Mometasone furoate

Description

Mometasone Furoate Cream USP, 0.1% is formulated for topical application and contains mometasone furoate, a synthetic corticosteroid recognized for its anti-inflammatory properties. The chemical designation of mometasone furoate is 9α, 21-dichloro-11β,17-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione 17-(2-furoate), with an empirical formula of C27H30Cl2O6 and a molecular weight of 521.4.

Mometasone furoate appears as a white to off-white powder that is practically insoluble in water, slightly soluble in octanol, and moderately soluble in ethyl alcohol. Each gram of Mometasone Furoate Cream USP, 0.1% contains 1 mg of mometasone furoate, incorporated into a cream base consisting of aluminum starch octenylsuccinate, ceteareth-20, phosphoric acid, propylene glycol, propylene glycol stearate, purified water, stearyl alcohol, titanium dioxide, white petrolatum, and white wax.

Uses and Indications

Mometasone Furoate Cream USP, 0.1% is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses in patients aged 2 years and older.

There are no teratogenic or nonteratogenic effects associated with the use of this medication.

Dosage and Administration

Healthcare professionals are advised to apply a thin film of the medication to the affected skin areas once daily. Treatment should be discontinued once adequate control of the condition is achieved. In cases where no improvement is observed within 2 weeks of initiation, a reassessment of the diagnosis is recommended.

It is important to note that the use of occlusive dressings with this medication should be avoided unless specifically directed by a physician.

Contraindications

Mometasone furoate cream is contraindicated in patients with a history of hypersensitivity to any of the components in the formulation. Use in these individuals may lead to severe allergic reactions.

Warnings and Precautions

Reversible hypothalamic-pituitary-adrenal (HPA) axis suppression may occur with the use of this medication, particularly following withdrawal of treatment. This condition can lead to glucocorticosteroid insufficiency, Cushing's syndrome, and hyperglycemia due to systemic absorption. It is essential for healthcare professionals to periodically evaluate patients who are applying a topical steroid over large surface areas or under occlusive dressings for signs of HPA axis suppression. Should evidence of suppression be observed, it is recommended to modify the treatment regimen accordingly.

Pediatric patients are particularly vulnerable to systemic toxicity associated with this medication. Therefore, careful monitoring and consideration of the risk-benefit ratio are advised when prescribing to this population.

Additionally, the use of this medication may elevate the risk of developing cataracts and glaucoma. Healthcare providers should remain vigilant for any visual symptoms in patients and consider referral to an ophthalmologist for further evaluation if such symptoms arise. Regular eye examinations may be warranted to monitor for these potential complications.

Side Effects

Patients using mometasone furoate cream may experience a range of adverse reactions. Common adverse reactions include burning, pruritus, and skin atrophy.

Serious adverse reactions may arise from systemic absorption of the medication, particularly in patients applying the cream to large surface areas or under occlusion. These reactions include reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, which can lead to glucocorticosteroid insufficiency upon withdrawal of treatment, Cushing's syndrome, and hyperglycemia. It is recommended that patients be periodically evaluated for evidence of HPA axis suppression, and modifications to treatment should be made if such suppression is detected.

Pediatric patients may be at an increased risk for systemic toxicity. Clinical data indicate that mometasone furoate cream caused HPA axis suppression in approximately 16% of pediatric subjects aged 6 to 23 months, who initially exhibited normal adrenal function prior to treatment. These subjects were treated for an average of three weeks over a mean body surface area of 41%. Follow-up testing revealed that one subject continued to show signs of HPA axis suppression. Additional concerns in pediatric patients include the potential for Cushing's syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension. Symptoms of adrenal suppression may manifest as low plasma cortisol levels and a lack of response to ACTH stimulation, while signs of intracranial hypertension may include bulging fontanelles, headaches, and bilateral papilledema.

Furthermore, the use of mometasone furoate cream may increase the risk of cataracts and glaucoma. If patients experience visual symptoms, a referral to an ophthalmologist should be considered.

Mometasone furoate cream is contraindicated in patients with a history of hypersensitivity to any of its components.

Drug Interactions

No drug-drug interaction studies have been conducted with mometasone furoate cream. Therefore, the potential for pharmacodynamic or pharmacokinetic interactions with other medications remains undefined. Clinicians are advised to exercise caution when prescribing mometasone furoate cream in conjunction with other therapies, and to monitor patients for any unexpected clinical effects.

Packaging & NDC

The table below lists all NDC Code configurations of Mometasone Furoate, the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.

Pediatric Use

Mometasone furoate cream may be used with caution in pediatric patients aged 2 years and older; however, the safety and efficacy of its use for longer than 3 weeks have not been established. The use of mometasone furoate cream is not recommended in pediatric patients under 2 years of age due to insufficient safety and efficacy data.

In a clinical trial involving 24 subjects with atopic dermatitis, including 19 patients aged 2 to 12 years, the majority achieved clearance within 3 weeks of once-daily treatment with mometasone furoate cream. However, caution is warranted as approximately 16% of pediatric subjects aged 6 to 23 months experienced HPA axis suppression after treatment for about 3 weeks, with a mean body surface area treated of 41% (range 15% to 94%).

Pediatric patients are at an increased risk of HPA axis suppression and Cushing's syndrome due to their higher ratio of skin surface area to body mass compared to adults. They are also more susceptible to adrenal insufficiency during and/or after withdrawal of treatment, as well as to skin atrophy, including striae, when treated with topical corticosteroids. Those applying topical corticosteroids to more than 20% of body surface area are at an elevated risk of HPA axis suppression.

Adverse effects associated with topical corticosteroid use in pediatric patients may include HPA axis suppression, Cushing's syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension. Manifestations of adrenal suppression can present as low plasma cortisol levels and an absence of response to ACTH stimulation, while signs of intracranial hypertension may include bulging fontanelles, headaches, and bilateral papilledema. Mometasone furoate cream is contraindicated for the treatment of diaper dermatitis.

Geriatric Use

Clinical studies of mometasone furoate cream included 190 subjects aged 65 years and older, with 39 subjects aged 75 years and older. The data from these studies indicate that there are no overall differences in safety or effectiveness between elderly patients and younger patients. Additionally, other reported clinical experiences have not identified significant differences in responses between geriatric patients and their younger counterparts.

It is important to note, however, that greater sensitivity to the effects of the medication in some older individuals cannot be ruled out. Therefore, healthcare providers should exercise caution when prescribing mometasone furoate cream to elderly patients, considering the potential for increased sensitivity. Monitoring for adverse effects and therapeutic efficacy is recommended in this population to ensure optimal treatment outcomes.

Pregnancy

There are no adequate and well-controlled studies in pregnant women regarding the use of mometasone furoate cream. Therefore, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Corticosteroids, including mometasone furoate, have been shown to be teratogenic in laboratory animals when administered systemically at relatively low dosage levels. Additionally, some corticosteroids have demonstrated teratogenic effects following dermal application in animal studies.

In studies involving pregnant rats, rabbits, and mice, mometasone furoate was associated with increased fetal malformations. The doses that produced these malformations also resulted in decreased fetal growth, as evidenced by lower fetal weights and/or delayed ossification. Furthermore, administration of mometasone furoate to rats during the end of pregnancy led to dystocia and related complications.

Specific findings from animal studies include the occurrence of cleft palate in mice at subcutaneous doses of 60 mcg/kg and above, with reduced fetal survival noted at 180 mcg/kg. No toxicity was observed at a dose of 20 mcg/kg. In rats, topical application of mometasone furoate at doses of 600 mcg/kg and above resulted in umbilical hernias, while a dose of 300 mcg/kg caused delays in ossification without malformations. In rabbits, multiple malformations, such as flexed front paws, gallbladder agenesis, umbilical hernia, and hydrocephaly, were observed at topical doses of 150 mcg/kg and above. An oral study indicated that at 700 mcg/kg, mometasone furoate increased resorptions and caused cleft palate and/or head malformations, with most litters being aborted or resorbed at 2800 mcg/kg. No toxicity was noted at 140 mcg/kg.

When administered subcutaneously to rats throughout pregnancy or during the later stages, a dose of 15 mcg/kg resulted in prolonged and difficult labor, as well as reduced numbers of live births, birth weight, and early pup survival. Similar adverse effects were not observed at a lower dose of 7.5 mcg/kg. Given these findings, healthcare professionals should carefully consider the risks and benefits of using mometasone furoate in pregnant patients.

Lactation

Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects in breastfed infants. The potential effects of topical administration of corticosteroids on breast milk are not well understood, as it is not known whether such administration could result in sufficient systemic absorption to produce detectable quantities in human milk. Given that many drugs are excreted in human milk, caution should be exercised when administering mometasone furoate cream to lactating mothers.

Renal Impairment

There is no specific information available regarding dosage adjustments, special monitoring, or safety considerations for patients with renal impairment. Healthcare professionals should exercise caution when prescribing to patients with reduced kidney function, as the absence of detailed guidance necessitates careful clinical judgment. Regular monitoring of renal function may be advisable in this patient population.

Hepatic Impairment

Patients with hepatic impairment have not been specifically studied in relation to the use of this medication. Consequently, there are no established dosage adjustments, special monitoring requirements, or precautions outlined for individuals with compromised liver function. It is recommended that healthcare providers exercise caution when prescribing this medication to patients with hepatic impairment, given the lack of data on its safety and efficacy in this population. Regular monitoring of liver function may be prudent in these cases, although specific parameters are not defined in the available information.

Overdosage

Topically applied mometasone furoate cream has the potential to be absorbed in sufficient quantities to elicit systemic effects. In the event of an overdosage, healthcare professionals should be vigilant for signs and symptoms that may arise due to excessive exposure.

Recommended Actions

In cases of suspected overdosage, it is imperative to assess the patient for any systemic effects that may manifest. Immediate medical evaluation is advised, and supportive care should be initiated as necessary.

Potential Symptoms

Symptoms of overdosage may include, but are not limited to, signs of adrenal suppression, such as fatigue, weakness, and hypotension. Additionally, patients may exhibit signs of Cushing's syndrome, which can include weight gain, hypertension, and glucose intolerance.

Management Procedures

Management of overdosage should focus on symptomatic treatment and supportive care. Monitoring of vital signs and laboratory parameters may be warranted to evaluate the extent of systemic involvement. If significant symptoms are present, referral to a specialist in toxicology or endocrinology may be appropriate for further management.

Healthcare professionals are encouraged to report any cases of overdosage to the appropriate regulatory authorities to contribute to the ongoing assessment of the safety profile of mometasone furoate cream.

Nonclinical Toxicology

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 also demonstrated teratogenic effects following dermal application in laboratory animals.

In studies involving pregnant rats, rabbits, and mice, mometasone furoate was associated with an increase in fetal malformations. The doses that produced these malformations also resulted in decreased fetal growth, as indicated by lower fetal weights and/or delayed ossification. Additionally, administration of mometasone furoate to rats during the later stages of pregnancy led to dystocia and related complications. In mice, subcutaneous doses of 60 mcg/kg and above resulted in cleft palate, with reduced fetal survival observed at 180 mcg/kg; no toxicity was noted at 20 mcg/kg. In rats, topical doses of 600 mcg/kg and above produced umbilical hernias, while a dose of 300 mcg/kg caused delays in ossification without malformations. In rabbits, multiple malformations, including flexed front paws, gallbladder agenesis, umbilical hernia, and hydrocephaly, were observed at topical doses of 150 mcg/kg and above. An oral study indicated that at 700 mcg/kg, mometasone furoate increased resorptions and caused cleft palate and/or head malformations, with most litters aborted or resorbed at 2800 mcg/kg; no toxicity was observed at 140 mcg/kg. Furthermore, subcutaneous doses of 15 mcg/kg administered throughout pregnancy or during the later stages resulted in prolonged and difficult labor, as well as reduced numbers of live births, birth weight, and early pup survival; similar effects were not observed at 7.5 mcg/kg.

Long-term animal studies have not been performed to evaluate the carcinogenic potential of mometasone furoate cream. However, long-term carcinogenicity studies conducted via inhalation in rats and mice showed no statistically significant increase in tumor incidence. In a 2-year study in Sprague Dawley rats, inhalation doses up to 67 mcg/kg did not result in a significant increase in tumors. Similarly, a 19-month study in Swiss CD-1 mice demonstrated no statistically significant increase in tumor incidence at inhalation doses up to 160 mcg/kg.

Mometasone furoate increased chromosomal aberrations in an in vitro Chinese hamster ovary cell assay but did not do so in an in vitro Chinese hamster lung cell assay. It was not mutagenic in the Ames test or mouse lymphoma assay and did not exhibit clastogenic effects in an in vivo mouse micronucleus assay, a rat bone marrow chromosomal aberration assay, or a mouse male germ-cell chromosomal aberration assay. Additionally, mometasone furoate did not induce unscheduled DNA synthesis in vivo in rat hepatocytes.

In reproductive studies involving rats, no impairment of fertility was observed in male or female rats at subcutaneous doses up to 15 mcg/kg.

Postmarketing Experience

Mometasone furoate cream has been associated with various postmarketing experiences reported voluntarily or through surveillance programs.

Excessive absorption of mometasone furoate cream through the skin may lead to adrenal gland suppression. Healthcare providers may conduct blood tests to monitor for potential adrenal gland dysfunction in patients using this medication.

Vision-related issues have been reported, with topical corticosteroids potentially increasing the risk of developing conditions such as cataracts and glaucoma. Patients are advised to inform their healthcare provider if they experience blurred vision or other visual disturbances during treatment.

Skin-related adverse events have also been noted, including allergic reactions such as contact dermatitis and localized skin infections at the site of application. Patients should discontinue use and consult their healthcare provider if they experience symptoms such as pain, tenderness, swelling, or delayed healing.

The most frequently reported side effects of mometasone furoate cream include burning, itching, and skin atrophy.

Patients are encouraged to report any side effects to the FDA at 1-800-FDA-1088.

Patient Counseling

Patients should be advised to read the FDA-approved patient labeling (Patient Information) prior to using mometasone furoate cream. It is essential that the cream is used strictly as directed by the physician and is intended for external use only. Patients must be cautioned to avoid contact with the eyes and to report any visual symptoms to their healthcare providers promptly.

Healthcare providers should instruct patients not to apply mometasone furoate cream on the face, underarms, or groin areas unless specifically directed by the physician. Additionally, patients should be informed that the cream should not be used for any condition other than the one for which it was prescribed.

Patients must be advised against bandaging or covering the treated skin area in a manner that creates an occlusive environment, unless directed by the physician. They should also report any signs of local adverse reactions to their physician.

It is important to inform patients that mometasone furoate cream should not be used in the treatment of diaper dermatitis, and they should avoid applying the cream in the diaper area, as diapers or plastic pants may act as an occlusive dressing.

Patients should discontinue therapy once control of the condition is achieved. If no improvement is observed within two weeks, they should contact their physician for further evaluation. Lastly, patients must be cautioned not to use other corticosteroid-containing products in conjunction with mometasone furoate cream without first consulting their physician.

Storage and Handling

The product is supplied in accordance with the National Drug Code (NDC) specifications. It should be stored at a temperature range of 20° to 25°C (68° to 77°F), adhering to the guidelines set forth by the United States Pharmacopeia (USP) for Controlled Room Temperature. It is essential to avoid exposure to excessive heat to maintain the integrity of the product. Proper storage conditions are critical to ensure the efficacy and safety of the product throughout its shelf life.

Additional Clinical Information

Patients may require periodic evaluation for hypothalamic-pituitary-adrenal (HPA) axis suppression, which can be assessed using the adrenocorticotropic hormone (ACTH) stimulation test. Clinicians should advise patients to report any visual symptoms and consider referral to an ophthalmologist for further evaluation. It is important to instruct patients to avoid contact of mometasone furoate cream with the eyes.

In the postmarketing experience, there have been reports of cataracts and glaucoma associated with the use of topical corticosteroids, including topical mometasone products.

FDA Insert (PDF)

This document is the official FDA-approved prescribing information for Mometasone Furoate as submitted by Padagis Israel Pharmaceuticals Ltd. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)