Mometasone Sandoz

Mometasone furoate.

Each actuation of the pump delivers a metered dose of 50 micrograms of mometasone furoate (as mometasone furoate monohydrate).
Excipients/Inactive Ingredients: Contains 0.02 mg benzalkonium chloride per actuation.
Microcrystalline cellulose (E460), Carmellose sodium (E468), Glycerol (E442), Citric acid monohydrate (E330), Sodium citrate dihydrate (E331), Polysorbate 80 (E433), Benzalkonium chloride, Purified water.

Pharmacotherapeutic group: Decongestants and other nasal preparations for topical use-corticosteroids. ATC Code: R01A D09.
Pharmacology: Pharmacodynamics: Mechanism of action: Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties.
It is likely that much of the mechanism for the anti-allergic and anti-inflammatory effects of mometasone furoate lies in its ability to inhibit the release of mediators of allergic reactions.
Clinical efficacy and safety: In studies utilising nasal antigen challenge, mometasone furoate 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 28% of the patients with seasonal allergic rhinitis, mometasone furoate nasal spray demonstrated a clinically significant onset of action within 12 hours after the first dose. The median (50%) onset time of relief was 35.9 hours.
Paediatric population: In a placebo-controlled clinical trial in which paediatric patients (n=49/group) were administered mometasone furoate nasal spray 100 micrograms daily for one year, no reduction in growth velocity was observed.
Pharmacokinetics: Mometasone furoate, administered as an aqueous nasal spray, has a negligible (<1%) systemic bioavailability and is generally undetectable in plasma, despite the use of a 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.
Toxicology: Preclinical safety data: No toxicological effects unique to mometasone furoate exposure were demonstrated. All observed effects are typical of this class of compounds and are related to exaggerated pharmacologic effects of glucocorticoids.
Preclinical studies demonstrate that mometasone furoate is devoid of androgenic, antiandrogenic, estrogenic or antiestrogenic activity but, like other glucocorticoids, it exhibits some antiuterotrophic activity and delays vaginal opening in animal models at high oral doses of 56 mg/kg/day and 280 mg/kg/day.
Like other glucocorticoids, mometasone furoate showed a clastogenic potential in-vitro at high concentrations. However, no mutagenic effects can be expected at therapeutically relevant doses.
In studies of reproductive function, subcutaneous mometasone furoate, at 15 micrograms/kg prolonged gestation and prolonged and difficult labour occurred with a reduction in offspring survival and body weight or body weight gain. There was no effect on fertility.
Like other glucocorticoids, mometasone furoate is a teratogen in rodents and rabbits. Effects noted were umbilical hernia in rats, cleft palate in mice and gallbladder agenesis, umbilical hernia, and flexed front paws in rabbits. There were also reductions in maternal body weight gains, effects on foetal growth (lower foetal body weight and/or delayed ossification) in rats, rabbits and mice, and reduced offspring survival in mice.
The carcinogenicity potential of inhaled mometasone furoate (aerosol with CFC propellant and surfactant) at concentrations of 0.25 to 2.0 micrograms/l was investigated in 24-month studies in mice and rats. Typical glucocorticoid-related effects, including several non-neoplastic lesions, were observed. No statistically significant dose-response relationship was detected for any of the tumour types.
The preclinical data show that benzalkonium chloride could have inhibitory effects on the cilia including irreversible standstill, dependent on the concentration and duration of treatment with this excipient. Also, histopathological changes of the nasal mucosa were induced.

Mometasone Sandoz nasal spray is indicated for use in adults, adolescents and children 2 years of age and older to treat the symptoms of seasonal allergic or perennial allergic rhinitis.
In patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis, prophylactic treatment with Mometasone Sandoz nasal spray may be initiated 2 to 4 weeks prior to the anticipated start of the pollen season.
Mometasone Sandoz 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.
Mometasone Sandoz nasal spray is indicated for the symptomatic treatment of nasal polyps in adults 18 years of age and older.
Mometasone Sandoz 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.
Mometasone Sandoz 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.

Posology: Seasonal or perennial allergic rhinitis: The usual recommended dose is two actuations (50 micrograms/actuation) in each nostril once daily (total dose 200 micrograms). Once symptoms are controlled, dose reduction to one actuation 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 actuations in each nostril once daily (total dose 400 micrograms). Dose reduction is recommended following control of symptoms.
Mometasone furoate nasal spray demonstrated a clinically significant onset of action within 12 hours after the first dose in some patients with seasonal allergic rhinitis; however, full benefit of treatment may not be achieved in the first 48 hours. Therefore, the patient should continue regular use to achieve full therapeutic benefit.
Paediatric population: Children between the ages of 2 and 11 years: The usual recommended dose is one actuation (50 micrograms/actuation) in each nostril once daily (total dose 100 micrograms).
Administration to young children should be aided by an adult.
Nasal congestion associated with seasonal allergic rhinitis: Adults and adolescent 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).
Paediatric population: 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).
Nasal polyposis: The usual recommended starting dose for polyposis is two actuations (50 micrograms/actuation) in each nostril once daily (total daily dose of 200 micrograms). If after 5 to 6 weeks symptoms are inadequately controlled, the dose may be increased to a daily dose of two sprays in each nostril twice daily (total daily dose of 400 micrograms). After effective control of symptoms is maintained, the dose should be lowered to once daily. If no improvement in symptoms is seen after 5 to 6 weeks of twice daily administration, alternative therapies should be considered.
Efficacy and safety studies of mometasone furoate nasal spray for the treatment of nasal polyposis were four months in duration.
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).
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.
Method of administration: Mometasone Sandoz is intended only for nasal use.
Before each use container should be shaken well. After initial priming of the Mometasone Sandoz nasal spray 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 reprimed with 2 actuations, until a uniform spray is observed, before next use.

Symptoms: Inhalation or oral administration of excessive doses of corticosteroids may lead to suppression of HPA axis function.
Management: Because the systemic bioavailability of Mometasone Sandoz is <1%, overdose is unlikely to require any therapy other than observation, followed by initiation of the appropriate prescribed dose.

Hypersensitivity to the active substance, mometasone furoate or to any of the excipients.
Mometasone furoate should not be used in the presence of untreated localised infection involving the nasal mucosa, such as herpes simplex.
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.

Immunosuppression: Mometasone Sandoz 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, or systemic viral infections.
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.
Local Nasal Effects: Following 12 months of treatment with mometasone furoate in a study of patients with perennial rhinitis, 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.
Nevertheless, patients using mometasone furoate nasal spray over several months or longer should be examined periodically for possible changes in the nasal mucosa. If localised fungal infection of the nose or pharynx develops, discontinuance of mometasone furoate nasal spray therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing mometasone furoate nasal spray.
Mometasone furoate is not recommended in case of nasal septum perforation (see Adverse Reactions).
In clinical studies, epistaxis occurred at a higher incidence compared to placebo. Epistaxis was generally self-limiting and mild in severity (see Adverse Reactions).
Systemic Effects of Corticosteroids: Systemic effects of nasal corticosteroids may occur, particularly at high doses prescribed for prolonged periods. These effects are much less likely to occur than with oral corticosteroids and may vary in individual patients and between different corticosteroid preparations. Potential systemic effects may include Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, cataract, glaucoma and more rarely, a range of psychological or behavioural effects including psychomotor hyperactivity, sleep disorders, anxiety, depression or aggression (particularly in children).
Following the use of intranasal corticosteroids, instances of increased intraocular pressure have been reported (see Adverse Reactions).
Patients who are transferred from long-term administration of systemically active corticosteroids to mometasone furoate 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 or symptoms of withdrawal (e.g., joint and/or muscular pain, lassitude, and depression initially) despite relief from nasal symptoms, systemic corticosteroid administration should be resumed and other modes of therapy and appropriate measures instituted. Such transfer may also unmask pre-existing allergic conditions, such as allergic conjunctivitis and eczema, previously suppressed by systemic corticosteroid therapy.
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.
Nasal Polyps: The safety and efficacy of mometasone furoate nasal spray has not been studied for use in the treatment of unilateral polyps, polyps associated with cystic fibrosis, or polyps that completely obstruct the nasal cavities.
Unilateral polyps that are unusual or irregular in appearance, especially if ulcerating or bleeding, should be further evaluated.
Following the use of intranasal corticosteroids, instances of nasal septum perforation or increased intraocular pressure have been reported very rarely.
The use of Mometasone Sandoz nasal spray may produce positive results in doping controls.
Mometasone Sandoz nasal spray contains benzalkonium chloride which is irritant and may cause nasal irritation. If used for a longer period, the preservative benzalkonium chloride may cause nasal mucosa swelling. In the case of such a reaction (persistently congested nose) medicinal drugs without a preservative should be used if possible. Unless such products are available another pharmaceutical form should be taken. See also Pharmacology: Toxicology: Preclinical safety data under Actions.
Non-nasal Symptoms: Although mometasone furoate nasal spray will control the nasal symptoms in most patients, the concomitant use of appropriate additional therapy may provide additional relief of other symptoms, particularly ocular symptoms.
Visual disturbance: Visual disturbance may be reported with systemic and topical 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 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.
Effects on ability to drive and use machines: None known.
Use in Children: Safety and efficacy of mometasone furoate nasal spray for the treatment of nasal polyposis in children and adolescents under 18 years have not been studied.
Safety and efficacy of mometasone furoate nasal spray for the treatment of symptoms of rhinosinusitis in children under 12 years of age have not been studied.
Effect on Growth in Paediatric Population: 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.
It is recommended that the height of children receiving prolonged treatment with nasal corticosteroids is regularly monitored. If growth is slowed, 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 the patient to a paediatric specialist.

Pregnancy: There are no or limited amount of data from the use of intranasal mometasone furoate in pregnant women.
Studies in animals have shown reproductive toxicity (see Pharmacology: Toxicology: Preclinical safety data under Actions). As with other nasal corticosteroid preparations, mometasone furoate should not be used in pregnancy unless the potential benefit to the mother justifies any potential risk to the mother, foetus or infant.
Infants born of mothers who received corticosteroids during pregnancy should be observed carefully for hypoadrenalism.
Breast-feeding: It is unknown whether mometasone furoate is excreted in human milk.
As with other nasal corticosteroid preparations, a decision must be made whether to discontinue breast-feeding or to discontinue/abstain from Mometasone Sandoz therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.
Fertility: There are no clinical data concerning the effect of mometasone furoate on fertility. Animal studies have shown reproductive toxicity, but no effects on fertility (see Pharmacology: Toxicology: Preclinical safety data under Actions).

Summary of the safety profile: 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 when compared to the active control nasal corticosteroids studied (up to 15%) as reported in clinical studies for allergic rhinitis. The incidence of all other adverse events was comparable with that of placebo.
In patients treated for nasal polyposis, the overall incidence of adverse events was similar to that observed for patients with allergic rhinitis.
Systemic effects of nasal corticosteroids may occur, particularly when prescribed at high doses for prolonged periods.
List of adverse reactions: Treatment related adverse reactions (≥1%) reported in clinical trials in patients with allergic rhinitis or nasal polyposis and post-marketing regardless of indication are presented. Adverse reactions are listed according to MedDRA primary system organ class. Within each system organ class, adverse reactions are ranked by frequency. Frequencies were defined as follows: Very common (>=1/10), common (>=1/100 to <1/10), uncommon (>=1/1,000 to <1/100). The frequency of post-marketing adverse events are considered as "not known (cannot be estimated from the available data)".
Treatment-related adverse reactions reported by system organ class and frequency: Infections and infestations: Common: Pharyngitis, upper respiratory tract infection^†
Immune system disorders: Not known: Hypersensitivity including anaphylactic reactions, angioedema, bronchospasm and dyspnoea.
Nervous system disorders: Common: Headache.
Eye disorders: Not known: Glaucoma, increased intraocular pressure, cataracts, vision blurred (see Precautions), central serous chorioretinopathy.
Respiratory, thoracic and mediastinal disorders: Very common: Epistaxis*.
Common: Epistaxis, nasal burning, nasal irritation, nasal ulceration.
Not known: Nasal septum perforation.
Gastrointestinal disorders: Common: Throat irritation*.
Not known: Disturbances of taste and smell.
*recorded for twice daily dosing for nasal polyposis.
†recorded at uncommon frequency for twice daily dosing for nasal polyposis.
Paediatric population: In the paediatric population, the incidence of recorded adverse events in clinical studies, e.g., epistaxis (6%), headache (3%), nasal irritation (2%) and sneezing (2%) was comparable to placebo.

(See Precautions for use with systemic corticosteroids.)
A clinical interaction study was conducted with loratadine. No interactions were observed.
Co-treatment with CYP3A inhibitors, including cobicistat-containing products, is expected to increase the risk of systemic side-effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side effects, in which case patients should be monitored for systemic corticosteroid side-effects.

Incompatibilities: Not applicable.
Special precautions for disposal and other handling: Shake well before use.
Any unused product or waste material should be disposed of in accordance with local requirements.
Preparing the nasal spray for use: Mometasone Sandoz Nasal Spray has a dust cap which protects the nozzle and keeps it clean. Take this off before using the spray and replace it after use.
If using the spray for the first time the patient needs to 'prime' the bottle by pumping the spray 10 times until a fine mist is produced: 1. Shake the bottle well.
2. Put the forefinger and middle finger on either side of the nozzle and the thumb underneath the bottle.
3. Point the nozzle away and then press down with the fingers to pump the spray.
If the patient has not used the spray for 14 days or more, the patient needs to "re-prime" the bottle by pumping the spray twice until a fine mist is produced.
At the usual dose of 2 sprays into each nostril once daily, a bottle of Mometasone Sandoz containing 17 g nasal spray suspension should provide enough doses for 30 days (120 sprays) or a bottle containing 18 g provide enough doses for 35 days (140 sprays).
How to use the nasal spray: 1. Shake the bottle well and remove the dust cap.
2. Gently blow nose.
3. Close one nostril and put the nozzle into the other nostril.
4. Tilt the head forward slightly, keeping the bottle upright.
5. Start to breathe in gently or slowly through the nose and whilst breathing in squirt a spray of fine mist into the nose by pressing down ONCE with the fingers.
6. Breathe out through the mouth. Repeat step 5 to inhale a second spray in the same nostril.
7. Remove the nozzle from this nostril and breathe out through the mouth.
8. Repeat steps 3 to 7 for the other nostril.
After using the spray, wipe the nozzle carefully with a clean handkerchief or tissue and replace the dust cap.
Cleaning the nasal spray: It is important to clean the nasal spray regularly, otherwise it may not work properly. Remove the dust cap and gently pull off the nozzle. Wash the nozzle and dust cap in warm water and then rinse under a running tap. 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.

Do not store above 30°C.
Do not freeze.
Shelf-life: After first opening of the bottle: 2 months.

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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