Medications for Allergy

Drug Approvals

(BANM, US Adopted Name, rINNM)

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (Mometasone Furoate). A white or almost white powder. Practically insoluble in water slightly soluble in alcohol soluble in acetone and in dichloromethane.

The United States Pharmacopeia 31, 2008 (Mometasone Furoate). A white to off-white powder. Soluble in acetone and in dichloromethane.

Profile

Mometasone furoate is a corticosteroid used topically for its glucocorticoid activity in the treatment of various skin disorders. It is usually used as a cream, ointment, or lotion containing 0.1%.

When applied topically, particularly to large areas, when the skin is broken, or under occlusive dressings, or when given intranasally, corticosteroids may be absorbed in sufficient amounts to cause systemic effects. The effects of topical corticosteroids on the skin are described. For recommendations concerning the correct use of corticosteroids on the skin, and a rough guide to the clinical potencies of topical corticosteroids.

A nasal suspension of mometasone furoate 0.05%, as the monohydrate, is given in the treatment and prophylaxis of the symptoms of allergic rhinitis. The usual adult dose is the equivalent of 100 micrograms of mometasone furoate in each nostril once daily, increased if necessary to 200 micrograms in each nostril daily. Once symptoms are controlled a dose of 50 micrograms in each nostril daily may be effective for maintenance. In the UK, the dose for children aged between 6 and 11 years is the equivalent of 50 micrograms in each nostril once daily. In the USA, similar doses may be given to treat allergic rhinitis in children from 2 years of age.

The nasal suspension is also given for the treatment of nasal polyps in patients 18 years and older the recommended initial dose in the UK is 100 micrograms into each nostril once daily, increased after 5 to 6 weeks to twice daily if needed. In the USA the recommended initial dose is 100 micrograms in each nostril twice daily, although once daily administration may be sufficient in some patients.

Mometasone furoate is used by dry powder inhaler for the prophylaxis of asthma. Doses may differ between countries and dosage units may be expressed differently, as either the amount of drug released per actuation or the amount delivered from the mouthpiece. UK licensed product information includes an initial dose of 400 micrograms inhaled once daily in the evening for mild to moderate asthma in adults and adolescents aged 12 years and older. This may be adjusted to a maintenance dose of 200 micrograms once or twice daily. In severe asthma, an initial dose of 400 micrograms twice daily is used, then titrated to the lowest effective dose once symptoms are controlled. US doses are provided in terms of the amount of drug released per actuation (an actuation that releases 110 micrograms delivers 100 micrograms from the mouthpiece). An initial dose of 220 micrograms once daily in the evening is used in adults and adolescents, aged 12 years and older, who have been treated with inhaled therapy only (bronchodilators or corticosteroids) this may be increased to a maximum of 440 micrograms daily as a single dose or 2 divided doses. Patients receiving oral corticosteroids may be started on 440 micrograms twice daily. Children aged 4 to 11 years may be given 110 micrograms once daily in the evening, regardless of prior therapy this is the maximum recommended daily dose.

Preparations

British Pharmacopoeia 2008: Mometasone Aqueous Nasal Spray Mometasone Cream Mometasone Ointment Mometasone Scalp Application

The United States Pharmacopeia 31, 2008: Mometasone Furoate Cream Mometasone Furoate Ointment Mometasone Furoate Topical Solution.

Proprietary Preparations

Argentina: Elocon Fenisona Metason Momeplus Nasonex Novasone Uniclar

Australia:: AllerMax † Elocon Nasonex Novasone

Austria: Asmanex Elocon Elovent Nasonex

Belgium: Elocom Nasonex

Brazil: Asmanexf Elocom Nasonex Topison

Canada: Elocom Nasonex

Chile: Dermenet Dermosona Elocom Flogocort Lisoder Momelab Nasonex Rinoval Uniclar

Czech Republic: Asmanex Elocom Nasonex

Denmark: Asmanex Elocon Nasonex

Finland: Asmanex Elocon Nasonex

France: Nasonex

Germany: Asmanex Ecural Nasonex

Greece: Asmanex Bioelementa Ecelecort Elocon Elovent Esine F-Din Fremomet Makiren Metason Mofur Molken Momecort Movesan Mozeton Nasamet Nasonex Pharmecort Yperod

Hong Kong: Elomet Nasonex Topcort

Hungary: Elocom Nasonex

India: Elocon Metaspray Momate Topcort

Indonesia: Dermovel Elocon Eloskin Elox Intercon Mefurosan Mesone Mofacort Mofulex Momet Motaderm Moteson Nasonex

Ireland: Asmanex Elocon Nasonex

Israel: Elocom Nasonex

Italy: Altosone Elocon Nasonex Rinelon Uniclar

Malaysia: Elomet Momate Nasonex

Mexico: Elica Elomet Elovent Rinelon Uniclar

The Netherlands: Asmanex Elocon Elovent Nasonex

Norway: Elocon Nasonex

New Zealand: Asmanex Bronconex Elocon

Philippines: Elica Elocon Momate Nasonex Rinelon

Poland: Elocom Elosone Nasonex

Portugal: Asmanex Elocom Elomet Elovent Nasomet Prospiril

Russia: Elocom Nasonex

South Africa: Elica Elocon Nasonex Rinelon

Singapore: Elomet Nasonex

Spain: Asmanexf Elica Elocom Nasonex Rinelon

Sweden: Asmanex Elocon Nasonex

Switzerland: Asmanex Elocom Nasonex

Thailand: Elomet Nasonex Rineloir †

Turkey: Elocon M-Furo Nasonex

UK: Asmanex Elocon Nasonex

USA: Asmanex Elocon Nasonex

Venezuela: Asmanex Cortynase Dergentil Elocon Eloconex † Elomet Nasonex Uniclar

Multi-ingredient

Argentina: Elosalic †

Austria: Elosalic

Chile: Velosalic

Czech Republic: Momesalic Monsalic †

Germany: Elosalic

Hong Kong: Elosalic

India: Momate-S

Indonesia: Elosalic

Poland: Elosalic

Portugal: Monsalic

Russia: Elocom-S

South Africa: Elosalic

Sweden: Elosalic

Thailand: Elosalic †

Turkey: Elosalic

Venezuela: Elosalic

The use of intranasal corticosteroids is increasingly becoming first-line therapy for many patients with allergic rhinitis, especially those with moderate to severe symptoms or those with perennial allergic rhinitis in which nasal symptoms predominate. Intranasal corticosteroids specifically inhibit the allergic inflammatory processes that contribute to the late-phase response of nasal congestion. When used prophylactically, they can also inhibit the early-phase response to allergens. Overall, they are effective in relieving sneezing, nasal itching, rhinorrhea, and congestion.

Table 3 lists available intranasal corticosteroids, along with dosing information and comparative costs. In general, these agents are considered more cost-effective for use as monotherapy than 2nd-generation antihistamines. A recent meta-analysis found intranasal corticosteroids to be more effective than oral antihistamines in reducing nasal blockage, nasal discharge, sneezing, nasal itch, postnasal drip, and total nasal symptoms. No significant difference was detected for nasal discomfort, nasal resistance, and eye symptoms. No particular product has demonstrated clinical superiority, selection of drug should be based on factors such as response, ease of administration, cost, and formulation.

Table 3 Intranasal corticosteroids

Application site irritation (e.g., nasal irritation, burning, or sneezing after administration) is the most commonly encountered side effect. Patients complaining of local irritation may be switched to various aqueous formulations. Although rare, mucosal erosion and septal perforations have been reported with long-term use. To minimize septal irritation, patients should be instructed to direct the spray upwards and toward the lateral portion of the nose. Periodic examination of the nasal septum should be performed.

Although systemic effects from intranasal corticosteroids at recommended doses are considered minimal, there are some concerns regarding long-term exposure. Reports of posterior subcapsular cataract formation have been linked with the use of intranasal or inhaled corticosteroids; however, more recent prospective trials did not reveal evidence of posterior subcapsular cataract formation or elevation in intraocular pressure.

In 1998, the FDA’s advisory committees on pulmonary and allergy drugs and on metabolic endocrine drugs convened to assess data suggesting that intranasal corticosteroids may have an effect on growth velocity in children. Consequently, a new class labeling for pediatric use of inhaled and intranasal corticosteroids was mandated. At this time, the long-term significance of growth velocity reduction on final adult height is unknown. The FDA recommends routine monitoring of growth in pediatric patients using intranasal corticosteroids and titration to the lowest effective dose to minimize systemic risks.

Patient education is essential in ensuring proper use and compliance to intranasal corticosteroid therapy. Patients should be instructed on instillation techniques and informed about the possible delay in symptomatic response. Assessment of maximal response may require a therapeutic trial of several weeks. The drug should be administered regularly on a daily basis, rather than as needed for rescue relief.

For patients with severe disease, the combined use of intranasal corticosteroids and antihistamines may be necessary to control symptoms. The use of oral corticosteroids should be reserved for patients with severe exacerbations or intractable disease due to high risk of systemic adverse effects.

Most intranasal corticosteroids (CS) take a few days to work with the exception of the newer, more potent agents fluticasone and mometasone. Regardless, the maximum effect requires 1-2 weeks and possibly up to 3 weeks. Patients should be encouraged to contact their healthcare provider if no benefit is seen in this time. Often anti-allergy therapy is prescribed on a presumptive basis. Patients may be on intranasal CS therapy and not be aware of which allergens they are sensitive to. Skin prick allergy testing can easily assess allergy status. Once specific allergens are identified, appropriate environmental controls can be instituted.

When a patient exhibits intolerance to a specific intranasal corticosteroids product, an excipient in the formulation may be the cause. A suggested intervention would be to switch to an alternative product. For example, an alcohol-free product could be recommended over a product containing alcohol. Additional reinforcement should target instructions on proper nasal CS administration, and nasal conditioning (moisturizing). Often overlooked are patient-specific nasal behaviors. For example, a patient may be reporting nosebleeds, and through further inquiry reveals he is a frequent nose-picker; another patient may irrigate the nose with hydrogen peroxide. If nosebleeds remain problematic for the patient, referral to an Ear, Nose and Throat Specialist may be warranted. To facilitate tailoring patient therapy, Table 8 compares various intranasal corticosteroids available in the U.S.

Conclusion

Allergic rhinitis is characterized by acute and late phase reactions. Inflammation plays a dominant role in maintaining the late phase and contributes to the increased risk of complications. Intranasal steroids have been proven effective treatment for allergic rhinitis and are superior to oral antihistamines. Therefore, first-line treatment of allergic rhinitis should be intranasal steroids in patients with allergic rhinitis of perennial or seasonal pattern with persistent or moderate symptoms. Environmental control measures should target allergens relevant to the individual. Pharmacists are in a unique position to provide balanced information and take patient-specific factors into consideration when evaluating an individual patient for specific therapy for allergic rhinitis.