Momeclir

White to off-white opaque suspension supplied with a metered-dose nasal spray.
Each mL contains: Mometasone Furoate 500 mcg (140 metered actuations).

Pharmacotherapeutic group: Decongestants and other nasal preparations for topical use-corticosteroids.
Pharmacology: Pharmacodynamics: Mechanism of Action: 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 anti-allergic 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 leukocytes of allergic patients. In cell culture, mometasone furoate demonstrated high potency in inhibition of synthesis and release of IL-1, IL-5, IL-6 and TNFα; it is also a potent inhibitor of leukotriene production. In addition, it is an extremely potent inhibitor of the production of the Th2 cytokines, IL-4 and IL-5, from human CD4+ T-cells.
Pharmacodynamic effects: In studies utilizing nasal antigen challenge, Mometasone furoate nasal spray suspension 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 suspension 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.
Pediatric population: In a placebo-controlled clinical trial in which pediatric patients (n=49/group) were administered Mometasone furoate nasal spray 100 micrograms daily for one year, no reduction in growth velocity was observed.
There are limited data available on the safety and efficacy of Mometasone furoate nasal spray in the pediatric population aged 3 to 5 years, and an appropriate dosage range cannot be established. In a study involving 48 children aged 3 to 5 years treated with intranasal Mometasone furoate 50, 100 or 200 μg/day for 14 days, there was no significant differences from placebo in the mean change in plasma cortisol level in response to the tetracosactrin stimulation test.
The European Medicines Agency has waived the obligation to submit the results of studies with Mometasone furoate Nasal spray suspension in all subsets of the pediatric population in seasonal and perennial allergic rhinitis.
Pharmacokinetics: Absorption: Mometasone furoate, administered as an aqueous nasal spray suspension, has a systemic bioavailability of <1% in plasma, using a sensitive assay with a lower quantitation limit of 0.25 pg/mL.
Distribution: Not applicable as Mometasone is poorly absorbed via the nasal route.
Biotransformation: The small amount that may be swallowed and absorbed undergoes extensive first-pass hepatic metabolism.
Elimination: Absorbed Mometasone furoate is extensively metabolized and the metabolites are excreted 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 fetal growth (lower fetal 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 concentration 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 tumor types.

Mometasone furoate (Momeclir) Nasal spray suspension is indicated for use in adults and children 2 years of age and older to treat the symptoms of seasonal allergic or perennial rhinitis. In patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis, prophylactic treatment with Mometasone furoate (Momeclir) Nasal spray suspension may be initiated up to four weeks prior to the anticipated start of the pollen season.
Mometasone furoate (Momeclir) Nasal spray suspension is indicated for the treatment of nasal polyps in adults 18 years of age and older.
Mometasone furoate (Momeclir) Nasal spray suspension is indicated for the treatment of acute rhinosinusitis without severe bacterial infection in adults and children 12 years of age and older.

After initial priming of the Mometasone furoate nasal spray pump (10 actuations until a uniform spray is observed), each actuation delivers approximately 100 mg of mometasone furoate suspension containing 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.
Seasonal or Perennial Allergic Rhinitis: Adults (including geriatric patients) and children 12 years of age and older: 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.
Children between the ages of 6 and 11 years: The usual recommended dose is one actuation (50 micrograms/actuation) in each nostril once daily (total dose 100 micrograms).
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). The dose should be titrated to the lowest dose at which effective control of symptoms is maintained. 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 (Momeclir) Nasal spray suspension for the treatment of nasal polyposis were four months in duration.
Acute Rhinosinusitis: The usual recommended starting dose for acute rhinosinusitis is two actuations (50 micrograms/actuation) in each nostril twice daily (total dose of 400 micrograms).

Hypersensitivity to any ingredients of Mometasone furoate (Momeclir) Nasal spray suspension.
Mometasone furoate (Momeclir) Nasal spray suspension should not be used in the presence of untreated localized infection involving the nasal mucosa.
Because of the inhibitory effects 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 furoate (Momeclir) Nasal spray suspension 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.
Local nasal effects: Following 12 months of treatment with Mometasone furoate (Momeclir) Nasal spray suspension 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 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 Mometasone furoate (Momeclir) Nasal spray suspension therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing Mometasone furoate (Momeclir) Nasal spray suspension.
Non-nasal symptoms: Although Mometasone furoate (Momeclir) Nasal spray suspension 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.
There is no evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression following prolonged treatment with Mometasone furoate (Momeclir) Nasal spray suspension. However, patients who are transferred from long-term administration of systemically active corticosteroids to Mometasone furoate (Momeclir) Nasal spray suspension 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 corticosteroids administration should be resumed and other modes of therapy and appropriate measures instituted.
During transfer from systemic corticosteroids to Mometasone furoate (Momeclir) Nasal spray suspension, 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 Mometasone furoate (Momeclir) Nasal Spray suspension. Such transfer may also unmask pre-existing allergic conditions, such as allergic conjunctivitis and eczema, previously suppressed by systemic corticosteroid therapy.
The safety and efficacy of Mometasone furoate (Momeclir) Nasal spray suspension 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.
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 corticosteroids, instances of nasal septum perforation or increased intraocular pressure have been reported very rarely.
Safety 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 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 patients to a pediatric specialist.
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 the additional systemic corticosteroid cover should be considered during periods of stress or elective surgery.

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

Treatment-related adverse events reported in clinical studies for allergic rhinitis in adult and adolescent patients are shown as follows (Table 1). (See Table 1.)

Click on icon to see table/diagram/image

Epistaxis was generally self-limiting and mild in severity, and occurred at 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%). The incidence of all other effects was comparable with that of placebo.
In the pediatric population, the incidence of adverse events, e.g., epistaxis (6%), headache (3%), nasal irritation (2%) and sneezing (2%) was comparable with that of placebo.
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.
Treatment-related adverse events in 1% of patients in clinical studies for polyposis are shown as follows (Table 2). (See Table 2.)

Click on icon to see table/diagram/image

In patients treated for acute rhinosinusitis, the incidence of epistaxis for Mometasone furoate (Momeclir) Nasal spray suspension was 3.3% vs. 2.6% for placebo and similar to that observed for patients treated with allergic rhinitis.
Rarely, immediate hypersensitivity reactions, including bronchospasm and dyspnea, may occur after intranasal administration of Mometasone furoate. Very rarely, anaphylaxis and angioedema have been reported.
Disturbances of taste and smell have been reported very rarely.
As with other intranasal corticosteroids rare cases of nasal septum perforation have been reported.
Systemic effects of nasal corticosteroids may occur, particularly when prescribed at high doses for prolonged periods.
Rare cases of glaucoma, increased intraocular pressure and/or cataracts have been reported with the use of intranasal corticosteroids.

(See Precautions for use with systemic corticosteroids).
A clinical interaction study was conducted with loratadine. No interactions were observed.

Store at temperatures not exceeding 30°C.

Nasal Decongestants & Other Nasal Preparations

D07AC13 - mometasone ; Belongs to the class of potent (group III) corticosteroids. Used in the treatment of dermatological diseases.

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