Mometasone Furoate eent

Name: Mometasone Furoate eent

Uses for Mometasone Furoate

Allergic Rhinitis

Prophylaxis1 2 3 and treatment1 2 4 5 6 of nasal symptoms of seasonal allergic rhinitis.1 2 7 8

Treatment of nasal symptoms of perennial allergic rhinitis.1 2 7 8

Cautions for Mometasone Furoate

Contraindications

  • Known hypersensitivity to mometasone furoate or any ingredient in the formulation.1

Warnings/Precautions

Warnings

Withdrawal of Systemic Corticosteroid Therapy

Possible corticosteroid withdrawal symptoms (e.g., joint pain, muscular pain, lassitude, depression), acute adrenal insufficiency, or severe symptomatic exacerbation of asthma or other clinical conditions if prolonged systemic corticosteroid therapy is replaced with topical corticosteroid therapy; careful monitoring recommended.1

Use particular caution in patients with associated asthma or other conditions that may be exacerbated by too rapid a reduction in systemic corticosteroid dosage.1

Hypercorticism

Excessive intranasal dosages or use in patients who are particularly sensitive to corticosteroid effects due to recent systemic corticosteroid therapy may cause systemic corticosteroid effects (e.g., menstrual irregularities, acneiform lesions, cushingoid features).1 (See Systemic Corticosteroid Effects under Cautions.)

Immunosuppressed Patients

Increased susceptibility to infections in patients who are taking immunosuppressant drugs.1 Certain infections (e.g., varicella [chickenpox], measles) can be serious or even fatal in such patients, particularly in children.1

Exposure to varicella and measles should be avoided in previously unexposed patients.1 If exposure to varicella or measles occurs in susceptible patients, consider administering varicella zoster immune globulin (VZIG) or immune globulin (IG), respectively.1 Consider treatment with an antiviral agent if varicella develops.1

Sensitivity Reactions

Rarely, immediate hypersensitivity reactions or wheezing may occur.1 2

General Precautions

Systemic Corticosteroid Effects

Possible growth suppression in children or adolescents.1 (See Pediatric Use under Cautions.)

Excessive intranasal dosages or use in patients who are particularly sensitive to corticosteroid effects may increase risk of systemic corticosteroid effects (e.g., hypercorticism, adrenal suppression).1

Avoid use of higher than recommended dosages.1 If systemic effects occur, slowly reduce dosage and discontinue drug.1

Nasopharyngeal Effects

Rarely, localized candidial infections of the nose and/or pharynx have been reported.1 Local treatment of such infections and/or discontinuance of intranasal therapy may be required.1

Possible nasal burning and irritation.1 2 Rarely, nasal septum perforation has been reported.1

Periodically examine nasal passages for signs of mucosal changes during long-term therapy (several months or longer).1

Use not recommended in patients with recent nasal septal ulcers, nasal surgery, or nasal trauma until healing has occurred.1

Concomitant Infections

Use with caution, if at all, in patients with clinical or asymptomatic Mycobacterium tuberculosis infection of the respiratory tract; untreated fungal, bacterial, or systemic viral infections; or ocular herpes simplex infections.1

Ophthalmic Effects

No ophthalmologic abnormalities (i.e., elevation in intraocular pressure, cataracts) observed in long-term studies with mometasone furoate.1 Glaucoma, increased intraocular pressure, and cataracts have been reported rarely with other nasal or inhaled corticosteroids.1

Monitor patients who have a change in vision and those with a history of glaucoma or cataracts.1

Specific Populations

Pregnancy

Category C.1

Use during pregnancy may result in hypoadrenalism in infants; monitor these infants carefully.1

Lactation

Not known whether mometasone furoate is distributed into milk; caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established in children <2 years of age.1

Intranasal corticosteroids may reduce growth velocity in pediatric patients.1 Routine monitoring of growth (e.g., via stadiometry) recommended.1 Titrate dosage to the lowest possible effective level.1

Geriatric Use

Adverse effects profiles similar to those in younger adults.1

Common Adverse Effects

Headache, viral infection, pharyngitis, epistaxis/blood-tinged mucus, coughing, upper respiratory tract infection, dysmenorrhea, musculoskeletal pain, sinusitis, vomiting.1 a

Mometasone Furoate Pharmacokinetics

Absorption

Bioavailability

Bioavailability <0.1% administered as a nasal spray; virtually undetectable in plasma.1 2 11

Onset

Symptomatic relief may be evident within 5–11 hours after the initial dose.1 2 9 1 2 Maximum benefit is usually achieved within 1–2 weeks.1

Distribution

Extent

Not known whether mometasone furoate crosses the placenta or distributes into breast milk.1

Plasma Protein Binding

Approximately 98–99%.1

Elimination

Metabolism

Swallowed portion of dose is extensively metabolized to multiple derivatives;1 a minor metabolite is formed by CYP3A4.1

Elimination Route

Excreted as metabolites principally via bile and to a lesser extent in urine.1

Half-life

5.8 hours.1

Actions

  • Inhibits multiple cell types (e.g., mast cells, macrophages, lymphocytes, monocytes, plasma cells) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation.2 11 a

  • Inhibits the expression of inflammatory mediators by cells involved in both the early and late phases of the allergic response,2 including reduced histamine and eosinophil cationic protein levels and reduced eosinophils, neutrophils, and epithelial adhesion proteins.a

  • Decreases nasal reactivity to allergensd and reduces intraepithelial eosinophilia and infiltration of inflammatory cells (e.g., eosinophils, lymphocytes, monocytes, neutrophils, plasma cells) in nasal mucosa.1 11 a

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