Allergic Rhinitis Medication

Updated: Nov 15, 2017
  • Author: Javed Sheikh, MD; Chief Editor: Michael A Kaliner, MD  more...
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Medication

Medication Summary

Most cases of allergic rhinitis respond to pharmacotherapy. Patients with intermittent symptoms are often treated adequately with oral antihistamines, decongestants, or both as needed. Regular use of an intranasal steroid spray may be more appropriate for patients with chronic symptoms. [81] Daily use of an antihistamine, decongestant, or both can be considered either instead of or in addition to nasal steroids. The newer, second-generation (ie, nonsedating) antihistamines are usually preferable to avoid sedation and other adverse effects associated with the older, first-generation antihistamines. Ocular antihistamine drops (for eye symptoms), intranasal antihistamine sprays, intranasal cromolyn, intranasal anticholinergic sprays, and short courses of oral corticosteroids (reserved for severe, acute episodes only) may also provide relief.

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Second-generation antihistamines

Class Summary

Often referred to as the nonsedating antihistamines. They compete with histamine for histamine receptor type 1 (H1) receptor sites in the blood vessels, GI tract, and respiratory tract, which, in turn, inhibits physiologic effects that histamine normally induces at the H1 receptor sites. Some do not appear to produce clinically significant sedation at usual doses, while others have a low rate of sedation. [83, 84, 85] Other adverse effects (eg, anticholinergic symptoms) are generally not observed.

All are efficacious in controlling symptoms of allergic rhinitis (ie, sneezing, rhinorrhea, itching) but do not significantly improve nasal congestion. For this reason, some second-generation antihistamines are available as combination preparations containing a decongestant. They are often preferred for first-line therapy of allergic rhinitis, especially for seasonal or episodic symptoms, because of their excellent efficacy and safety profile. They can be used prn or daily.

Topical azelastine and olopatadine are nasal sprays antihistamines that effectively reduce sneezing, itching, and rhinorrhea but also effectively reduces congestion. [86, 87, 88] Used twice per day, especially when combined with a topical nasal corticosteroid, azelastine is effective at managing both allergic and nonallergic rhinitis.

The second-generation oral antihistamines currently available in the United States are cetirizine, levocetirizine, desloratadine, fexofenadine, and loratadine. A limited number of studies comparing these agents suggest no major differences in efficacy. Only cetirizine causes drowsiness more frequently than placebo. [85] Cetirizine, fexofenadine, and loratadine are also available in decongestant-containing preparations.

Cetirizine (Zyrtec)

Competes with histamine for H1 receptors in GI tract, blood vessels, and respiratory tract, reducing hypersensitivity reactions. Once-daily dosing is convenient. Bedtime dosing may be useful if sedation is a problem.

Levocetirizine (Xyzal)

Histamine1-receptor antagonist. Active enantiomer of cetirizine. Peak plasma levels reached within 1 h and half-life is about 8 h. Available as a 5-mg breakable (scored) tab. Indicated for seasonal and perennial allergic rhinitis.

Fexofenadine (Allegra Allergy, Mucinex Allergy)

Second-generation agent with a rate of sedation not significantly different from that of placebo. Competes with histamine for H1 receptors in GI tract, blood vessels, and respiratory tract, reducing hypersensitivity reactions. Available in qd and bid preparations.

Loratadine (Claritin, Loradamed, QlearQuil 24 hr Relief, Triaminic Allerchews, Alavert)

Selectively inhibits peripheral histamine H1 receptors. Tolerated well, with rate of sedation not significantly different from placebo.

Pseudoephedrine/loratadine (Alavert Allergy & Sinus, Claritin D-12 Hour Allergy & Congestion, Claritin-D 24 Hour Allergy & Congestion)

Selectively inhibits peripheral histamine H1 receptors. Tolerated well, with rate of sedation not significantly different from placebo.

Pseudoephedrine stimulates vasoconstriction by directly activating alpha-adrenergic receptors of the respiratory mucosa. Induces also bronchial relaxation and increases heart rate and contractility by stimulating beta-adrenergic receptors.

Tolerated well, with rate of sedation not significantly different from that of placebo. Some patients may notice anxiety or insomnia owing to pseudoephedrine component.

Pseudoephedrine/fexofenadine (Allegra-D 12 Hour, Allegra-D 24 Hour)

Fexofenadine is a nonsedating second-generation medication with fewer adverse effects than first-generation medications. Competes with histamine for H1 receptors on GI tract, blood vessels, and respiratory tract, reducing hypersensitivity reactions. Does not sedate.

Pseudoephedrine stimulates vasoconstriction by directly activating alpha-adrenergic receptors of the respiratory mucosa. Induces also bronchial relaxation and increases heart rate and contractility by stimulating beta-adrenergic receptors.

Desloratadine (Clarinex)

Relieves nasal congestion and systemic effects of seasonal allergy. Long-acting tricyclic histamine antagonist selective for H1-receptor. Major metabolite of loratadine, which after ingestion is extensively metabolized to active metabolite 3-hydroxydesloratadine.

Cetirizine/pseudoephedrine (Zyrtec D Allergy & Congestion)

Cetirizine selectively inhibits histamine H1 receptor sites in blood vessels, GI tract, and respiratory tract, which in turn inhibits physiologic effects that histamine normally induces at H1 receptor sites. Once-daily dosing is convenient. Bedtime dosing may be useful if sedation is a problem.

Pseudoephedrine stimulates vasoconstriction by directly activating alpha-adrenergic receptors of the respiratory mucosa. Induces also bronchial relaxation and increases heart rate and contractility by stimulating beta-adrenergic receptors.

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Leukotriene receptor antagonists

Class Summary

Alternative to oral antihistamine to treat allergic rhinitis. One of the leukotriene receptor antagonists, montelukast (Singulair), has been approved in the United States for treatment of seasonal and perennial allergic rhinitis. [89, 90, 91] When used as single agent, produces modest improvement in allergic rhinitis symptoms. [92]

Montelukast (Singulair)

Selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene (CysLT 1) receptor. Selectively prevents action of leukotrienes released by mast cells and eosinophils. When used as a single agent, has been shown to result in a reduction of seasonal allergic rhinitis symptoms, similar in degree to that of loratadine.

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First-generation antihistamines

Class Summary

The older, first-generation H1 antagonists (eg, diphenhydramine, hydroxyzine) are effective in reducing most symptoms of allergic rhinitis, but they produce a number of adverse effects (eg, drowsiness, anticholinergic effects). They can be used prn, but adverse effects may limit their usefulness when taken on a daily basis. Some patients tolerate the adverse effects with prolonged use, but they may experience cognitive impairment, and driving skills may be affected. [93, 94, 95, 96, 97] Administration at bedtime may help with drowsiness, but sedation and impairment of cognition may continue until the next day.

The second-generation antihistamines are nonsedating in most patients and are preferred as first-line therapy. Few adverse effects are reported (cetirizine may cause drowsiness in as many as 10% of patients); therefore, many specialists prefer the use of second-generation agents for allergic rhinitis. Caution patients taking medications with sedative effects about driving and operating heavy machinery. [96, 97]

Chlorpheniramine (Chlor-Trimeton, Aller-Chlor, Allergy Relief, Allergy-Time, Ed-ChlorPed, Pharbechlor)

First-generation agent, available OTC in the United States. Competes with histamine on H1-receptor sites on effector cells in blood vessels and respiratory tract.

Diphenhydramine (Benadryl, Aler-Dryl, Allergy Relief, Banophen, Diphen, Genahist, Ormir)

Common first-generation agent available OTC in the United States. Competes with histamine on H1-receptor sites on effector cells in blood vessels and respiratory tract. For symptomatic relief of symptoms caused by release of histamine in allergic reactions.

Hydroxyzine (Vistaril)

Effective first-generation agent but frequently produces sedation. Considerable sedation may occur with higher doses. Antagonizes H1 receptors in periphery. May suppress histamine activity in subcortical region of CNS.

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Decongestants

Class Summary

Stimulate vasoconstriction by directly activating alpha-adrenergic receptors of the respiratory mucosa. Pseudoephedrine produces weak bronchial relaxation (unlike epinephrine or ephedrine) and is not effective for treating asthma. Increases heart rate and contractility by stimulating beta-adrenergic receptors, and increases blood pressure by stimulating alpha adrenergic receptors. Used alone or in combination with antihistamines to treat nasal congestion. Anxiety and insomnia may occur. Expectorants may thin and loosen secretions, although experimental evidence for their efficacy is limited. Numerous preparations are available containing combinations of various decongestants, expectorants, or antihistamines. Alternatively, a separate decongestant and antihistamine can be administered to allow for individual dose titration of each drug.

Pseudoephedrine (Sudafed, Genaphed, Psudatabs, SudoGest, Suphedrine, Zephrex-D)

Stimulates vasoconstriction by directly activating alpha-adrenergic receptors of the respiratory mucosa. Available OTC in the United States. Helpful for nasal and sinus congestion.

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Nasal corticosteroids

Class Summary

The intranasal steroids are divided into three generations based on their bioavailability. First generation corticosteroids, such as, beclomethasone, are more bioavailable and tend to produce more systemic adverse effects than newer intranasal corticosteroids. The second- and third-generation categories are less bioavailable and have limited systemic adverse effects.

Nasal steroid sprays are highly efficacious in treating allergic rhinitis. [98, 99, 100, 101, 102] They control the 4 major symptoms of rhinitis (ie, sneezing, itching, rhinorrhea, congestion). They are effective as monotherapy, although they do not significantly affect ocular symptoms. Studies have shown nasal steroids to be more effective than monotherapy with nasal cromolyn or antihistamines. [99, 100] Greater benefit may occur when nasal steroids are used with other classes of medication. They are safe to use and not associated with significant systemic adverse effects in adults (this may also be true for children, but the data are less clear).

In October 2013, the FDA approved once-daily triamcinolone acetonide (Nasacort Allergy 24HR) nasal spray as an over-the-counter treatment for nasal allergy symptoms in children aged 2 years or older, adolescents, and adults. It is the first over-the-counter glucocorticoid approved for the treatment of nasal allergy symptoms.Flonase was approved by FDA to be available over the counter on July 24, 2014, and Rhinocort was recently approved last year March 23, 2015. [103]

Local adverse effects of nasal steroid sprays are limited to minor irritation or nasal bleeding, which resolve with temporary discontinuation of the medication. Nasal septal perforations are rarely reported and are less common with the newer corticosteroids and delivery systems. Safety during pregnancy has not been established; however, clinical experience suggests nasal corticosteroids (particularly beclomethasone, which has most experience in use) are not associated with adverse fetal effects.

The nasal steroids can be used prn, but seem to be maximally effective when used on a daily basis as maintenance therapy. They may also be helpful for vasomotor rhinitis or mixed rhinitis (a combination of vasomotor and allergic rhinitis) and can help to control nasal polyps.

 

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.

Budesonide, intranasal (Rhinocort Aqua, Rhinocort Allergy)

Corticosteroid considered efficacious and safe for allergic rhinitis. May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.

Fluticasone (Flonase Allergy Relief, GoodSense Nasoflow, Ticaspray, 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. May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.

Ciclesonide (Omnaris, Zetonna)

Newer corticosteroid nasal spray indicated for allergic rhinitis. 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.

Triamcinolone (Nasacort Allergy 24 HR, Nasal Allergy 24 HR)

Intranasal corticosteroid efficacious and safe for allergic rhinitis. May decrease number and activity of inflammatory cells, resulting in decreased nasal inflammation.

Mometasone, intranasal (Nasonex, Propel Mini)

Nasal spray; 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).

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Nasal corticosteroids and antihistamine combinations

Class Summary

These drug combinations may improve compliance. The antihistamine component will inhibit the release of histamine, which is responsible for causing the allergic response while the corticosteroid component will inhibit inflammatory reactions.

Azelastine/fluticasone intranasal (Dymista)

New formulation of combined intranasal steroids and intranasal antihistamines. More effective than using intranasal steroids or intranasal azelastine alone. Can be used in adults and children who are at least 6 years old.  Patients may experience an unpleasant taste after use.

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Antihistamines, Intranasal

Class Summary

Alternative to oral antihistamines to treat allergic rhinitis.

Azelastine (Astepro)

Use prn or on a regular basis. Use alone or in combination with other medications. Unlike oral antihistamines, has some effect on nasal congestion. Helpful for vasomotor rhinitis. Some patients experience a bitter taste. Systemic absorption may occur, resulting in sedation (reported in approximately 11% of patients).

Olopatadine intranasal (Patanase)

For relief of symptoms of seasonal allergic rhinitis. Before initial use, prime product by releasing 5 sprays or until fine mist appears. When product has not been used for more than 7 days, re-prime by releasing 2 sprays. Avoid spraying into eyes.

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Mast Cell Stabilizers

Class Summary

Produce mast cell stabilization and antiallergic effects that inhibit degranulation of mast cells. [104] Have no direct anti-inflammatory or antihistaminic effects. Effective for prophylaxis. May be used just before exposure to a known allergen (eg, animal, occupational). Begin treatment 1-2 wk before pollen season and continue daily to prevent seasonal allergic rhinitis. Effect is modest compared with that of intranasal corticosteroids. Excellent safety profile and are thought to be safe for use in children and pregnancy.

Cromolyn sodium (Nasalcrom)

Available OTC in the United States. Used daily for seasonal or perennial allergic rhinitis. Significant effect may not be observed for 4-7 d. For patients with isolated and predictable periods of exposure (eg, animal allergy, occupational allergy), administer just before exposure. Generally less effective than nasal corticosteroids. Protective effect lasts 4-8 h, frequent dosing is necessary.

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Intranasal anticholinergic agents

Class Summary

Used for reducing rhinorrhea in patients with allergic or vasomotor rhinitis. No significant effect on other symptoms. Can be used alone or in conjunction with other medications. In the United States, ipratropium bromide (Atrovent Nasal Spray) is available in a concentration of 0.03% (officially indicated for treatment of allergic and nonallergic rhinitis) and 0.06% (officially indicated for the treatment of rhinorrhea associated with common cold). The 0.03% strength is discussed.

Ipratropium (Atrovent Nasal Spray)

Chemically related to atropine. Has anti-secretory properties, and when applied locally, inhibits secretions from serous and seromucous glands lining the nasal mucosa. Poor absorption by nasal mucosa; therefore, not associated with adverse systemic effects. Local adverse effects (eg, dryness, epistaxis, irritation) may occur.

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Allergy Extracts

Class Summary

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

Grass pollens allergen extract (Oralair)

SL immunotherapy is 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), Kentucky bluegrass (Poa pratensis), Timothy grass (Phleum pratense), Orchard grass (Dactylis glomerata), and Sweet Vernal grass (Anthoxanthum odoratum).

Timothy grass pollen allergen extract (Grastek)

SL immunotherapy is indicated for allergic rhinitis (with or without conjunctivitis) confirmed by positive skin test or in vitro testing for Timothy grass pollen-specific IgE antibodies.

Ragweed allergen extract (Ragwitek)

SL immunotherapy is indicated for allergic rhinitis (with or without conjunctivitis) confirmed by positive skin test or in vitro testing for ragweed (Ambrosia artemisiifolia) grass pollen-specific IgE antibodies.

House dust mite immunotherapy (Odactra)

The precise mechanisms of action of allergen immunotherapy is not known. The SL tablet consists of standardized extract with consistent biological potency. It is indicated for dust mite-induced allergic rhinitis with or without conjunctivitis, confirmed by in vitro testing for IgE antibodies to Dermatophagoides farinae or Dermatophagoides pteronyssinus house dust mites, or skin testing to licensed house dust mite allergen extracts, in people aged 18-65 years.

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