Nasonex

Mometasone furoate.

Each metered-dose pump actuation of Nasonex aqueous nasal spray delivers approximately mometasone furoate suspension 100 mg, containing mometasone furoate monohydrate equivalent to mometasone furoate 50 mcg. It also contains cellulose, glycerol, citric acid monohydrate, sodium citrate dihydrate, polysorbate 80 and purified water as inactive ingredients. It also contains benzalkonium chloride 0.2 mg/g and phenylethyl alcohol 2.5 mg/g as preservatives.
Nasonex aqueous nasal spray is a metered-dose, manual pump spray unit containing a suspension of mometasone furoate.

Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties at doses that are not systemically active.
It is likely that much of the mechanism for the antiallergic and anti-inflammatory effects of mometasone furoate lies in its ability to inhibit the release of mediators of allergic reactions. Mometasone furoate significantly inhibits the release of leukotrienes from leucocytes of allergic patients. In cell culture, mometasone furoate demonstrated potency in inhibition of synthesis and release of IL-l, IL-5, IL-6 and TNFα. It is also a potent inhibitor of leukotriene production. In addition, it is an inhibitor of the production of the Th 2 cytokines IL-4 and IL-5, from human CD4+ T-cells. In studies utilizing nasal antigen challenge, Nasonex aqueous nasal spray has shown anti-inflammatory activity in both the early- and late-phase allergic responses. This has been demonstrated by decreases (vs placebo) in histamine and eosinophil activity and reductions (vs baseline) in eosinophils, neutrophils and epithelial cell adhesion proteins. In patients with seasonal allergic rhinitis, Nasonex aqueous nasal spray demonstrated a clinically significant onset of action within 12 hrs after the 1st dose.
Pharmacokinetics: Mometasone furoate, administered as a nasal spray, has negligible (≤0.1%) systemic bioavailability and is generally undetectable in plasma, despite the use of sensitive assay with a lower quantitation limit of 50 pg/mL; thus, there are no relevant pharmacokinetic data for this dosage form. Mometasone furoate suspension is very poorly absorbed from the gastrointestinal tract, and the small amount that may be swallowed and absorbed undergoes extensive first-pass hepatic metabolism prior to excretion in urine and bile.

Treatment of symptoms of seasonal or perennial rhinitis, especially in moderate to severe persistent allergy in adults, adolescents and children between the age of 2 and 11 years.
Treatment of nasal polyps in adult patients ≥18 years.
Treatment of symptoms associated with mild to moderate uncomplicated acute rhinosinusitis in adults and children ≥12 years where signs or symptoms of bacterial infection are not present.

Seasonal Allergic or Perennial Rhinitis: After initial priming of Nasonex aqueous nasal spray (usually 6 or 7 actuations until a uniform spray is released), each actuation delivers approximately 100 mg of mometasone furoate suspension, containing mometasone furoate monohydrate equivalent to mometasone furoate 50 mcg. Prior to administration of the 1st dose, shake container well and actuate pump well before each use. If Nasonex has not been used for 14 days or longer, it should be reprimed before next use.
Adults (Including the Elderly) and Children ≥12 years: The usual recommended dose for prophylaxis and treatment, 2 sprays (50 mcg/spray) in each nostril once daily (total dose 200 mcg). Once symptoms are controlled, dose reduction to 1 spray in each nostril (total dose 100 mcg) may be effective for maintenance.
If symptoms are inadequately controlled, the dose may be increased to a maximum daily dose of 4 sprays in each nostril once daily (total dose 400 mcg). Dose reduction is recommended following control of symptoms.
Children 2-11 years: The usual recommended dose is 1 spray (50 mcg/spray) in each nostril once daily (total dose 100 mcg).
Administration to young children should be aided by an adult.
Nasonex aqueous nasal spray demonstrates a clinically significant onset of action within 12 hrs after the 1st dose in some patients with seasonal allergic rhinitis; this was also shown in a clinical trial with Nasonex aqueous nasal spray. However, full benefit of treatment may not be achieved in the first 48 hrs. Therefore, the patient should continue regular use to achieve full therapeutic benefit.

Because of the negligible (≤0.1%) systemic bioavailability of Nasonex, overdose is unlikely to require any therapy other than observation, followed by initiation of the appropriate prescribed dosage.

Hypersensitivity to any ingredients of Nasonex. It should not be used in the presence of untreated localized infection involving the nasal mucosa. Because of the inhibitory effect of corticosteroids on wound healing, patients who have experienced recent nasal surgery or trauma; hence, the patient should not use a nasal corticosteroid until healing has occurred.

Nasonex should not be used in the presence of untreated localized infection involving the nasal mucosa.
Because of the inhibitory effect of corticosteroids on wound healing, patients who have experienced recent nasal surgery or trauma should not use a nasal corticosteroid until healing has occurred.
Following 12 months of treatment with Nasonex, there was no evidence of atrophy of the nasal mucosa; also, mometasone furoate tended to reverse the nasal mucosa closer to a normal histologic phenotype. As with any long-term treatment, patients using Nasonex over several months or longer should be examined periodically for possible changes in the nasal mucosa. If localized fungal infection of the nose or pharynx develops, discontinuance of Nasonex or appropriate treatment may be required. Persistent nasopharyngeal irritation may be an indication for discontinuing Nasonex.
Nasonex should be used with caution, if at all, in patients with active or quiescent tuberculous infections of the respiratory tract, or in untreated fungal, bacterial, systemic viral infections or ocular herpes simplex.
There is no evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression following prolonged treatment with Nasonex. However, patients who are transferred from long-term administration of systemically active corticosteroids to Nasonex require careful attention. Systemic corticosteroid withdrawal in such patients may result in adrenal insufficiency for a number of months until recovery of HPA axis function. If these patients exhibit signs and symptoms of adrenal insufficiency, systemic corticosteroid administration should be resumed and other modes of therapy and appropriate measures should be instituted.
During transfer from systemic corticosteroids to Nasonex, some patients may experience withdrawal symptoms from systemically active corticosteroids (eg, joint and/or muscle pain, lassitude and depression initially) despite relief from nasal symptoms and will require encouragement to continue Nasonex therapy. Such transfer may also unmask preexisting allergic conditions eg, allergic conjunctivitis and eczema, previously suppressed by systemic corticosteroid therapy.
Patients receiving corticosteroids who are potentially immunosuppressed should be warned of the risk of exposure to certain infections (eg, chickenpox, measles) and of the importance of obtaining medical advice if such exposure occurs.
Following the use of intranasal aerosolized corticosteroids, instances of nasal septum perforation or increased intraocular pressure have been reported very rarely.
Systemic effects of nasal corticosteroids may occur, particularly at high doses prescribed for prolonged periods. Growth retardation has been reported in children receiving nasal corticosteroids at licensed doses.
Treatment with higher than recommended doses may result in clinically significant adrenal suppression. If there is evidence for higher than recommended doses being used, then additional systemic corticosteroid cover should be considered during periods of stress or elective surgery.
Use in pregnancy & lactation: There are no adequate or well-controlled studies in pregnant women. Following intranasal administration of the maximal recommended clinical dose to patients, mometasone plasma concentrations are not measurable; thus, fetal exposure is expected to be negligible and the potential for reproductive toxicity is very low.
As with other nasal corticosteroid preparations, Nasonex should not be used in pregnant women, nursing mothers or women of childbearing age unless the potential benefit justifies the potential risk to the mother, fetus or infant. Infants born of mothers who received corticosteroids during pregnancy should be observed carefully for hypoadrenalism.
Use in children: It is recommended that the height of children receiving prolonged treatment with nasal corticosteroids be regularly monitored. If growth is slow, therapy should be reviewed with the aim of reducing the dose of nasal corticosteroid, if possible to the lowest dose at which effective control of symptoms is maintained. In addition, consideration should be given to referring patient to a pediatric specialist.

There are no adequate or well-controlled studies in pregnant women. Following intranasal administration of the maximal recommended clinical dose to patients, mometasone plasma concentrations are not measurable; thus, fetal exposure is expected to be negligible and the potential for reproductive toxicity is very low.
As with other nasal corticosteroid preparations, Nasonex should not be used in pregnant women, nursing mothers or women of childbearing age unless the potential benefit justifies the potential risk to the mother, fetus or infant. Infants born of mothers who received corticosteroids during pregnancy should be observed carefully for hypoadrenalism.

Treatment-related local adverse events reported in clinical studies include headache (8%), epistaxis (ie, frank bleeding, blood-tinged mucus and blood fleck) (8%), pharyngitis (4%), nasal burning (2%) nasal irritation (2%) and nasal ulceration (1%), which were typically observed with the use of a corticosteroid nasal spray. Epistaxis was generally self-limiting and mild in severity, and occurred at a higher incidence compared to placebo (5%), but at a comparable or lower incidence compared to active control nasal corticosteroids studied (up to 15%). The incidence of all other effects was comparable with that of placebo.
In the pediatric population, the incidence of adverse effects eg, headache (3%), epistaxis (6%), nasal irritation (2%) and sneezing (2%) was comparable to placebo.

Store between 2°-25°C. Do not freeze.

Nasal Decongestants & Other Nasal Preparations

R01AD09 - mometasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.

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