Mometasone furoate

Description

Mometasone Furoate Ointment USP, 0.1% contains mometasone furoate, a synthetic corticosteroid recognized for its anti-inflammatory properties, intended for topical application. The chemical structure of mometasone furoate is defined 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 521.43.

Mometasone furoate appears as a white or almost white powder, which is practically insoluble in water, freely soluble in acetone and methylene chloride, and slightly soluble in alcohol. Each gram of Mometasone Furoate Ointment USP, 0.1% contains 1 mg of mometasone furoate, incorporated within an ointment base that includes hexylene glycol, phosphoric acid, propylene glycol monopalmitostearate, purified water, white petrolatum, and white wax.

Uses and Indications

Mometasone furoate ointment 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 ointment 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 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 evaluate patients who are applying a topical steroid over large surface areas or under occlusive dressings periodically 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 risk-benefit profile 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 professionals should remain vigilant for any visual symptoms in patients and consider referral to an ophthalmologist for further evaluation if such symptoms arise.

Side Effects

Patients using mometasone furoate ointment may experience a range of adverse reactions. Common adverse reactions reported include burning, pruritus, skin atrophy, tingling or stinging sensations, and furunculosis.

Serious warnings associated with the use of this medication include the potential for reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, which may lead to glucocorticosteroid insufficiency following withdrawal of treatment. Patients applying the topical steroid over large surface areas or under occlusion should be periodically evaluated for signs of HPA axis suppression, and modifications to treatment should be made if such suppression is observed. Additionally, there is an increased risk of developing cataracts and glaucoma; therefore, if patients experience visual symptoms, a referral to an ophthalmologist should be considered.

Pediatric patients may be particularly susceptible to systemic toxicity, with reports indicating that topical corticosteroids can lead to HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension. In children, manifestations of adrenal suppression may include low plasma cortisol levels and a lack of response to ACTH stimulation. Symptoms of intracranial hypertension can present as bulging fontanelles, headaches, and bilateral papilledema.

It is important to note that mometasone furoate ointment is contraindicated in individuals with a history of hypersensitivity to any of its components. Furthermore, while systemically administered corticosteroids are known to appear in human milk and may suppress growth or interfere with endogenous corticosteroid production, it remains unclear whether topical corticosteroids can achieve sufficient systemic absorption to produce detectable quantities in human milk.

Drug Interactions

No drug-drug interaction studies have been conducted with mometasone furoate ointment. Therefore, the potential for drug interactions remains undefined. Clinicians are advised to exercise caution when prescribing this medication alongside other treatments, as the absence of specific interaction data necessitates careful monitoring of the patient's overall therapeutic regimen.

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 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 ointment 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 HPA axis suppression after treatment for about 3 weeks, with a mean body surface area of 39% (range 15% to 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 than adults for HPA axis suppression and Cushing’s syndrome due to their greater skin surface area relative to body mass. They are also more susceptible to glucocorticosteroid insufficiency during and after treatment withdrawal, as well as to skin atrophy, including striae. 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 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 a lack of response to ACTH stimulation, while signs of intracranial hypertension may include bulging fontanelles, headaches, and bilateral papilledema. Mometasone furoate ointment should not be used for the treatment of diaper dermatitis.

Geriatric Use

Clinical trials of Mometasone furoate ointment 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 in some older individuals cannot be ruled out. Therefore, healthcare providers should exercise caution when prescribing Mometasone furoate ointment 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 ointment. 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. The doses that produced these 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 mometasone furoate was administered during the later stages of pregnancy.

Specific findings from animal studies indicate that in mice, subcutaneous 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, topical doses of 150 mcg/kg and above caused multiple malformations, including flexed front paws, gallbladder agenesis, umbilical hernia, and hydrocephaly. An oral study in rabbits indicated that a dose of 700 mcg/kg increased resorptions and caused cleft palate and/or head malformations, with most litters being 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 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 mometasone furoate use in pregnant patients and counsel women of childbearing potential accordingly.

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, could result in sufficient systemic absorption to produce detectable quantities in human milk. Therefore, caution should be exercised when administering mometasone furoate ointment 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 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

Topically applied mometasone furoate ointment has the potential to be absorbed in sufficient quantities, which may lead to systemic effects.

In the event of an overdosage, healthcare professionals should be vigilant for signs and symptoms associated with excessive exposure to corticosteroids. These may include, but are not limited to, adrenal suppression, Cushing's syndrome, and other systemic corticosteroid-related effects.

Management of overdosage should focus on the immediate cessation of the topical application of mometasone furoate. Supportive care and monitoring of the patient’s clinical status are essential. If systemic effects are observed, appropriate interventions should be initiated based on the severity of the symptoms.

Healthcare professionals are advised to consult relevant clinical guidelines and toxicology resources for further management strategies in cases of corticosteroid overdosage.

Nonclinical Toxicology

Long-term animal studies have not been performed to evaluate the carcinogenic potential of mometasone furoate ointment. However, long-term carcinogenicity studies of mometasone furoate were conducted via the inhalation route in rats and mice. In a 2-year carcinogenicity study involving Sprague Dawley rats, mometasone furoate did not demonstrate a statistically significant increase in tumor incidence at inhalation doses up to 67 mcg/kg, which is approximately 0.04 times the estimated maximum clinical topical dose from mometasone furoate ointment on a mcg/m² basis. Similarly, a 19-month carcinogenicity study in Swiss CD-1 mice showed no statistically significant increase in tumor incidence at inhalation doses up to 160 mcg/kg, approximately 0.05 times the estimated maximum clinical topical dose from mometasone furoate ointment on a mcg/m² basis.

In terms of mutagenicity, mometasone furoate increased chromosomal aberrations in an in vitro Chinese hamster ovary cell assay; however, it did not increase chromosomal aberrations in an in vitro Chinese hamster lung cell assay. Mometasone furoate was not found to be mutagenic in the Ames test or the mouse lymphoma assay, and it 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.

Reproductive studies in rats indicated that impairment of fertility was not observed in either male or female rats at subcutaneous doses up to 15 mcg/kg, which is approximately 0.01 times the estimated maximum clinical topical dose from mometasone furoate ointment on a mcg/m² basis.

Postmarketing Experience

Reports of local adverse reactions have been documented, and patients are advised to inform their physician of any such occurrences. Vision-related issues have been noted, with topical corticosteroids potentially increasing the risk of developing conditions such as cataracts and glaucoma. Patients should notify their healthcare provider if they experience blurred vision or other vision problems during treatment with mometasone furoate ointment.

Skin-related adverse events have also been reported, including allergic reactions (contact dermatitis) and skin infections at the site of application. Patients are instructed to discontinue use and consult their healthcare provider if they experience any skin reactions, such as pain, tenderness, swelling, or difficulties in healing while using mometasone furoate ointment.

The most frequently reported side effects associated with mometasone furoate ointment 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) carefully. It is important to inform patients that mometasone furoate ointment should be used strictly as directed by their physician and is intended for external use only. Patients should be cautioned to avoid contact with the eyes and to report any visual symptoms, such as blurred vision, to their healthcare provider.

Patients must be instructed not to apply mometasone furoate ointment to the face, underarms, or groin areas, and to use it solely for the condition for which it was prescribed. They should not bandage, cover, or wrap the treated skin area in a manner that is occlusive unless specifically directed by their physician. Additionally, patients should be made aware that mometasone furoate ointment is not suitable for treating diaper dermatitis and should not be applied in the diaper area due to the risk of occlusion from diapers or plastic pants.

Patients should discontinue therapy once control of the condition is achieved. If no improvement is observed within two weeks, they should contact their physician. It is essential to inform patients not to use other corticosteroid-containing products concurrently with mometasone furoate ointment without prior consultation with their healthcare provider.

Patients should apply a thin film of mometasone furoate ointment to the affected skin area once daily and continue its use until improvement is noted. They should wash their hands after application and be aware that excessive absorption of the ointment through the skin may lead to adrenal gland suppression, for which their healthcare provider may conduct blood tests.

Healthcare providers should discuss the potential for vision problems associated with topical corticosteroids, including an increased risk of cataracts and glaucoma. Patients should be instructed to report any vision changes during treatment. Furthermore, skin reactions such as allergic dermatitis or infections at the treatment site may occur; patients should stop using the ointment and inform their healthcare provider if they experience pain, tenderness, swelling, or issues with healing.

Finally, patients should be advised to store mometasone furoate ointment at room temperature, between 68°F to 77°F (20°C to 25°C), avoiding refrigeration and freezing. It is crucial to keep the ointment and all medications out of the reach of children.

Storage and Handling

The product is supplied in various package configurations, with specific NDC numbers available upon request. It should be stored at a controlled room temperature of 25°C (77°F), with permissible excursions between 15°C to 30°C (59°F to 86°F). It is essential to avoid refrigeration and prevent freezing to maintain product integrity. Proper handling and storage conditions are crucial to ensure the efficacy and safety 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 Glenmark Pharmaceuticals Inc. , USA. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)