Pediatric Allergic Rhinitis Medication

Updated: Nov 15, 2017
  • Author: Jack M Becker, MD; Chief Editor: Harumi Jyonouchi, MD  more...
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Medication

Medication Summary

Many groups of medications are used for allergic rhinitis (AR), including antihistamines, corticosteroids, decongestants, saline, sodium cromolyn, and leukotriene receptor antagonists. These can be further subdivided into intranasal and oral therapies. Intranasal administration has the advantage of directly affecting the site of action, and, in general, intranasal medications have fewer adverse effects and no systemic effects. The main advantage of oral therapy is ease of use. Some patients resist using intranasal medications.

Allergen-specific immunotherapy is an alternative form of therapy that has several advantages. Most importantly, it is the only form of therapy that can cure allergy symptoms. Allergen-specific immunotherapy must be customized to the patient's individual allergies and involves weekly injections of increasing concentrations of an allergen until the maintenance dose is reached and a monthly injection of the maintenance dose for several years. The process usually does not produce clinical results in the first 6 months but results are seen afterwards. The recommended course is usually 4-5 years. Allergen-specific immunotherapy has been demonstrated to be more cost effective and improves the patient's quality of life more efficiently than standard allergy medications.

Sublingual (SL) immunotherapy has been available in other countries of the world. [9] In this form of therapy, small amounts of the allergen are placed under the tongue on a daily basis. The 2 main advantages are that no injections are necessary and treatment can be administered at home. In spite of the safety record of sublingual therapy, which has very few serious reactions, the FDA recommendations are that the first dose be given in a physician's office and an epinephrine autoinjector is to be prescribed.

In April 2014, the FDA approved 3 SL tablets. Two are for grass allergies and the third is for ragweed. Oralair consists of 5 calibrated grass pollen extracts (Oralair). It contains Perennial Ryegrass (Lolium perenne), Kentucky bluegrass (Poa pratensis), Timothy grass (Phleum pratense), Orchard grass (Dactylis glomerata), and Sweet Vernal grass (Anthoxanthum odoratum). [11] The Oralair SL tablet needs to be initiated 4 months prior to the season for the specific allergen. It is approved for adults and children aged 10-65 years.

The second SL immunotherapy for grass is only one type of grass. Timothy grass (Grastek) was also approved in April 2014. It should be initiated at least 12 weeks before the start of the grass pollen season. [12] Efficacy and safety in North America was established in a large study (n=1500) of adults and children aged 5-65 years. Results showed a 23% improvement of symptoms in the entire grass pollen season. [13] Timothy grass cross-reacts with the following grasses, including sweet vernal, orchard (also known as cocksfoot), perennial rye, Kentucky blue (also known as June grass), meadow fescue, and redtop. This high cross-reactivity allows for Grastek to be effective for a patient with grass allergies.

The third one is Ragwitek. Like the other 2, it needs to be started prior to the onset of the season. It is a short ragweed extract (Ambrosia artemisiifolia) for adults aged 18-65 years.

Saline nasal irrigation is effective in approximately 50% of patients with allergic rhinitis. Irrigation assists the body's natural function of rinsing allergens out of nasal passages. Tap water cannot be used because it is hypotonic and causes edema, leading to greater congestion.

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Antihistamines, 2nd Generation

Class Summary

Antihistamines are classified in several ways, including sedating and nonsedating, newer and older, and first- and second-generation antihistamines (most widely accepted classification). First-generation antihistamines are primarily over-the-counter OTC) and are included in many combination products for cough, colds, and allergies. These include brompheniramine, chlorpheniramine (Chlor-Trimeton), and diphenhydramine (Benadryl). Some 2nd generation antihistamines, such as fexofenadine (Allegra), loratadine (Claritin), and cetirizine (Zyrtec) are now available OTC without a prescription. Second-generation antihistamines include desloratadine (Clarinex), and levocetirizine dihydrochloride (XYZAL), which require a prescription.

Cetirizine (Zyrtec, Zyrtec Allergy, Children's Zyrtec Allergy)

Low-sedating second-generation medication with fewer adverse effects than first-generation medications. Selectively inhibits peripheral histamine H1 receptors. Available as syr (5 mg/5 mL) and 5- or 10-mg tab.

Levocetirizine (Xyzal)

Histamine H1-receptor antagonist. Active enantiomer of cetirizine. Peak plasma levels are reached within 1 h, and half-life is about 8 h. Available as a 5-mg breakable (scored) tab. Indicated for seasonal and perennial AR

Loratadine (Claritin)

Nonsedating second-generation antihistamine. Fewer adverse effects than with first-generation medications. Selectively inhibits peripheral histamine H1 receptors. Available as tab, disintegrating tab (Reditab), syr (5 mg/5 mL), or combined with pseudoephedrine in 12- or 24-h preparations. The only one that is presently available without a prescription

Desloratadine (Clarinex, Clarinex RediTabs)

Nonsedating second-generation antihistamine. Fewer adverse effects than with first-generation antihistamines. Selectively inhibits peripheral histamine H1 receptors. Relieves nasal congestion and systemic effects of seasonal allergies. Long-acting tricyclic histamine antagonist selective for H1-receptor. Major metabolite of loratadine, which, after ingestion, is extensively metabolized to active metabolite 3-hydroxydesloratadine. Available as tabs, syr (0.5 mg/mL), or PO disintegrating Reditabs (2.5 and 5 mg).

Fexofenadine (Allegra, Allegra Allergy 12 Hour, Allegra Allergy 24 Hour, Children's Allegra Allergy)

Nonsedating second-generation medication with fewer adverse effects than first-generation medications. Competes with histamine for H1 receptors in GI tract, blood vessels, and respiratory tract, reducing hypersensitivity reactions. Available OTC in qd and bid preparations. Also OTC available combined with pseudoephedrine.

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Antihistamines, Intranasal

Class Summary

These agents are an alternative to oral antihistamines to treat allergic rhinitis. Currently, azelastine and olopatadine are the only agents available in the United States.

Azelastine (Astelin Nasal Spray, Astepro)

An effective antihistamine delivered via the intranasal route. Mechanism is similar to PO antihistamines. Systemic absorption occurs and may cause sedation, headache, and nasal burning.

Olopatadine intranasal (Patanase)

Intranasal antihistamine spray for seasonal allergic rhinitis. Available as 6% intranasal solution (delivers 665 mcg/spray).

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Corticosteroids, Intranasal

Class Summary

This class of medications is most effective. Intranasal corticosteroids are potent anti-inflammatory agents shown to decrease allergic rhinitis symptoms in more than 90% of patients. Presently, 9 medications are available in this class, and all are essentially equivalent in efficacy, although few head-to-head studies have been performed. Mometasone (Nasonex) and fluticasone furoate (Veramyst) have been demonstrated to have a somewhat faster onset of action; however, after one week, no difference is found between medications. Most can be used on a once-daily basis, and all have a similar safety profile. Nasonex is the only medication that did not show an effect on growth at one year. Veramyst did not show a growth effect in a 2-week study that is designed to evaluate for growth affects.

There are 2 nasal inhalers, Qnasl and Zetonna. They are a spray form and allow for better nasal deposition for some patients who like a spray-type inhaler. They have shown to help decrease ocular symptoms. In the spring of 2014, Nasacort (triamcinolone) was approved as an over-the-counter medication.

Beclomethasone, intranasal (Beconase AQ, QNASL)

Corticosteroid with potent anti-inflammatory properties. Elicits effects on various cells, including mast cells and eosinophils. It also elicits effects on inflammatory mediators (eg, histamine, eicosanoids, leukotrienes, cytokines). Available in solution or suspension forms and delivered as a metered-dose nasal sprays. Beconase AQ is approved for children aged 6 y or older. QNASL is indicated for children aged 4 y or older.

Budesonide intranasal (Rhinocort Aqua)

May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.

Ciclesonide intranasal (Omnaris, Zetonna)

Corticosteroid nasal spray indicated for AR. Prodrug that is enzymatically hydrolyzed to pharmacologic active metabolite C21-desisobutyryl-ciclesonide following intranasal application. Corticosteroids have a wide range of effects on multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (eg, histamines, eicosanoids, leukotrienes, cytokines) involved in allergic inflammation. Each spray delivers 50 mcg.

Flunisolide intranasal (Nasarel)

May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.

Fluticasone intranasal (Flonase, Veramyst)

May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.  Veramyst is now available as OTC (Brand name: Flonase sensimist)

Mometasone, intranasal (Nasonex)

May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation. Demonstrated no mineralocorticoid, androgenic, antiandrogenic, or estrogenic activity in preclinical trials. Decreases rhinovirus-induced up-regulation in respiratory epithelial cells and modulate pretranscriptional mechanisms. Reduces intraepithelial eosinophilia and inflammatory cell infiltration (eg, eosinophils, lymphocytes, monocytes, neutrophils, plasma cells).

Triamcinolone, intranasal (Nasacort AQ)

May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.

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Antihistamine/Corticosteroid, Intranasal

Class Summary

Combination products are emerging on the market for patients who require an intranasal antihistamine and corticosteroids.

Azelastine/fluticasone intranasal (Dymista)

This combination product elicits histamine H1-receptor antagonist activity and anti-inflammatory effects. It is indicated for seasonal allergic rhinitis in adults and children aged 12 years or older.

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Intranasal decongestants

Class Summary

Decongestants are effective for short-term symptom control. They decrease nasal discharge and congestion and are available without a prescription. The 2 medications in this group are oxymetazoline hydrochloride (Afrin) and ipratropium bromide (Atrovent). Oxymetazoline hydrochloride is effective in shrinking nasal membranes and is not recommended for long-term use. Use of oxymetazoline hydrochloride for more than 7-10 days can cause rebound congestion. When used for >4-6 days nasal vasoconstrictive medications, that are used topically, can cause rhinitis medicamentosa, a condition characterized by nasal congestion in the absence of rhinorrhea or sneezing. Ipratropium bromide can be used for a prolonged period of time.

Ipratropium intranasal (Atrovent Nasal Spray)

Anticholinergic used for reducing rhinorrhea in patients with AR or vasomotor rhinitis. An excellent medication for decreasing rhinitis. Does not cause rebound congestion and lasts for 12 hours. Does not shrink the nasal mucosa, but inhibits secretion that causes rhinitis. Used alone or in conjunction with other medications.

Oxymetazoline (Afrin 12 Hour, Afrin Sinus, Mucinex Nasal Spray Full Force, Sinus Nasal Spray, Dristan Spray)

A representative topical decongestant applied directly to mucous membranes, where it stimulates alpha-adrenergic receptors and causes vasoconstriction. Decongestion occurs without drastic changes in BP, vascular redistribution, and cardiac stimulation. Use not recommended for >3 days.

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Leukotriene Receptor Antagonists

Class Summary

Montelukast has been approved as monotherapy for allergic rhinitis. It has been shown to be most effective in patients in whom significant congestion is a primary complaint. It has also been shown to work as adjunctive therapy with present second-generation antihistamines to provide greater relief of symptoms than antihistamines alone. It is beneficial in patients with symptoms in whom present antihistamines are not adequate. A study has shown a combination with cetirizine is as effective as an intranasal corticosteroid. Antileukotriene can also be added to the treatment plan in patients receiving antihistamines and intranasal therapy.

Montelukast (Singulair)

Inhibits airway cysteinyl leukotriene receptors. Because these receptors are found throughout the airway, the medication can mediate the effect in the upper and lower airway.

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Allergen Immunotherapy

Class Summary

Immunotherapy with daily sublingual (SL) tablets may be able to replace weekly injections in some individuals, depending on the offending allergens. Depending on the particular SL tablet, therapy must be initiated at least 3-4 months before the allergen season that is being treated.

Grass pollens allergen extract (Oralair)

SL immunotherapy indicated for grass pollen–induced allergic rhinitis (with or without conjunctivitis) confirmed by positive skin test or in vitro testing for grass pollen–specific immunoglobulin E antibodies for any of the 5 grass species contained in the product. It consists of 5 purified and calibrated pollen extracts: Perennial Ryegrass (Lolium perenne Poa pratensis), Timothy grass (Phleum pretense), Orchard grass (Dactylis glomerata), and Sweet Vernal grass (Anthoxanthum odoratum). It is approved for adults and children aged 10-65 years.

Timothy grass pollen allergen extract (Grastek)

SL immunotherapy indicated for allergic rhinitis (with or without conjunctivitis) confirmed by positive skin test or in vitro testing for Timothy grass pollen-specific IgE antibodies. It is approved for adults and children aged 5-65 years.

Ragweed allergen extract (Ambrosia artemisiifolia, Ragwitek)

SL immunotherapy indicated for short ragweed (Ambrosia artemisiifolia) pollen-induced allergic rhinitis (with or without conjunctivitis) confirmed by positive skin test or in vitro testing for ragweed-specific IgE antibodies. It is approved for adults aged 18-65 years.

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Mast Cell Stabilizers, Intranasal

Class Summary

These are effective therapy for AR in approximately 70-80% of patients. They produce mast cell stabilization and antiallergic effects by inhibiting mast cell degranulation. They have no direct anti-inflammatory or antihistaminic effects and minimal bronchodilator effects. They are effective for prophylaxis. They also clean out antigens mechanically, similar to saline. These products are now available over the counter.

Cromolyn sodium, intranasal (NasalCrom)

Used on a daily basis for seasonal or perennial AR. Significant effect may not be seen for 4-7 d. Administer just before exposure in patients with isolated and predictable periods of exposure (eg, animal allergy, occupational allergy). Generally less effective than nasal corticosteroids. Protective effect lasts 4-8 h; thus, frequent dosing is necessary. If desired, may be used with other medicines, including other allergy medicines.

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