Monitazone

Mometasone furoate.

1mL contains Mometasone Furoate 0.5mg.

Pharmacology: Pharmacodynamics: 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 or allergic reactions. Mometasone furoate significantly inhibits the release of leukotrienes from leucocytes 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.
Pharmacokinetics: Mometasone furoate, administered as an aqueous nasal spray, has a systemic bioavailability of <1% in plasma, using a sensitive assay with a lower quantitation limit 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.

Adults and pediatric patients 2 years of age and older: Treatment and prophylaxis of the nasal symptoms of seasonal allergic rhinitis; Treatment of perennial allergic rhinitis; Initiation of prophylaxis is recommended 2 to 4 weeks prior to the anticipated start of the pollen season.
Treatment of nasal polyps in patients 18 years of age and older.
Treatment of acute episodes of sinusitis as adjunctive treatment to antibiotics in patients 12 years of age and older.

Allergic rhinitis: Mometasone Furoate suspension is emitted about 100mg in each spray and it contains 0.05mg of Mometasone Furoate (on the anhydrous basis). For uniform spraying. use it after 10 test sprays. If the spray pump has not been used for 14 days or longer, it should be 2 test sprays again before next use
Adults (including geriatric patients) and children 12 years of age and older: The usual recommended dose is 2 sprays in each nostril once daily (total daily dose of 0.2mg). Once symptom are controlled, dose reduction to 1 spray in each nostril (total daily dose of 0.1mg). If symptoms are inadequately controlled, the dose may be increased to a maximum daily dose of 4 sprays in each nostril once daily (total daily dose of 0.4mg). Dose reduction is recommended following control of symptoms. The patient should continue regular use to achieve full therapeutic benefit.
Children 2 to 11 Years of Age: The recommended dose is 1 spray in each nostril once daily (total daily dose of 0.1mg).
Nasal polyps: The usual recommended dose is 2 sprays in each nostril once daily (total daily dose of 0.2mg). If symptoms are inadequately controlled after 5-6 weeks, the dose may be increased to a maximum daily dose of 2 sprays in each nostril twice daily (total daily dose of 0.4mg). Dose reduction is recommended following control of symptoms. If symptoms are still inadequately controlled, other therapy is recommended. There is no evidence that the spray has been used more than 4 months for nasal polyps therapy.
Acute episodes of sinusitis: The recommended dose is 2 sprays in each nostril twice daily (total daily dose of 0.4mg).

Because of the negligible (≤ 0.1%) systemic bioavailability of Monitazone, 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 HPA axis function.

Hypersensitivity to any ingredients of Monitazone Nasal spray.
Monitazone Nasal spray should not be used in the presence of untreated localised 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.

Careful administration: Patients with active or quiescent tuberculous infections of the respiratory tract, or in untreated fungal, bacterial, systemic viral infections or ocular herpes simplex.
General Precautions: Following 12 months of treatment with Mometasone Furoate, 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 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 therapy or appropriate treatment may be required. Persistence of nasopharyngeal inflation may be an indication for discontinuing Monitazone Nasal spray.
Although Mometasone Furoate 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. However, patients who are transferred from long-term administration of systemically active corticosteroids to Mometasone Furoate 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.
During transfer from systemic corticosteroids to Mometasone Furoate. Some patients may experience symptoms of withdrawal from systemically active corticosteroids (e.g. joint and/or muscular pain, lassitude, and depression initially) despite relief to continue with Mometasone Furoate therapy. Such transfer may also unmask pre-existing allergic conditions 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.

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 foetal exposure is expected to be negligible and the potential for reproductive toxicity very low.
As with other nasal corticosteroid preparations, Monitazone Nasal spray should not be used in pregnancy or lactation 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.

In controlled US and international clinical studies, a total of 3210 adult and adolescent patients 12 years and older with allergic rhinitis received treatment with Mometasone Furoate at doses of 50 to 800μg/day. The majority of patients (n = 2103) were treated with 200 μg/day. In controlled US and international clinical studies, a total of 990 pediatric patients (3 to 11 years) with allergic rhinitis received treatment with Mometasone Furoate at doses of 25 to 200μg/day. The majority of patients (n = 720) were treated with 100μg/day. A total of 513 adult and pediatric patients have been treated for one year or longer. Adverse events did not differ significantly based on age, sex, or race. Four percent or less of patients in clinical trials discontinued treatment because of adverse events and the discontinuation rate was similar for the vehicle and active comparators.
All adverse events (regardless of relationship to treatment) reported by 5% or more of adult and adolescent patients ages 12 years and older who received Mometasone Furoate, 200μg/day and pediatric patients ages 3 to 11 years who received Mometasone Furoate, 100μg/day vs. placebo and that were more common with Mometasone Furoate than placebo, are displayed in table as follows. (See table.)

Click on icon to see table/diagram/image

Other adverse events which occurred in less than 5% but greater than or equal to 2% of adult and adolescent patients (ages 12 years and older) treated with Mometasone Furoate, 200μg/day (regardless of relationship to treatment), and more frequently than in the placebo group included: arthralgia, asthma, bronchitis, chest pain, conjunctivitis, diarrhea, dyspepsia, earache, flu-like symptoms, myalgia, nausea, and rhinitis.
Other adverse events which occurred in less than 5% but greater than or equal to 2% of adult and adolescent patients (ages 3 to 11 years) treated with Mometasone Furoate, 100μg/day (regardless of relationship to treatment), and more frequently than in the placebo group included: diarrhea, nasal irritation, otitis media, wheezing.
The adverse event (regardless of relationship to treatment) reported by 5% of pediatric patients ages 2 to 5 years who received Mometasone Furoate 100μg/day in a clinical trial vs. placebo including 56 subjects (28 each Mometasone Furoate and placebo) and that was more common with Mometasone Furoate than placebo, included: upper respiratory tract infection (7% vs. 0%, respectively). The other adverse event which occurred in less than 5% but greater than or equal to 2% of mometasone furoate pediatric patients ages 2 to 5 years treated with 100μg doses vs. placebo (regardless of relationship to treatment) and more frequently than in the placebo group included: skin trauma.
Nasal ulcers and nasal and oral candidiasis were also reported in patients treated with Mometasone Furoate primarily in patients treated for longer than 4 weeks.
The following adverse reactions have been identified during the post-marketing period for Mometasone Furoate: nasal burning and irritation, anaphylaxis and angioedema, disturbances in taste and smell and nasal septal perforation. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
In controlled clinical studies, the types of adverse events observed in patients with nasal polyps were similar to those observed for patients with allergic rhinitis.

No formal drug-drug interaction studies have been conducted with Mometasone Furoate. Inhibitors of Cytochrome P450 3A4: Studies have shown that mometasone furoate is primarily and extensively metabolized in the liver of all species investigated and undergoes extensive metabolism to multiple metabolites. In vitro studies have confirmed the primary role of cytochrome CYP 3A4 in the metabolism of this compound. Coadministration with ketoconazole, a potent CYP 3A4 inhibitor, may increase the plasma concentrations of mometasone furoate.

Precaution to administer: Shake applicator well and pump 10 sprays (for uniform spraying) before first use. If the spray pump has not been used for 14 days or longer, it should be 2 test sprays again before next use. Shake well before every use. Do not use Monitazone Nasal spray after 140 sprays or after 2 months from first use.
Do not spray into eyes or the nasal septum (the wall between the two nostrils).

Store below 30°C in tight container.
Shelf life: 24 months.

Nasal Decongestants & Other Nasal Preparations

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

POM

Nasal spray 0.5 mg/mL (white or almost white suspension) x 140 sprays.