Pediatric Allergic Rhinitis Medication

Many groups of medications are used for allergic rhinitis (AR), including antihistamines, corticosteroids, decongestants, saline, sodium cromolyn, and antileukotrienes. 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 immunotherapy is also available in some parts of the United States as well as 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 that it can be administered at home. The efficacy rate is about 20-30% in countries outside of the United States. Currently, it is not approved by the US Food and Drug Administration (FDA), and the formulation that is presently used has not been shown to be effective for this use. The formulations that have been tested in other countries are not available in the United States. This form of treatment is controversial.

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.

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 and are included in many combination products for cough, colds, and allergies. These include brompheniramine, chlorpheniramine (Chlor-Trimeton), and diphenhydramine (Benadryl), fexofenadine (Allegra), loratadine (Claritin) and cetirizine (Zyrtec) are now available over-the-counter (OTC) without a prescription. Second-generation antihistamines include desloratadine (Clarinex), and levocetirizine dihydrochloride (XYZAL), which require a prescription.

Cetirizine (Zyrtec)

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)

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)

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.

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)

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

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 affect 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. A longer study began in late 2007.

Beclomethasone (Beconase AQ, QNASL)

May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation. QNASL available as intranasal dry powder.

Budesonide inhaled (Rhinocort Aqua)

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

Ciclesonide (Omnaris)

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 (AeroBid)

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

Fluticasone propionate (Flonase)

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

Fluticasone furoate (Veramyst)

Intranasal corticosteroid. Indicated for seasonal and perennial allergic rhinitis. Relieves nasal symptoms associated with allergic rhinitis. Has also demonstrated improvement in allergic eye symptoms. Contains 27.5 mcg/spray.

Mometasone (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 inhaled (Nasacort AQ)

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

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 an addictive medication that is effective in shrinking nasal membranes and is not recommended for long-term use. Use of oxymetazoline hydrochloride for more than 7-10 d is habit forming. Patients can be addicted for years at a time. Addiction is termed rhinitis medicamentosa. Ipratropium bromide can be used for a prolonged period of time.

Ipratropium bromide 0.03% or 0.06% (Atrovent)

Anticholinergic used for reducing rhinorrhea in patients with AR or vasomotor rhinitis. An excellent medication for decreasing rhinitis. Nonaddictive 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.

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 (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.

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.