Mometasone furoate monohydrate.
NASONEX Aqueous Nasal Spray is a metered-dose, manual pump spray unit containing a suspension of mometasone furoate. Each metered-dose pump actuation of NASONEX Aqueous Nasal Spray delivers approximately 100 mg of mometasone furoate suspension, containing mometasone furoate monohydrate equivalent to 50 micrograms mometasone furoate.
Excipients/Inactive Ingredients: cellulose, glycerol, citric acid monohydrate, sodium citrate dihydrate, polysorbate 80 and purified water.
Preservatives: benzalkonium chloride 0.2 mg/g.
Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties at doses that are not systemically active.
Pharmacology: Pharmacodynamics: In studies utilizing nasal antigen challenge, mometasone furoate in 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. Because of the low systemic availability of mometasone furoate after intranasal administration, any pharmacodynamic correlations have to be based upon sensitive indices of possible systemic exposure rather than measured mometasone furoate levels. Systemic activity of exogenous corticosteroids is commonly expressed by evaluating the hypothalamic-pituitary-adrenal (HPA) axis activity.
Pharmacokinetics: Mometasone furoate monohydrate, administered as an aqueous nasal spray, has a systemic bioavailability of <1% in plasma, using a sensitive assay with a lower quantitation limit (LLOQ) of 0.25 pg/ml. 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.
Seasonal or Perennial Rhinitis: NASONEX Aqueous Nasal Spray is indicated for use in adults, adolescents, and children between the ages of 2 and 11 years to treat the symptoms of seasonal or perennial rhinitis.
In patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis, prophylactic treatment with NASONEX Aqueous Nasal Spray is recommended two to four weeks prior to the anticipated start of the pollen season.
Treatment of Nasal Congestion Associated with Seasonal Allergic Rhinitis: NASONEX Aqueous Nasal Spray is indicated for the relief of nasal congestion associated with seasonal allergic rhinitis, in adults and pediatric patients 2 years of age and older.
Adjunctive Treatment of Acute Episodes of Sinusitis: NASONEX Aqueous Nasal Spray is also indicated for use in adults and adolescents 12 years of age and older as adjunctive treatment to antibiotics for acute episodes of sinusitis.
Adjunctive treatment of acute episodes of sinusitis.
Nasal Polyposis: NASONEX Aqueous Nasal Spray is also indicated for the treatment of nasal polyps and associated symptoms including congestion and loss of smell in adults patients 18 years of age and older.
Acute Rhinosinusitis: NASONEX Aqueous Nasal Spray is also indicated for the treatment of symptoms associated with acute rhinosinusitis in patients 12 years of age and older without signs or symptoms of bacterial infection.
Seasonal or Perennial Rhinitis: Adults (including geriatric patients) and adolescents: The usual recommended dose for prophylaxis and treatment is two sprays (50 micrograms/spray) in each nostril once daily (total dose 200 micrograms). Once symptoms are controlled, dose reduction to one spray in each nostril (total dose 100 micrograms) may be effective for maintenance.
If symptoms are inadequately controlled, the dose may be increased to a maximum daily dose of four sprays in each nostril once daily (total dose 400 micrograms). Dose reduction is recommended following control of symptoms.
Clinically significant onset of action occurs as early as 12 hours after the first dose.
Children between the ages of 2 and 11 years: The usual recommended dose is one spray (50 micrograms/spray) in each nostril once daily (total dose 100 micrograms).
Administration to young children should be aided by an adult.
Treatment of Nasal Congestion Associated with Seasonal Allergic Rhinitis: Adults and adolescents 12 years of age and older: The recommended dose for treatment of nasal congestion associated with seasonal allergic rhinitis is two sprays (50 mcg of mometasone furoate in each spray) in each nostril once daily (total daily dose of 200 mcg).
Children 2 to 11 years of age: The recommended dose for treatment of nasal congestion associated with seasonal allergic rhinitis is one spray (50 mcg of mometasone furoate in each spray) in each nostril once daily (total daily dose of 100 mcg).
Adjunctive Treatment of Acute Episodes of Sinusitis: Adults (including geriatric patients) and adolescents 12 years of age and older: The usual recommended dose is two sprays (50 micrograms/spray) in each nostril twice daily (total dose 400 micrograms).
If symptoms are inadequately controlled, the dose may be increased to four sprays (50 micrograms/spray) in each nostril twice daily (total dose 800 micrograms).
Nasal Polyposis: Adults (including geriatric patients) and adolescents 18 years of age and older: The usual recommended dose for polyposis is two sprays (50 micrograms/spray) in each nostril twice daily (total daily dose of 400 micrograms). Once symptoms are adequately controlled, dose reduction to two sprays in each nostril once daily (total daily dose 200 micrograms) is recommended.
Acute Rhinosinusitis: The usual recommended dose for acute rhinosinusitis is two actuations (50 micrograms/actuation) in each nostril twice daily (total daily dose of 400 micrograms). If symptoms worsen during treatment, the patients should be advised to consult their physician.
Mode of Administration: After initial priming of the NASONEX Aqueous Nasal Pump (10 actuations, until a uniform spray is observed), each actuation delivers approximately 100 mg of mometasone furoate suspension, containing mometasone furoate monohydrate equivalent to 50 micrograms mometasone furoate. If the spray pump has not been used for 14 days or longer it should be re-primed 2 actuations, until a uniform spray is observed before next use.
Shake container well before each use.
Because the systemic bioavailability of NASONEX Aqueous Nasal Spray is <1% (using a sensitive assay with a lower quantitation limit of 0.25 pg/mL), overdose is unlikely to require any therapy other than observation, followed by initiation of the appropriate prescribed dosage.
Inhalation or oral administration of excessive doses of corticosteroids may lead to suppression of Hypothalamic-Pituitary-Adrenal axis function.
Hypersensitivity to any ingredients of NASONEX Aqueous Nasal Spray.
NASONEX Aqueous Nasal Spray 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 Aqueous Nasal Spray, 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 Aqueous Nasal Spray 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 Aqueous Nasal Spray therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing NASONEX Aqueous Nasal Spray.
NASONEX Aqueous Nasal Spray 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 of ocular herpes simplex.
There is no evidence of Hypothalamic-Pituitary-Adrenal (HPA) axis suppression following prolonged treatment with NASONEX Aqueous Nasal Spray. However, patients who are transferred from long-term administration of systemically active corticosteroids to NASONEX Aqueous Nasal Spray 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 instituted.
In a placebo-controlled clinical trial in which pediatric patients were administered NASONEX Aqueous Nasal Spray 100 micrograms daily for one year, no reduction in growth velocity was observed.
Safety and efficacy of NASONEX Aqueous Nasal Spray for the treatment of nasal polyposis in children and adolescents less than 18 years of age have not been studied.
During transfer from systemic corticosteroids to NASONEX Aqueous Nasal Spray, some patients may experience symptoms of withdrawal from systemically active corticosteroids (e.g. joint and/or muscular pain, lassitude and depression initially) despite relief from nasal symptoms and will require encouragement to continue NASONEX Aqueous Nasal Spray therapy. Such transfer may also unmask pre-existing allergic condition such as 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 (e.g., 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.
Visual disturbance may be reported with systemic and topical (including, intranasal, inhaled and intraocular) corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes of visual disturbances which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids.
Acute Rhinosinusitis: If signs or symptoms of severe bacterial infection are observed (such as fever, persistent severe unilateral facial/tooth pain, orbital, or peri-orbital facial swelling, or worsening of symptoms after an initial improvement), the patient should be advised to consult their physician immediately.
Use in Children: Safety and efficacy of NASONEX Aqueous Nasal Spray for the treatment of symptoms of rhinosinusitis in children under 12 years of age have not been studied.
There are no adequate or well controlled studies in pregnant women. As with other nasal corticosteroid preparations, NASONEX Aqueous Nasal Spray should be used in pregnant women, nursing mother or women of childbearing age only if 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.
Seasonal Allergic or Perennial Rhinitis:
Treatment-related local adverse events reported in clinical studies in adult patients and adolescents include headache (8%), epistaxis (i.e. frank bleeding, blood-tinged mucus, and blood flecks) (8%), pharyngitis (4%), nasal burning (2%), nasal irritation (2%) and nasal ulceration (1%), which are typically observed with 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, e.g., headache (3%), epistaxis (6%), nasal irritation (2%) and sneezing (2%) was comparable to placebo.
Rarely, immediate hypersensitivity reactions (e.g. bronchospasm, dyspnea) may occur after intranasal administration of mometasone furoate monohydrate. Very rarely, anaphylaxis and angioedema have been reported.
Disturbances of taste and smell have been reported very rarely.
Nasal Congestion Associated with Seasonal Allergic Rhinitis:
A total of 1008 patients aged 12 years and older received NASONEX Aqueous Nasal Spray 200 mcg/day (n = 506) or placebo (n = 502) for 15 days. Adverse events that occurred more frequently in patients treated with NASONEX Aqueous Nasal Spray than in patients with the placebo included sinus headache (1.2% in NASONEX Aqueous Nasal Spray group vs. 0.2% in placebo) and epistaxis (1% in NASONEX Aqueous Nasal Spray group vs. 0.2% in placebo) and the overall adverse event profile was similar to that observed in the other allergic rhinitis trials.
Adjunctive Treatment of Acute Episodes of Sinusitis:
In adult and adolescent patients receiving NASONEX Aqueous Nasal Spray as adjunctive treatment for acute episodes of sinusitis, treatment-related adverse events, which occurred at an incidence comparable to placebo, included headache (2%), pharyngitis (1%), nasal burning (1%) and nasal irritation (1%). Epistaxis was mild in severity and also occurred at an incidence comparable to placebo (5% vs. 4%, respectively).
In patients treated for nasal polyposis, the overall incidence of adverse events was comparable to placebo and similar to that observed for patients with allergic rhinitis.
In patients treated for acute rhinosinusitis, the overall incidence of adverse events was comparable to placebo and similar to that observed for patients with allergic rhinitis.
The following additional adverse reactions have been reported in post-marketing use with NASONEX Aqueous Nasal Spray: vision blurred.
NASONEX Aqueous Nasal Spray has been administered concomitantly with loratadine with no apparent effect on plasma concentrations of loratadine or its major metabolite. In these studies mometasone furoate plasma concentrations were not detectable using an assay with a LLOQ of 50 pg/mL. The combination therapy was well tolerated.
Mometasone furoate is metabolized by CYP3A4.
Coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, cobicistat-containing products) may lead to increased plasma concentrations of corticosteroids and potentially increase the risk for systemic corticosteroid side-effects. Consider the benefit of coadministration versus the potential risk of systemic corticosteroid effects, in which case patients should be monitored for systemic corticosteroid side-effects.
Instructions for Use: Proper administration of NASONEX Aqueous Nasal Spray is essential to achieve maximum efficacy and minimize the risk of complications. For optimal compliance, NASONEX Aqueous Nasal Spray dosage and administration guidelines should be reinforced with patients before therapy is started. Instructions for use are as follows: Shake the NASONEX Aqueous Nasal Spray container well before use. Read complete instructions carefully and use only as directed.
1. Remove dust cap.
2. NASONEX Aqueous Nasal Spray must be primed before using for the first time. Do not pierce the nasal applicator. To prime, press up and down on the white collar, using the forefinger and middle finger while supporting the base of the bottle with the thumb 10 times until a fine spray appears. The pump is now ready for use. If the spray pump has not been used for 14 days or longer, it should be re-primed 2 times, until a fine spray appears.
3. Shake container well before each use.
4. Gently blow the nose to clear the nostrils. Close one nostril. Tilt the head forward slightly and, keeping the bottle upright, carefully insert the nasal applicator into the other nostril.
5. For each spray press firmly downwards once on the white collar, using the forefinger and middle finger while supporting the base of the bottle with the thumb. Breathe gently inwards through the nostril.
6. Repeat in other nostril.
7. Replace the plastic dust cap.
Cleaning: It is important to clean the nasal spray regularly, otherwise it may not work properly. Remove the plastic dust cap and gently pull off the nozzle. Wash the nozzle and dust cap in warm water and then rinse under a running tap. Do not try to unblock the nasal applicator by inserting a pin or other sharp object as this will damage the applicator and cause not to get the right dose of medicine. Allow to dry in a warm place. Push the nozzle back onto the bottle and replace the dust cap. The spray will need to be re-primed with 2 sprays when first used after cleaning.
Store in a cool place, below 30°C. Do not freeze. Store away from heat.
R01AD09 - mometasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
Aqueous nasal spray 50 mcg/dose x 60 doses, 140 doses.