T.O.-Mometasone Aqueous Nasal Spray

T.O.-Mometasone Aqueous Nasal Spray

mometasone

Manufacturer:

Apotex Inc

Distributor:

T O Med

Marketer:

T. O. Chemicals
Full Prescribing Info
Contents
Mometasone furoate.
Description
Each actuation delivers approximately 100 mg of mometasone furoate suspension, containing 50 mcg of mometasone furoate.
T.O.-MOMETASONE is formulated as an aqueous nasal suspension for nasal administration via a metered-spray manual pump spray 100 microliters delivering 140 doses of 50 mcg mometasone furoate.
Action
Pharmacology: Mechanism of Action: Mometasone furoate is a topical glucocorticosteroid with local anti-inflammatory properties at doses that are minimally systemically active. Mometasone furoate is a corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Corticosteroids inhibit the release of arachidonic acid (a precursor of inflammation mediators) by inducing lipocortins that inhibit phospholipase A2. Although the exact anti-inflammatory mechanism is unknown, corticosteroids have a wide range of effects on various cell types (including mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (including histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation.
Following 12 months of therapy with mometasone furoate (200 mcg daily) in patients with allergic rhinitis, a marked reduction in intraepithelial eosinophilia and infiltration of inflammatory cell (eg, eosinophils, lymphocytes, monocytes, neutrophils, and plasma cells) in nasal mucosa was observed.
Pharmacodynamics: Mometasone furoate nasal spray provided rapid onset of symptom relief in the treatment of seasonal allergic rhinitis. Patients then remained within the park over a 12-hour observation period, recording hourly the severity of their symptoms. The mean improvement in total symptom scores (nasal and non-nasal) was significantly greater in the mometasone treatment group, compared with the placebo group at post-dose assessment hours 5 through 12. Morning and evening total symptom/sign scores showed significantly more improvement in the mometasone group than in the placebo group, except for evening assessments during week 2. Unlike the placebo group, the mometasone group had decreased eosinophilic cationic protein, tryptase and albumin levels in nasal lavage fluid, as well as improved nasal airway resistance, mucociliary clearance and olfactory function, at day 15 as compared to baseline.
Intranasal corticosteroids should be considered for first-line therapy of allergic rhinitis. Compared to antihistamines, decongestants, and mast cell stabilizers, intranasal corticosteroids have the following positive effects: (1) They suppress late phase allergic reactions and at least attenuate early phase reactions; (2) They are as effective as oral corticosteroids; (3) They reduce all nasal symptoms; and (4) They relieve upper airway inflammation which reduces seasonal asthma and decreases bronchial hyperreactivity. Clinical studies have also shown that patients prefer intranasal corticosteroids over other treatments. Adverse reactions are usually limited to the nasal mucosa and are usually mild. Systemic adverse effects such as hypothalamic pituitary adrenal axis suppression and subcapsular lens changes are rare. Growth suppression in children has not been confirmed.
Mometasone nasal spray is approved for the treatment of nasal polyps. Nasal congestion and size of polyps were reduced with mometasone nasal spray.
Mometasone furoate aqueous nasal spray safely and effectively controlled the symptoms of seasonal allergic rhinitis in pediatric patients. All patients monitored for HPA axis suppression exhibited normal responses to cosyntropin stimulation. All active treatments were well tolerated; adverse events were mild or moderate in severity, with headache and epistaxis most frequently reported.
Pharmacokinetics: Absorption: Mometasone furoate monohydrate, administered as a nasal spray, has a systemic bioavailability of <1% in plasma, and is virtually undetectable in plasma following administration of a single 400-mcg intranasal dose in healthy adults.
Distribution: Volume distribution of mometasone furoate is 152 L.
The in vitro protein binding for mometasone furoate was reported to be 98% to 99% in concentration range of 5 to 500 ng/mL.
Metabolism: There are no major metabolites detectable in plasma. One of the minor metabolites formed is 6β-hydroxy-mometasone furoate. In human liver microsomes, the formation of the metabolite is regulated by cytochrome P-450 3A4 (CYP3A4).
Elimination: Following intravenous administration, the effective plasma elimination half-life of mometasone furoate is 5.8 hours. Any absorbed drug is excreted as metabolites mostly via the bile, to extent into feces (74%) and to a limited extent, into the urine (8%).
Indications/Uses
T.O.-MOMETASONE (mometasone furoate aqueous nasal spray) is indicated for: Treat the symptoms of seasonal or perennial rhinitis; For treatment of nasal congestion associated with seasonal allergic rhinitis; Adjunctive treatment of acute episodes of sinusitis; For the treatment of nasal polyposis; For treatment of symptoms associated with acute rhinosinusitis.
Dosage/Direction for Use
Recommended Dose: Dosing Considerations: The therapeutic effects of corticosteroids may not be immediate and not to exceed the recommended dosage. Benefit requires regular use and usually occurs within a few days. One to two weeks may pass before full effect is achieved.
Instruct patients to clear nasal passages before use. In the presence of excessive nasal mucous secretion or edema of the nasal mucosa, the drug may fail to reach the site of action. In such cases, it is advisable to use a nasal vasoconstrictor for 2 to 3 days prior to starting treatment with mometasone furoate aqueous nasal spray.
Recommended Dose and Dosage Adjustment: Seasonal or Perennial Rhinitis: T.O.-MOMETASONE 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 T.O.-MOMETASONE is recommended two to four weeks prior to the anticipated start of the pollen season.
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: T.O.-MOMETASONE is indicated for the relief of nasal congestion associated with seasonal allergic rhinitis, in adults and pediatric patients 2 years of age and older.
Adult 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 micrograms of mometasone furoate in each spray) in each nostril once daily (total daily dose of 200 micrograms).
Children 2 to 11 years of age: The recommended dose for treatment of nasal congestion associated with seasonal allergic rhinitis is one spray (50 micrograms of mometasone furoate in each spray) in each nostril once daily (total daily dose of 100 micrograms).
Adjunctive Treatment of Acute Episodes of Sinusitis: T.O.-MOMETASONE 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.
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: T.O.-MOMETASONE is also indicated for the treatment of nasal polyps and associated symptoms including congestion and loss of smell in adult patients 18 years of age and older.
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: T.O.-MOMETASONE is also indicated for the treatment of symptoms associated with acute rhinosinusitis in patients 12 years of age and older without signs of symptoms of bacterial infection.
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 T.O.-MOMETASONE (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.
Instruction for using T.O.-MOMETASONE: SHAKE CONTAINER WELL BEFORE EACH USE.
Patients should be instructed on the correct method of use, which is to blow the nose, then insert the nozzle carefully into the nostril, compress the opposite nostril and actuate the spray while inspiring through the nose, with the mouth closed.
1) Remove the plastic dust cap.
2) The very first time the spray is used; prime the pump by pressing downward on the shoulders of the white applicator, using the forefinger and middle finger while supporting the base of the bottle with a thumb. Press down and release the pump ten (10) times or until a fine spray appears. The pump is now ready to use. The pump may be stored unused for up to 2 weeks without repriming. If unused for more than 2 weeks, prime the pump again two (2) times, until a fine spray appears.
3) Gently blow nose to clear the nostrils. Close one nostril using a finger. Tilt head forward slightly and, keeping the bottle upright, carefully insert the nasal applicator into the other nostril.
4) For each spray, press firmly downward once on the shoulder of the white applicator, using the forefinger and middle finger while supporting the base of the bottle with the thumb. Spray while breathing gently inward through the nostril, with the mouth closed.
5) Then breathe out through the mouth.
6) Repeat in the other nostril.
7) Replace the plastic dust cap after each use.
The correct amount of medication in each spray can only be assured up to 140 sprays from the bottle even though the bottle may not be completely empty. Patient should keep track of the number of sprays used from each bottle of T.O.-MOMETASONE, and discard the bottle after using 140 sprays (approximately five weeks of supply, depending on the prescribed dose).
Instruction for cleaning T.O.-MOMETASONE: Cleaning: To clean the nasal applicator remove the plastic dust cap and pull gently upward on the white nasal applicator so that it comes free. Wipe the tip of the bottle with a clean tissue and replace the nasal applicator followed by the plastic dust cap. Do not try to unblock the nasal applicator by inserting a pin or other sharp object as this will damage the applicator and cause to not get the right dose of medicine. Re-prime the pump with 2 sprays when first used after cleaning.
Overdosage
Importance of not exceeding the recommended dose or dosing frequency. If the patient notices other side effects that are caused by this medicine, contact the physician.
Acute ingestion is rarely a clinical problem; effects rarely occur with administration of less than three weeks duration. Acute adrenal insufficiency rarely reported after overdose. Because the systemic bioavailability is <1% (using a sensitive assay with a lower quantitation limit of 0.25 pg/mL) after administration of mometasone furoate via mometasone furoate monohydrate aqueous nasal spray, overdose is unlikely to require any therapy other than observation.
Adrenal suppression or hypercorticism may occur, especially with higher than recommended doses for prolonged durations, postoperatively, or during periods of stress; dosage adjustment required (see WARNINGS).
Treatment: Significant toxicity is not expected after overdose; gastrointestinal decontamination is generally not necessary. Moderate to severely symptomatic patients and those with deliberate overdose should be sent to a healthcare facility for evaluation and treated until symptoms resolve. When adrenal insufficiency occurs, the systemic corticosteroids should be adjusted to the adequate maintenance therapy of a systemic corticosteroid (see PRECAUTIONS).
Contraindications
Patients who are hypersensitive to this drug or to any ingredient in the formulation or component of the container (see DESCRIPTION).
T.O.-MOMETASONE 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.
Warnings
Do not use in patients with gastric or duodenal ulcer disease, diabetes, tuberculosis, viral infections.
Special warnings: General: During transfer from systemic corticosteroid to mometasone furoate 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 mometasone furoate aqueous nasal spray therapy. Such transfer may also unmask pre-existing allergic conditions such as rhinitis, conjunctivitis, eczema, arthritis, eosinophilic conditions, previously suppressed by systemic corticosteroid therapy. This is particularly important in patients who have asthma or other conditions where too rapid a decrease in systemic corticosteroids may cause a severe exacerbation of their symptoms.
Hypercorticism: Manifestation of hypercorticism, including very rare case of menstrual irregularities, acneiform lesions, and cushingoid feature, may occur in patients who are particularly sensitive or predisposed to corticosteroid effect because of recent systemic corticosteroid therapy or when recommended dosages of intranasal corticosteroids, including mometasone furoate, are exceeded.
Infections: Patients who become immunosuppressed while receiving corticosteroids have increased susceptibility to infections compared with individuals, and certain infections (e.g., varicella [chickenpox], measles) can have a more serious or even fatal outcome in such patients.
Sensitivity reaction: Rarely, immediate hypersensitivity reactions may occur following intranasal administration of mometasone. Wheezing has reported very rarely.
Special Precautions
General: There is no evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression following prolonged (12 months) treatment with mometasone furoate monohydrate aqueous nasal spray. However, patients who are transferred from long-term administration of systemically active corticosteroids to mometasone furoate 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.
Nasopharyngeal effects: Mometasone furoate 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 mometasone furoate monohydrate 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 mometasone furoate 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 mometasone furoate aqueous nasal spray therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing mometasone furoate aqueous nasal spray.
Following the use of intranasal aerosolized corticosteroids, instances of nasal septum perforation have been reported very rarely.
Epistaxis observed more frequently in patients with allergic rhinitis treated with mometasone compared with those who received placebo in clinical studies.
Concomitant infections: Use caution or avoid use in patients with active or quiescent tuberculosis, untreated fungal, bacterial or systemic viral infections or ocular herpes simplex infections.
Ophthalmologic effects: Following the use of intranasal aerosolized corticosteroids, instances of increased intraocular pressure have been reported very rarely.
Use in Pregnancy & Lactation: There are no adequate or well-controlled studies in pregnant or nursing women.
As with other nasal corticosteroid preparations, mometasone furoate aqueous nasal spray should be used in pregnant women, nursing mothers 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.
Use in Children: Safety and effectiveness of the nasal spray have not been established for the treatment of nasal polyps in pediatric patients and adolescents less than 18 years of age have not been studied.
Safety and effectiveness of the nasal spray have not been established for the treatment of seasonal allergic and perennial allergic rhinitis in pediatric patients under 2 years of age.
Safety and effectiveness of the nasal spray have not been established for the prophylaxis of nasal symptoms of seasonal allergic rhinitis in pediatric patients under 12 years of age.
Use In Pregnancy & Lactation
Pregnancy: Teratogenic Effects: Pregnancy Category C: When administered to pregnant mice, rats, and rabbits, mometasone furoate increased fetal malformations. The doses that produced malformations also decreased fetal growth, as measured by lower fetal weights and/or delayed ossification. Mometasone furoate also caused dystocia and related complications when administered to rats during the end of pregnancy. Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available.
Drugs should be given only if the potential benefit justifies the potential risk to the fetus. Infants born of mothers who received corticosteroids during pregnancy should be observed carefully for hypoadrenalism.
Lactation: Systemic corticosteroids are excreted in human milk. It is not known if sufficient quantities of mometasone furoate is absorbed following nasal route to produce detectable amounts in breast milk; however, oral absorption is limited (<1%). Caution is advised if the drug is administered to nursing women. As with other nasal corticosteroid preparations, mometasone furoate aqueous nasal spray should be used in pregnant women, nursing mothers or women of childbearing age only if the potential benefit justifies the potential risk to the mother, fetus, or infant.
Adverse Reactions
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.
If recommended doses of intranasal corticosteroids are exceeded or if individuals are particularly sensitive or predisposed by virtue of recent systemic corticosteroid therapy, symptoms of hypercorticism may occur, including, very rarely, menstrual irregularities, acneiform lesions, and cushingoid features [See Warnings].
Adverse effects occurring in 5% or more and more frequency than with placebo: Allergic Rhinitis: In patients treated for allergic rhinitis, the incidences of adverse effects occurring in 5% or more include headache, viral infection, pharyngitis, epistaxis/blood-tinged mucus, coughing, and upper respiratory tract infection; in addition, dysmenorrhea, musculoskeletal pain, and sinusitis (in patients 12 years of age or older) and vomiting (in patients 3-11 years of age).
Nasal Polyps: In patients treated for nasal polyps, the overall incidence of adverse effects occurring in 5% or more and more frequency than with placebo include epistaxis.
The frequency of 1% to < 5%: The following adverse effects in clinical trials in patients using mometasone furoate monohydrate aqueous nasal spray with an incidence of 1% to 5% and occurred at a frequency equal to or less than placebo: Cardiovascular effects: chest pain (2% to 5%).
Gastrointestinal effects: diarrhea (2% to 5%) in adults and adolescents (12 years of age and older) with seasonal and perennial allergic rhinitis, including pediatric patients (ages 3 to 11 years) with allergic rhinitis, indigestion (2% to 5%), nausea (2% to 5%).
Musculoskeletal and connective tissue disorders: arthralgia (2% to 5%), myalgia (2% to 5%).
Neurologic effects: sinus headache (1.2%).
Ophthalmic effects: conjunctivitis (2% to 5%).
Otic effects: otalgia (2% to 5%), otitis media (2% to 5%) in pediatric patients (3 to 11 years of age) with allergic rhinitis.
Respiratory effects: asthma (2% to 5%), bronchitis (2% to 5%), nasal irritation (2% to 5%) in pediatric patients (3 to 11 years of age) with allergic rhinitis, wheezing (2% to 5%).
Other effects: influenza like symptoms (2% to 5%).
Post-Market Adverse Drug Reactions: The following adverse reactions have been identified during the post-marketing period for mometasone furoate monohydrate aqueous nasal spray: anaphylaxis and angioedema, nasal burning and irritation, disturbances in smell and nasal septal perforation. Asthma exacerbation, which may include cough, dyspnea, wheezing, and bronchospasm has been reported. 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.
Drug Interactions
Drug-Drug Interactions: 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, atazanavir, clarithromycin, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin, a potent CYP 3A4 inhibitor, may increase the plasma concentrations of mometasone furoate.
Storage
T.O.-MOMETASONE should be stored below 30°C. Do not freeze.
ATC Classification
R01AD09 - mometasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.
Presentation/Packing
Aqueous nasal spray (bottle) 50 mcg/actuation x 140 metered doses.
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