MOSASPRAY Mometasone Furoate 50mcg / actuation Nasal Spray 120actuations
RXDRUG-DRP-6145-120
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Indicated for use in adults and children 6 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 furoate nasal spray may be initiated up to four weeks prior to the anticipated start of the pollen season.
Indicated for the symptomatic treatment of nasal polyps in adults 18 years of age and older.
In patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis, prophylactic treatment with mometasone furoate nasal spray may be initiated up to four weeks prior to the anticipated start of the pollen season.
Indicated for the symptomatic treatment of nasal polyps in adults 18 years of age and older.
Dosage/Direction for Use
Seasonal allergic or perennial rhinitis: Adults (including older patients) and children 12 years of age and older:
The usual recommended dose is two actuations (50 μg/actuation) in each nostril once daily (total dose 200 μg).
Once symptoms are controlled, dose reduction to one actuation in each nostril (total dose 100 μ9) 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 μg). Dose reduction is recommended following control of symptoms.
Children between the ages of 3 and 11 years: The usual recommended dose is one actuation (50 μg/actuation) in each nostril once daily (total dose 100 μ9).
Mometasone furoate demonstrated a clinically significant onset of action within 12 hours alter 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.
Treatment with mometasone furoate may need to be initiated some days before the expected start of the pollen season in patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis.
Nasal polyposis: The usual recommended starting dose for polyposis is two actuations (50 μg/actuation) in each nostril once daily (total daily dose of 200 μg). If alter 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 μg). The dose should be titrated to the lowest dose at which effective control of symptoms is maintained. If no improvement in symptoms is seen alter 5 to 6 weeks of twice daily administration, the patient should be re-evaluated and treatment strategy reconsidered.
Efficacy and safety studies of mometasone furoate for the treatment of nasal polyposis were four months in duration.
Paediatric population: Seasonal allergic rhinitis and perennial rhinitis: The safety and efficacy of mometasone furoate in children under 3 years of age have not been established.
Nasal polyposis: The safety and efficacy of mometasone furoate in children and adolescents under 18 year, of age have not been established.
Method of Administration: Prior to administration of the first dose, shake container well and actuate the pump 10 times (until a uniform spray is obtained). If the pump is not used for 14 days or longer, reprime the pump with 2 actuations until a uniform spray is observed, before next use.
Shake container well before each use. The bottle should be discarded alter the labelled number of actuations or within 2 months of first use.
Preparing your nasal spray for use: Mometasone furoate 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 to be used for the first time, '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 linger on either side of the nozzle and the thumb underneath the bottle.
3. Point the nozzle away and then press down with fingers to pump the spray.
If not used for 14 days or more, "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, this medicine should provide enough doses for 30 days (120 sprays) and 35 days (140 sprays).
How to use the nasal spray: 1. Shake the bottle well and remove the dust cop.
2. Gently blow nose.
3. Close one nostril and put the nozzle into the other nostril.
4. Tilt head forward slightly, keeping the bottle upright.
5. Start ta breathe in gently or slowly through the nose and whilst breathing in squirl a spray of fine mist into the nose by pressing down ONCE with fingers.
6. Breathe out through the mouth. Repeat step 5 lo 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 cop.
Cleaning the nasal spray: It is important that the nasal spray is cleaned regularly, otherwise it may not work properly. Remove the dust cap and gently pull off the nozzle. Wash the nozzle and dust cap in worm water and then rinse under a running tap. Allow to dry in a warm place. Push the nozzle bock onto the bottle and replace the dust cap. The spray will need to be re-primed with 2 sprays when first used after cleaning.
The usual recommended dose is two actuations (50 μg/actuation) in each nostril once daily (total dose 200 μg).
Once symptoms are controlled, dose reduction to one actuation in each nostril (total dose 100 μ9) 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 μg). Dose reduction is recommended following control of symptoms.
Children between the ages of 3 and 11 years: The usual recommended dose is one actuation (50 μg/actuation) in each nostril once daily (total dose 100 μ9).
Mometasone furoate demonstrated a clinically significant onset of action within 12 hours alter 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.
Treatment with mometasone furoate may need to be initiated some days before the expected start of the pollen season in patients who have a history of moderate to severe symptoms of seasonal allergic rhinitis.
Nasal polyposis: The usual recommended starting dose for polyposis is two actuations (50 μg/actuation) in each nostril once daily (total daily dose of 200 μg). If alter 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 μg). The dose should be titrated to the lowest dose at which effective control of symptoms is maintained. If no improvement in symptoms is seen alter 5 to 6 weeks of twice daily administration, the patient should be re-evaluated and treatment strategy reconsidered.
Efficacy and safety studies of mometasone furoate for the treatment of nasal polyposis were four months in duration.
Paediatric population: Seasonal allergic rhinitis and perennial rhinitis: The safety and efficacy of mometasone furoate in children under 3 years of age have not been established.
Nasal polyposis: The safety and efficacy of mometasone furoate in children and adolescents under 18 year, of age have not been established.
Method of Administration: Prior to administration of the first dose, shake container well and actuate the pump 10 times (until a uniform spray is obtained). If the pump is not used for 14 days or longer, reprime the pump with 2 actuations until a uniform spray is observed, before next use.
Shake container well before each use. The bottle should be discarded alter the labelled number of actuations or within 2 months of first use.
Preparing your nasal spray for use: Mometasone furoate 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 to be used for the first time, '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 linger on either side of the nozzle and the thumb underneath the bottle.
3. Point the nozzle away and then press down with fingers to pump the spray.
If not used for 14 days or more, "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, this medicine should provide enough doses for 30 days (120 sprays) and 35 days (140 sprays).
How to use the nasal spray: 1. Shake the bottle well and remove the dust cop.
2. Gently blow nose.
3. Close one nostril and put the nozzle into the other nostril.
4. Tilt head forward slightly, keeping the bottle upright.
5. Start ta breathe in gently or slowly through the nose and whilst breathing in squirl a spray of fine mist into the nose by pressing down ONCE with fingers.
6. Breathe out through the mouth. Repeat step 5 lo 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 cop.
Cleaning the nasal spray: It is important that the nasal spray is cleaned regularly, otherwise it may not work properly. Remove the dust cap and gently pull off the nozzle. Wash the nozzle and dust cap in worm water and then rinse under a running tap. Allow to dry in a warm place. Push the nozzle bock onto the bottle and replace the dust cap. The spray will need to be re-primed with 2 sprays when first used after cleaning.
Overdosage
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 furoate is <1%, overdose is unlikely to require any therapy other than observation, followed by initiation of the appropriate prescribed dose.
Management: Because the systemic bioavailability of mometasone furoate is <1%, overdose is unlikely to require any therapy other than observation, followed by initiation of the appropriate prescribed dose.
Contraindications
Hypersensitivity to the active substance, mometasone furoate, or to any of the excipients.
Mometasone furoate should not be used in the presence of untreated localized 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.
Mometasone furoate should not be used in the presence of untreated localized 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.
Special Precautions
Immunosuppression: Mometasone furoate 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 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 therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing mometasone furoate.
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 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 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.
Non-nasal symptoms: 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.
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: Effect on growth in paediatric population: 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.
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 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 therapy or appropriate treatment may be required. Persistence of nasopharyngeal irritation may be an indication for discontinuing mometasone furoate.
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 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 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.
Non-nasal symptoms: 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.
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: Effect on growth in paediatric population: 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.
Use In Pregnancy & Lactation
Pregnancy: There are no or limited amount of data from the use of mometasone furoate in pregnant women.
Studies in animals have shown reproductive toxicity (see Preclinical safety data). 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.
Lactation: 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 furoate 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).
Studies in animals have shown reproductive toxicity (see Preclinical safety data). 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.
Lactation: 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 furoate 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).
Adverse Reactions
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 also Precautions), central serious 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 irritation1; 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.
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 also Precautions), central serious 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 irritation1; 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.
Drug Interactions
(See Precautions for 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.
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.
Caution For Usage
Incompatibilities: Not applicable.
Storage
Store at temperatures not exceeding 30° C.
Do not freeze. Discard unused suspension 2 months after first opening.
Do not freeze. Discard unused suspension 2 months after first opening.
Action
Pharmacotherapeutic Group: Nasal preparations, decongestants and other nasal preparations for topical use. ATC Code: R01D09.
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 leucocytes of allergic patients. In cell culture, mometasone furoate demonstrated high potency in inhibition of synthesis and release of lL-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 has shown antiinflammatory 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 demonstrated a clinically significant onset of action within 12 hours alter 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 l00 μg daily for one year, no reduction in growth velocity was observed.
There are limited data available on the safety and efficacy of mometasone furoate in the paediatric population aged 3 ta 5 years, and an appropriate dose 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 in all subsets of the paediatric population in seasonal and perennial allergic rhinitis (see Dosage & Administration for information on paediatric use).
Pharmacokinetics: Absorption: Mometasone furoate, administered as an aqueous nasal spray, has a systemic bioavailability of <l % 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 same 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 l 5 μg/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 μg/L was investigated in 2.4-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.
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 leucocytes of allergic patients. In cell culture, mometasone furoate demonstrated high potency in inhibition of synthesis and release of lL-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 has shown antiinflammatory 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 demonstrated a clinically significant onset of action within 12 hours alter 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 l00 μg daily for one year, no reduction in growth velocity was observed.
There are limited data available on the safety and efficacy of mometasone furoate in the paediatric population aged 3 ta 5 years, and an appropriate dose 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 in all subsets of the paediatric population in seasonal and perennial allergic rhinitis (see Dosage & Administration for information on paediatric use).
Pharmacokinetics: Absorption: Mometasone furoate, administered as an aqueous nasal spray, has a systemic bioavailability of <l % 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 same 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 l 5 μg/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 μg/L was investigated in 2.4-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.
MedsGo Class
Nasal Decongestants & Other Nasal Preparations
Features
Brand
Mosaspray
Full Details
Dosage Strength
50mcg / actuation
Drug Ingredients
- Mometasone
Drug Packaging
Nasal Spray 120act.
Generic Name
Mometasone Furoate
Dosage Form
Nasal Spray
Registration Number
DRP-6145
Drug Classification
Prescription Drug (RX)
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