TOPOCORT

Mometasone furoate is a corticosteroid drug that can be used for the treatment of asthma, rhinitis, and certain skin conditions Label 14, 15.

It has a glucocorticoid receptor binding affinity 22 times stronger than dexamethasone and higher than many other corticosteroids as well 2.

Mometasone furoate is formulated as a dry powder inhaler, nasal spray, and ointment for its different indications Label 14, 15.

Inhaled mometasone furoate is indicated for prophylaxis of asthma in patients ≥4 years.

Applied topically as an ointment, mometasone furoate is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years.

Mometasone furoate nasal spray is available both over-the-counter (OTC) and by prescription.

OTC nasal spray formulation of mometasone furoate is indicated for the treatment of upper respiratory allergic symptoms (e.g. rhinorrhea, sneezing) in patients ≥2 years of age.

The prescription formulation is indicated for the treatment of chronic rhinosinusitis with nasal polyps in patients ≥18 year old and for the and prophylaxis of seasonal allergic rhinitis in patients ≥12 years old.

It is also approved in combination with olopatadine for the symptomatic treatment of seasonal allergic rhinitis in patients ≥12 years.

Mometasone is a synthetic corticosteroid with an affinity for glucocorticoid receptors 22 times higher than that of dexamethasone 2.

Mometasone furoate also has a lower affinity to mineralocorticoid receptors than natural corticosteroids, making it more selective in its action 2.

Mometasone furoate diffuses across cell membranes to activate pathways responsible for reducing inflammation Label 1, 2, 3, 14, 15.

The mean time to peak concentration is 1.0-2.5 hours Label.

Bioavailability has been reported as <1% Label but studies of repeat doses of inhaled corticosteroids suggest a bioavailability of 11% 3.

The 0.1% ointment may have a bioavailability of 0.7% 15.

Steady state volume of distribution of 152 L Label.

of mometasone furoate is largely performed hepatically by cytochrome P450 3A4 producing a number of metabolites Label 14, 1, 3.

Some of these metabolites include free mometasone and 6-beta-hydroxy-mometasone furoate 1, 3, 4.

Hover over products below to view reaction partners Mometasone furoate 6-beta-hydroxy-mometasone furoate Mometasone 21-chloro-17-alpha-hydroxy-16-alpha-methyl-9-beta,11beta-oxidopregna-1,4-diene-3,20-dione 17-(2-furoate) 21-beta-chloro-21-alpha-hydroxy-16-alpha-methyl-9-beta,11-beta-oxidopregna-1,4,17,20-tetraen-3-one 21-(2-furoate 21-chloro-17-alpha-hydroxy-16-alpha-methyl-9-beta,11-beta-oxidopregna-1,4-diene-3,20-dione 9-alpha,21-beta-dichloro-11-beta,21-alpha-dihydroxy-16-alpha-methylpregna-1,4,17,20-tetraen-3-one 21-(2-furoate) 21-beta-chloro-21-alpha-hydroxy-16-alpha-methyl-9-beta,11-beta-oxidopregna-1,4,17,20-tetraen-3-one 21-(2-furoate.

For an inhaled dose, approximately 74% is excreted in the feces and 8% is excreted in the urine Label 14.

The terminal half life of an inhaled dose is approximately 5 hours Label though it has been reported as 5.8 hours by other sources 14, 2.

The clearance rate of mometasone furoate is not readily available 1, though it may be close to 90 L/h 2.

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Overdose with a mometasone furoate inhaler may occur with chronic overuse Label 14.

Symptoms of chronic overuse may present as hypercorticism and adrenal suppression, and patients may not require any more treatment than monitoring Label 14.

In animal studies of pregnancy, some fetal toxic effects were seen at or above the maximum recommended human dose, though rodents are more sensitive to these effects than humans Label 14, 15.

The benefits and risks of use should be considered in pregnant patients 14, 15 It is unknown if mometasone furoate is excreted in breast milk but other corticosteroids are and therefore caution should be exercised when administering to nursing mothers Label 14, 15.

Safety and effectiveness in pediatric populations has been established through clinical trials, though there may be a reduction in expected growth of about 1cm per year depending on the dose and duration of treatment Label.

Pediatric patients should be titrated to the lowest effective dose for mometasone furoate inhalers Label.

A trial of geriatric patients showed no difference in safety or efficacy compared to younger patients, however patients of an even greater age may still be more sensitive to mometasone furoate Label 14, 15.

The use of a mometasone furoate inhaler in moderate or severe hepatic impairment rarely leads to detectable plasma concentrations though caution may be prudent with increasing degrees of severity Label 14.

The effects of mometasone furoate in renal impairment, and across gender and race have not been studied Label 14.

Mometasone furoate cream, 0.1% is contraindicated in those patients with a history of hypersensitivity to any of the components in the preparation.

Apply a thin film of mometasone furoate cream, 0.1% to the affected skin areas once daily.

Mometasone furoate cream, 0.1% may be used in pediatric patients 2 years of age or older.

Since safety and efficacy of mometasone furoate cream, 0.1% have not been established in pediatric patients below 2 years of age; use in this is not recommended.

Therapy should be discontinued when control is achieved.

If no improvement is seen within 2 weeks, reassessment of diagnosis may be necessary.

Do not use mometasone furoate cream, 0.1% with occlusive dressings unless directed by a physician.

Do not apply mometasone furoate cream, 0.1% in the diaper area if the patient still requires diapers or plastic pants, as these garments may constitute occlusive dressing.

Avoid contact with eyes.

Wash hands after each application.

Avoid use on the face, groin, or axillae.

Mometasone furoate cream, 0.1% is for topical use only.

It is not for oral, ophthalmic, or intravaginal use.

• Apply a thin film to the affected skin areas once daily.

• Discontinue therapy when control is achieved.

• If no improvement is seen within 2 weeks, reassess diagnosis.

• Do not use with occlusive dressings unless directed by a physician.

Mometasone furoate cream

USP, 0.1% is a white to off-white, uniform and smooth cream and is supplied in 15 g (NDC 68462-192-17) and 45 g (NDC 68462-192-55) tubes.

Store at 25°C (77°F); excursions permitted to 15° to 30°C (59 to86°F) .

Avoid excessive heat.

There are no adequate and well-controlled studies in pregnant women.

Therefore, mometasone furoate cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Corticosteroids have been shown to be teratogenic in laboratory animals when administered systemically at relatively low dosage levels.

Some corticosteroids have been shown to be teratogenic after dermal application in laboratory animals.

When administered to pregnant rats, rabbits, and mice, 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.

In mice, mometasone furoate caused cleft palate at subcutaneous doses of 60 mcg/kg and above.

Fetal survival was reduced at 180 mcg/kg. No toxicity was observed at 20 mcg/kg. (Doses of 20, 60, and 180 mcg/kg in the mouse are approximately 0.01, 0.02, and 0.05 times the estimated maximum clinical topical dose from mometasone furoate cream on a mcg/m 2 basis). In rats, mometasone furoate produced umbilical hernias at topical doses of 600 mcg/kg and above.

A dose of 300 mcg/kg produced delays in ossification, but no malformations. (Doses of and 600 mcg/kg in the rat are approximately 0.2 and 0.4 times the estimated maximum clinical topical dose from mometasone furoate cream on a mcg/m 2 basis). In rabbits, mometasone furoate caused multiple malformations (e.g., flexed front paws, gallbladder agenesis, umbilical hernia, hydrocephaly) at topical doses of 150 mcg/kg and above (approximately 0.2 times the estimated maximum clinical topical dose from mometasone furoate cream on a mcg/m 2 basis).

In an oral study, mometasone furoate increased resorptions and caused cleft palate and/or head malformations (hydrocephaly and domed head) at 700 mcg/kg. At 2800 mcg/kg most litters were aborted or resorbed.

No toxicity was observed at 140 mcg/kg. (Doses at 140, 700, and 2800 mcg/kg in the rabbit are approximately 0.2, 0.9, and 3.6 times the estimated maximum clinical topical dose from mometasone furoate cream on a mcg/m 2 basis). When rats received subcutaneous doses of mometasone furoate throughout pregnancy or during the later stages of pregnancy, 15 mcg/kg caused prolonged and difficult labor and reduced the number of live births, birth weight, and early pup survival.

Similar effects were not observed at 7.5 mcg/kg. (Doses of 7.5 and 15 mcg/kg in the rat are approximately 0.005 and 0.01 times the estimated maximum clinical topical dose from mometasone furoate cream on a mcg/m 2 basis).

Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects.

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk.

Because many drugs are excreted in human milk, caution should be exercised when mometasone furoate cream is administered to a nursing woman.

Mometasone furoate cream may be used with caution in pediatric patients 2 years of age or older, although the safety and efficacy of drug use for longer than 3 weeks have not been established.

Since safety and efficacy of mometasone furoate cream have not been established in pediatric patients below 2 years of age, its use in this is not recommended.

In a pediatric trial, 24 atopic dermatitis subjects, of whom 19 subjects were age to 12 years, were treated with mometasone furoate cream once daily.

The majority of subjects cleared within 3 weeks.

Mometasone furoate cream caused

HPA axis suppression in approximately 16% of pediatric subjects ages to 23 months, who showed normal adrenal function by Cortrosyn test before starting treatment, and were treated for approximately 3 weeks over a mean body surface area of 41% (range 15% to 94%).

The criteria for suppression were: basal cortisol level of ≤5 mcg/dL, 30-minute post-stimulation level of ≤18 mcg/dL, or an increase of <7 mcg/dL.

Follow-up testing to 4 weeks after trial completion, available for of the subjects, demonstrated suppressed HPA axis function in 1 subject, using these same criteria.

Long-term use of topical corticosteroids has not been studied in this population.

Because of a higher ratio of skin surface area to body mass, pediatric patients are at a greater risk than adults of HPA axis suppression and Cushing’s syndrome when they are treated with topical corticosteroids.

They are, therefore, also at greater risk of adrenal insufficiency during and/or after withdrawal of treatment.

Pediatric patients may be more susceptible than adults to skin atrophy, including striae, when they are treated with topical corticosteroids.

Pediatric patients applying topical corticosteroids to greater than 20% of body surface are at higher risk of HPA axis suppression.

HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension have been reported in pediatric patients receiving topical corticosteroids.

Manifestations of adrenal suppression in children include low plasma cortisol levels and an absence of response to ACTH stimulation.

Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema.

Mometasone furoate cream should not be used in the treatment of diaper dermatitis.

Clinical studies of mometasone furoate cream included 190 subjects who were 65 years of age and over and 39 subjects who were 75 years of age and over.

No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients.

However, greater sensitivity of some older individuals cannot be ruled out.