent bronchospasm

    associated with exercise-induced asthma or nocturnal asthma. Several studies have suggested that short-acting

    beta2-agonists such as albuterol may produce adverse outcomes (eg, decreased peak flow or increased risk of

    exacerbations) in patients homozygous for arginine (Arg/Arg) at the 16th amino acid position of beta-adrenergicreceptor gene compared with patients homozygous for glycine (Gly-Gly). Similar findings are reported for long-

    acting beta2-agonists, such as salmeterol.

    View full drug information

    Albuterol sulfate (Proventil HFA, Ventolin HFA, ProAir HFA)

    This beta2-agonist is the most commonly used bronchodilator that is available in multiple forms (eg, solution for

    nebulization, MDI, PO solution). This is most commonly used in rescue therapy for acute asthmatic symptoms.

    Used as needed. Prolonged use may be associated with tachyphylaxis due to beta2-receptor downregulation and

    receptor hyposensitivity.

    View full drug information

    Pirbuterol(Maxair Autohaler)

    Pirbuterolis available as a breath-actuated or ordinary inhaler. The ease of administration with the breath-actuated

    device makes it an attractive choice in the treatment of acute symptoms in younger children who otherwise cannot

    use an MDI. The Autohaler delivers 200 mcg per actuation.

    Nonracemic Form of the Beta2-Agonist Albuterol

    Class Summary

    This nonracemic form of albuterol offers a significant reduction in the adverse effects associated with racemic

    albuterol (eg, muscle tremors, tachycardia, hyperglycemia, hypokalemia).

    View full drug information

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    Levalbuterol (Xopenex)

    Nonracemic form of albuterol, levalbuterol (R isomer) is effective in smaller doses and is reported to have fewer

    adverse effects (eg, tachycardia, hyperglycemia, hypokalemia). The dose may be doubled in acute severe

    episodes when even a slight increase in the bronchodilator response may make a big difference in the

    management strategy (eg, in avoiding patient ventilation). It is available as an MDI (45 mcg per actuation) or

    solution for nebulized inhalation.

    Long-Acting Beta2-AgonistsClass Summary

    Long-acting bronchodilators (LABA) are not used for the treatment of acute bronchospasm. They are used for the

    preventive treatment of nocturnal asthma or exercise-induced asthmatic symptoms, for example.

    Currently, 2 LABA are available in the United States: salmeterol (Serevent) and formoterol (Foradil). Salmeterol

    and formoterol are available as combination products with inhaled corticosteroids in the United States (Advair,

    Symbicort, Dulera).

    LABA may increase the chance of severe asthma episodes and death when those episodes occur. Most cases

    have occurred in patients with severe and/or acutely deteriorating asthma; they have also occurred in a fewpatients with less severe asthma.

    LABAs are not considered first-line medications to treat asthma. LABAs should not be used as isolated

    medications and should be added to the asthma treatment plan only if other medicines do not control asthma,

    including the use of low- or medium-dose corticosteroids. If used as isolated medication, LABAs should be

    prescribed by a subspecialist (ie, pulmonologist, allergist).

    View full drug information

    Salmeterol (Serevent Diskus)

    This long-acting preparation of a beta2-agonist is used primarily to treat nocturnal or exercise-induced symptoms.It has no anti-inflammatory action and is not indicated in the treatment of acute bronchospastic episodes. It may

    be used as an adjunct to inhaled corticosteroids to reduce the potential adverse effects of the steroids. The

    medication is delivered via a Diskus DPI.

    View full drug information

    Formoterol (Foradil Aerolizer)

    Formoterol relieves bronchospasm by relaxing the smooth muscles of the bronchioles in conditions associated

    with asthma.

    Methylxanthines

    Class Summary

    These agents are used for long-term control and prevention of symptoms, especially nocturnal symptoms.

    View full drug information

    Theophylline (Theo-24, Theochron, Uniphyl)

    Theophylline is available in short-acting and long-acting formulations. Because of the need to monitor serum

    concentrations, this agent is used infrequently. The dose and frequency depend on the particular product selected.

    Inhaled Corticosteroids

    Class Summary

    http://reference.medscape.com/drug/theo-dur-quibron-t-sr-theophylline-343447#1http://reference.medscape.com/drug/theo-dur-quibron-t-sr-theophylline-343447#1http://reference.medscape.com/drug/foradil-aerolizer-perforomist-formoterol-343432#1http://reference.medscape.com/drug/foradil-aerolizer-perforomist-formoterol-343432#1http://reference.medscape.com/drug/serevent-diskus-salmeterol-343445#1http://reference.medscape.com/drug/serevent-diskus-salmeterol-343445#1http://reference.medscape.com/drug/xopenex-hfa-levalbuterol-343438#1
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    Steroids are the most potent anti-inflammatory agents. Inhaled forms are topically active, poorly absorbed, and

    least likely to cause adverse effects. They are used for long-term control of symptoms and for the suppression,

    control, and reversal of inflammation. Inhaled forms reduce the need for systemic corticosteroids.

    Inhaled steroids block late asthmatic response to allergens; reduce airway hyperresponsiveness; inhibit cytokine

    production, adhesion protein activation, and inflammatory cell migration and activation; and reverse beta2-receptor

    downregulation and subsensitivity (in acute asthmatic episodes with LABA use).

    View full drug information

    Ciclesonide (Alvesco)

    Ciclesonide is an aerosol inhaled corticosteroid indicated for maintenance treatment of asthma as prophylactic

    therapy in adult and adolescent patients aged 12 y and older. Not indicated for relief of acute bronchospasm.

    Corticosteroids have wide range of effects on multiple cell types (eg, mast cells, eosinophils, neutrophils,

    macrophages, lymphocytes) and mediators (eg, histamines, eicosanoids, leukotrienes, cytokines) involved in

    inflammation.

    Individual patients experience variable time to onset and degree of symptom relief. Maximum benefit may not be

    achieved for 4 wk or longer after initiation of therapy.

    After asthma stability is achieved, it is best to titrate to lowest effective dosage to reduce the possibility of adverse

    effects. For patients who do not adequately respond to the starting dose after 4 wk of therapy, higher doses may

    provide additional asthma control.

    View full drug information

    Beclomethasone (QVAR)

    Beclomethasone inhibits bronchoconstriction mechanisms; causes direct smooth muscle relaxation; and may

    decrease the number and activity of inflammatory cells, which, in turn, decreases airway hyperresponsiveness. It

    is available as 40 mcg/actuation or 80 mcg/actuation.

    View full drug information

    Fluticasone (Flovent Diskus, Flovent HFA)

    Fluticasone has extremely potent vasoconstrictive and anti-inflammatory activity. It has a weak hypothalamic-

    pituitary adrenocortical axis inhibitory potency when applied topically. It is available as an MDI aerosolized product

    (HFA) or DPI (Diskus).

    View full drug information

    Budesonide inhaled (Pulmicort Flexhaler or Respules)

    Budesonide has extremely potent vasoconstrictive and anti-inflammatory activity. It has a weak hypothalamic-

    pituitary adrenocortical axis inhibitory potency when applied topically. It is available as a DPI in 90 mcg/actuation

    (delivers about 80 mcg/actuation) or 180 mcg/actuation (delivers about 160 mcg/actuation). A nebulized susp (ie,

    Respules) is also available for young children.

    View full drug information

    Mometasone furoate inhalation powder (Asmanex Twisthaler)

    Mometasone is a corticosteroid for inhalation. It is indicated for asthma as prophylactic therapy.

    Systemic Corticosteroids

    Class Summary

    These agents are used for short courses (3-10 d) to gain prompt control of inadequately controlled acute asthmatic

    http://reference.medscape.com/drug/asmanex-twisthaler-mometasone-inhaled-343406#1http://reference.medscape.com/drug/asmanex-twisthaler-mometasone-inhaled-343406#1http://reference.medscape.com/drug/pulmicort-respules-pulmicort-flexhaler-budesonide-inhaled-343428#1http://reference.medscape.com/drug/pulmicort-respules-pulmicort-flexhaler-budesonide-inhaled-343428#1http://reference.medscape.com/drug/flovent-diskus-flovent-hfa-fluticasone-inhaled-343415#1http://reference.medscape.com/drug/flovent-diskus-flovent-hfa-fluticasone-inhaled-343415#1http://reference.medscape.com/drug/qvar-beclomethasone-inhaled-343427#1http://reference.medscape.com/drug/qvar-beclomethasone-inhaled-343427#1http://reference.medscape.com/drug/alvesco-ciclesonide-inhaled-343436#1http://reference.medscape.com/drug/alvesco-ciclesonide-inhaled-343436#1
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    episodes. They are also used for long-term prevention of symptoms in severe persistent asthma as well as for

    suppression, control, and reversal of inflammation. Frequent and repetitive use of beta2-agonists has been

    associated with beta2-receptor subsensit ivity and downregulation; these processes are reversed with

    corticosteroids.

    Higher-dose corticosteroids have no advantage in severe asthma exacerbations, and intravenous administration

    has no advantage over oral therapy, provided that GI transit time or absorption is not impaired. The usual regimen

    is to continue frequent multiple daily dosing until the FEV1or peak expiratory flow (PEF) is 50% of the predicted or

    personal best values; then, the dose is changed to twice daily. This usually occurs within 48 hours.

    View full drug information

    Prednisone (Deltasone, Orasone) and prednisolone (Pediapred, Prelone, Orapred)

    An immunosuppressant for the treatment of autoimmune disorders, prednisone may decrease inflammation by

    reversing increased capillary permeability and suppressing polymorphonuclear neutrophil (PMN) act ivity.

    View full drug information

    Methylprednisolone (Solu-Medrol)

    Methylprednisolone may decrease inflammation by reversing increased capillary permeability and suppressingPMN activity.

    Leukotriene Modifiers

    Class Summary

    Knowledge that leukotrienes cause bronchospasm, increased vascular permeability, mucosal edema, and

    inflammatory cell infiltration has led to the concept of modifying their action by using pharmacologic agents. These

    are either 5-lipoxygenase inhibitors or leukotriene-receptor antagonists.

    View full drug information

    Zafirlukast (Accolate)

    Zafirlukast is a selective competitive inhibitor of LTD4 and LTE4 receptors.

    View full drug information

    Montelukast (Singulair)

    The last agent introduced in its class, montelukast has the advantages that it is chewable, it has a once-a-day

    dosing, and it has no significant adverse effects.

    Monoclonal Antibodies

    Class Summary

    These agents bind selectively to human IgE on the surface of mast cells and basophils.

    View full drug information

    Omalizumab (Xolair)

    Omalizumab is a recombinant, DNA-derived, humanized IgG monoclonal antibody that binds selectively to humanIgE on surface of mast cells and basophils. It reduces mediator release, which promotes allergic response. It is

    indicated for moderate-to-severe persistent asthma in patients who react to perennial allergens in whom symptoms

    are not controlled by inhaled corticosteroids.

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    Combination Inhaled Steroids/Long-Acting Beta2-Agonists

    Class Summary

    These combinations may decrease asthma exacerbations when inhaled short-acting beta2-agonists and

    corticosteroids have failed. Refer to previous discussion in the LABAs section regarding increased risk of severe

    asthma episodes and death with LABAs. In a recent study, use of combination therapy using fluticasone

    propionate and salmeterol prolonged time to first severe asthma exacerbation.[61]

    Budesonide is an inhaled corticosteroid that alters level of inflammation in airways by inhibiting multiple types of

    inflammatory cells and decreasing production of cytokines and other mediators involved in the asthmatic response.

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

    View full drug information

    Budesonide/formoterol (Symbicort)

    Formoterol relieves bronchospasm by relaxing the smooth muscles of the bronchioles in conditions associated

    with asthma. Budesonide is an inhaled corticosteroid that alters the level of inflammation in airways by inhibiting

    multiple types of inflammatory cells and decreasing production of cytokines and other mediators involved in the

    asthmatic response. This combination is available as an MDI in 2 strengths; each actuation delivers formoterol 4.5-mcg with either 80-mcg or 160-mcg of budesonide.

    View full drug information

    Mometasone and formoterol (Dulera)

    This is a combination corticosteroid and LABA metered-dose inhaler. Mometasone elicits local anti-inflammatory

    effects in the respiratory tract with minimal systemic absorption. Formoterol elicits bronchial smooth muscle

    relaxation.

    This combination is indicated for prevention and maintenance of asthma symptoms in patients inadequately

    controlled with other asthma controller medications (eg, low-dose to medium-dose inhaled corticosteroids) orwhose disease severity clearly warrants initiation of treatment with 2 maintenance therapies, including a LABA.

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

    View full drug information

    Salmeterol/fluticasone inhaled (Advair)

    This is a combination corticosteroid and LABA metered-dose inhaler. Fluticasone inhibits bronchoconstriction

    mechanisms, produces direct smooth muscle relaxation, and may decrease number and activity of inflammatory

    cells, in turn decreasing airway hyper-responsiveness. It also has vasoconstrictive activity. Salmeterol relaxes the

    smooth muscles of the bronchioles in conditions associated with bronchitis, emphysema, asthma, or

    bronchiectasis and can relieve bronchospasms. Its effect may also facilitate expectoration. Adverse effects aremore likely to occur when administered at high or more frequent doses than recommended. 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.

    Anticholinergic Agents

    Class Summary

    These agents may be added to beta2-agonist therapy for treatment of acute exacerbations.

    View full drug information

    Ipratropium (Atrovent)

    Chemically related to atropine, protropium has antisecretory properties and, when applied locally, inhibits

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    secretions from serous and seromucous glands lining the nasal mucosa. The MDI delivers 17 mcg/actuation.

    Solution for inhalation contains 500 mcg/2.5 mL (ie, 0.02% solution for nebulization).

    Contributor Information and DisclosuresAuthor

    Girish D Sharma, MD, FCCP, FAAP Professor of Pediatrics, Director, Section of Pediatric Pulmonology and

    Rush Cystic Fibrosis Center, Rush Medical College; Senior Attending, Department of Pediatrics, Rush

    University Medical Center

    Girish D Sharma, MD, FCCP, FAAP is a member of the following medical societies:American Academy of

    Pediatrics,American College of Chest Physicians,American Thoracic Society, and Royal College of

    Physicians of Ireland

    Disclosure: Nothing to disclose.

    Coauthor(s)

    Payel Gupta, MD Department of Allergy and Immunology, ENT Faculty Practice

    Payel Gupta, MD is a member of the following medical societies:American College of Physicians

    Disclosure: Nothing to disclose.

    Specialty Editor Board

    Thomas Scanlin, MD Chief, Division of Pulmonary Medicine and Cystic Fibrosis Center, Department of

    Pediatrics, Rutgers Robert Wood Johnson Medical School

    Thomas Scanlin, MD is a member of the following medical societies: American Association for the

    Advancement of Science,American Society for Biochemistry and Molecular Biology,American Thoracic

    Society, Society for Pediatric Research, and Society for Pediatric Research

    Disclosure: Nothing to disclose.

    Mary L Windle, PharmD Adjunct Associate Professor, University of Nebraska Medical Center College ofPharmacy; Editor-in-Chief, Medscape Drug Reference

    Disclosure: Nothing to disclose.

    Charles Callahan, DO Professor, Deputy Chief of Clinical Services, Walter Reed Army Medical Center

    Charles Callahan, DO is a member of the following medical societies: American Academy of Pediatrics,

    American College of Chest Physicians,American College of Osteopathic Pediatricians,American Thoracic

    Society,Association of Military Surgeons of the US, and Christian Medical & Dental Society

    Disclosure: Nothing to disclose.

    Chief Editor

    Michael R Bye, MD Professor of Clinical Pediatrics, State University of New York at Buffalo School of

    Medicine; Attending Physician, Pediatric Pulmonary Division, Women's and Children's Hospital of Buffalo

    Michael R Bye, MD is a member of the following medical societies:American Academy of Pediatrics,American

    College of Chest Physicians, andAmerican Thoracic Society

    Disclosure: Nothing to disclose.

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