Mometasone furoate

Description

Mometasone Furoate Ointment USP, 0.1% contains mometasone furoate for topical use. Mometasone furoate is a synthetic corticosteroid with anti-inflammatory activity. Chemically, it is identified as 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 g/mol. The compound appears as a white to off-white powder and is practically insoluble in water, slightly soluble in octanol, and moderately soluble in ethyl alcohol. Each gram of Mometasone Furoate Ointment USP, 0.1% contains 1 mg of mometasone furoate in a white to off-white uniform ointment base composed of hexylene glycol, phosphoric acid, propylene glycol stearate (55% monoester), purified water, white wax, and white petrolatum.

Uses and Indications

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

Limitations of Use: The safety and efficacy of Mometasone Furoate Ointment in pediatric patients under 2 years of age have not been established. There are no reported 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 Ointment, 0.1% is contraindicated in patients with a history of hypersensitivity to any of the components in the formulation. Use in these patients may lead to severe allergic reactions.

Warnings and Precautions

Reversible suppression of the hypothalamic-pituitary-adrenal (HPA) axis may occur with the use of this medication, particularly following withdrawal of treatment. This suppression 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 any evidence of suppression be identified, 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 risks versus benefits are advised when prescribing to this population.

Additionally, there is an increased risk of developing cataracts and glaucoma with the use of this medication. 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 Ointment, 0.1% may experience a range of adverse reactions. Common adverse reactions reported include burning, pruritus, skin atrophy, tingling or stinging sensations, and furunculosis.

Serious adverse reactions may include reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, which can lead to glucocorticosteroid insufficiency following the withdrawal of treatment. This condition, along with Cushing’s syndrome and hyperglycemia, may occur due to systemic absorption, particularly in patients applying the topical steroid over large surface areas or under occlusion. It is recommended that these patients be evaluated periodically for signs 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, including HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension. Manifestations of adrenal suppression in children can include low plasma cortisol levels and a lack of response to ACTH stimulation. Symptoms of intracranial hypertension may present as bulging fontanelles, headaches, and bilateral papilledema.

Additionally, the use of Mometasone Furoate Ointment may elevate the risk of cataracts and glaucoma. Patients experiencing visual symptoms should be referred to an ophthalmologist for further evaluation.

It is important to note that Mometasone Furoate Ointment is contraindicated in individuals with a history of hypersensitivity to any of its components.

Drug Interactions

There are currently no documented drug interactions associated with this medication. Additionally, there is no information available regarding interactions with laboratory tests. As such, no specific recommendations for dosage adjustments or monitoring are warranted at this time.

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 Ointment, 0.1% 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 this medication is not recommended in pediatric patients under 2 years of age due to insufficient safety and efficacy data.

In a study involving pediatric subjects aged 6 to 23 months, approximately 27% experienced hypothalamic-pituitary-adrenal (HPA) axis suppression after treatment for about 3 weeks, with a mean body surface area of 39% (range 15%-99%). The criteria for HPA axis suppression included a basal cortisol level of ≤5 mcg/dL, a 30-minute post-stimulation level of ≤18 mcg/dL, or an increase of <7 mcg/dL. Follow-up testing 2 to 4 weeks post-treatment in 8 subjects revealed that 3 continued to show suppressed HPA axis function.

Pediatric patients are at a higher risk of HPA axis suppression and Cushing’s syndrome due to their greater skin surface area relative to body mass. They may also experience glucocorticosteroid insufficiency during and/or after withdrawal of treatment. Additionally, children may be more susceptible to skin atrophy, including striae, when treated with topical corticosteroids. Those applying topical corticosteroids to more than 20% of their body surface area are at an increased risk of HPA axis suppression.

Adverse effects associated with topical corticosteroid use in children include HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension. Manifestations of adrenal suppression may present as low plasma cortisol levels and a lack of response to ACTH stimulation, while signs of intracranial hypertension can include bulging fontanelles, headaches, and bilateral papilledema. Mometasone Furoate Ointment, 0.1% should not be used for the treatment of diaper dermatitis.

Geriatric Use

Clinical trials of mometasone furoate ointment, 0.1%, included 310 subjects aged 65 years and older, with 57 subjects aged 75 years and older. The data from these trials indicated no overall differences in safety or effectiveness between elderly patients and their younger counterparts. Additionally, other reported clinical experiences have not identified significant differences in responses between geriatric patients and younger individuals.

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 ointment to elderly patients, considering potential variations in sensitivity and the need for careful monitoring of therapeutic responses.

Pregnancy

Mometasone Furoate Ointment, 0.1% is classified as Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women; 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. In studies involving pregnant rats, rabbits, and mice, mometasone furoate was associated with increased fetal malformations. Notably, the doses that produced malformations also resulted in decreased fetal growth, as evidenced by lower fetal weights and/or delayed ossification. Additionally, dystocia and related complications were observed in rats when administered mometasone furoate during the later stages of pregnancy.

In mice, subcutaneous administration of mometasone furoate at doses of 60 mcg/kg and above resulted in cleft palate, with reduced fetal survival noted at 180 mcg/kg. No toxicity was observed at a dose of 20 mcg/kg. In rats, topical doses of 600 mcg/kg and above produced umbilical hernias, while a dose of 300 mcg/kg led to delays in ossification without causing 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 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 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. It is not known whether topical administration of corticosteroids, such as Mometasone Furoate Ointment, 0.1%, could result in sufficient systemic absorption to produce detectable quantities in human milk. Therefore, caution should be exercised when administering this medication to lactating mothers.

Renal Impairment

Patients with renal impairment have not been specifically addressed in the available data regarding dosage adjustments, special monitoring, or safety considerations. Therefore, healthcare professionals should exercise caution when prescribing this medication to individuals with reduced kidney function, as the lack of information necessitates careful clinical judgment. Regular monitoring of renal function may be advisable in these patients to ensure safety and efficacy.

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

In the absence of specific overdosage information, it is essential for healthcare professionals to remain vigilant regarding the potential for overdose with this medication. In cases where an overdose is suspected, immediate medical attention should be sought.

Healthcare providers are advised to monitor patients closely for any signs or symptoms that may indicate an overdose. These may include, but are not limited to, increased severity of known side effects, unusual behavioral changes, or any other atypical clinical manifestations.

Management of an overdose should be guided by the clinical presentation of the patient. Supportive care is paramount, and symptomatic treatment should be initiated as necessary. It is recommended that healthcare professionals consult local poison control centers or relevant toxicology resources for specific guidance on the management of overdose cases.

In summary, while specific overdosage data is not available, healthcare professionals should exercise caution, remain observant for potential overdose symptoms, and implement appropriate management strategies as needed.

Nonclinical Toxicology

There are no adequate and well-controlled studies in pregnant women; therefore, Mometasone Furoate Ointment, 0.1% 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, mometasone furoate caused dystocia and related complications when administered to rats during the later stages of pregnancy. In mice, subcutaneous administration of mometasone furoate at 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 a dose of 20 mcg/kg. In rats, topical doses of 600 mcg/kg and above produced umbilical hernias, while a dose of 300 mcg/kg led to delays in ossification without causing 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, when rats received subcutaneous doses of mometasone furoate throughout pregnancy or during the later stages, a dose of 15 mcg/kg resulted in prolonged and difficult labor, as well as reduced 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 ointment, 0.1%. However, long-term carcinogenicity studies conducted via inhalation in rats and mice showed no statistically significant increase in tumors at inhalation doses up to 67 mcg/kg in a 2-year study in Sprague Dawley rats and up to 160 mcg/kg in a 19-month study in Swiss CD-1 mice. Mometasone furoate increased chromosomal aberrations in an in vitro Chinese hamster ovary cell assay but did not increase chromosomal aberrations 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

Postmarketing experience with Mometasone Furoate Ointment, 0.1% has identified several adverse events reported voluntarily or through surveillance programs.

There have been reports of potential systemic effects due to excessive absorption of the ointment, which may lead to adrenal gland dysfunction. Healthcare providers may conduct blood tests to monitor adrenal function in patients using this medication.

Vision-related issues have also been noted, with topical corticosteroids being associated with an increased risk of developing cataracts and glaucoma. Patients are advised to inform their healthcare provider if they experience blurred vision or other visual disturbances during treatment.

Skin reactions have been documented, including allergic reactions such as contact dermatitis and localized skin infections at the application site. 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 include burning, itching, skin atrophy, tingling, stinging, and the formation of boils.

Patients are encouraged to seek medical advice regarding any side effects and may report adverse events to the FDA at 1-800-FDA-1088.

Patient Counseling

Healthcare providers should advise patients to read the FDA-approved patient labeling (Patient Information) prior to using Mometasone Furoate Ointment, 0.1%. It is essential to use the ointment strictly as directed by the physician, emphasizing that it is for external use only. Patients should be instructed to avoid contact with the eyes and to report any visual symptoms to their healthcare provider immediately.

Patients must be informed that Mometasone Furoate Ointment, 0.1% should not be applied to the face, underarms, or groin areas, and it should only be used for the specific disorder for which it was prescribed. They should also be cautioned against bandaging or covering the treated skin area in an occlusive manner unless directed by their physician. Any signs of local adverse reactions should be reported to the physician without delay.

It is critical to inform patients that Mometasone Furoate Ointment, 0.1% is not indicated for the treatment of diaper dermatitis and should not be applied in the diaper area, as diapers or plastic pants may create an occlusive dressing. Patients should discontinue therapy once control is achieved and should contact their physician if no improvement is observed within two weeks.

Healthcare providers should advise patients not to use other corticosteroid-containing products concurrently with Mometasone Furoate Ointment, 0.1% without prior consultation. The ointment is intended for use on the skin only and should not be applied to the eyes, mouth, or vagina. Additionally, it should not be used in children under 2 years of age, and its safety and efficacy in children beyond three weeks of use have not been established.

Before initiating treatment with Mometasone Furoate Ointment, 0.1%, patients should inform their healthcare provider about all existing medical conditions and any medications they are currently taking, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Patients should be instructed to apply a thin film of the ointment to the affected skin area once daily and to continue using it until improvement is noted. They should also be reminded to wash their hands after application.

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), in compliance with USP Controlled Room Temperature guidelines. Proper storage conditions are essential to maintain the integrity and efficacy of the product.

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.

In postmarketing experience, cataracts and glaucoma have been reported in patients using topical corticosteroid products, including those containing mometasone.

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)