Mometasone furoate

Description

Mometasone furoate, USP ointment 0.1% is formulated for topical use and contains mometasone furoate, a synthetic corticosteroid recognized for its anti-inflammatory properties. 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 521.4.

This compound 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 the ointment contains 1 mg of mometasone furoate, combined with an ointment base consisting of hexylene glycol, phosphoric acid, propylene glycol stearate, purified water, white wax, and white petrolatum.

Uses and Indications

Mometasone furoate, USP 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.

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, USP 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 evaluate patients who are applying a topical steroid over large surface areas or under occlusive dressings periodically for signs of HPA axis suppression. Should 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, 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, USP 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 arise from the systemic absorption of the medication. Notably, reversible hypothalamic-pituitary-adrenal (HPA) axis suppression can occur, leading to potential glucocorticosteroid insufficiency following the withdrawal of treatment. Additionally, Cushing's syndrome and hyperglycemia have been associated with systemic absorption of the drug. Patients applying the ointment to large surface areas or under occlusion should be monitored periodically for signs of HPA axis suppression, and modifications to treatment should be made if such suppression is detected.

Pediatric patients may exhibit increased susceptibility to systemic toxicity, necessitating careful evaluation and monitoring. Furthermore, the use of topical corticosteroids may elevate the risk of cataracts and glaucoma; therefore, if patients experience visual symptoms, a referral to an ophthalmologist should be considered.

It is important to note that mometasone furoate, USP ointment 0.1% is contraindicated in individuals with a history of hypersensitivity to any of its components. The potential for systemic effects from topically applied mometasone furoate should also be acknowledged, as sufficient absorption can lead to adverse reactions beyond the local application site.

Drug Interactions

No drug-drug interaction studies have been conducted with mometasone furoate, USP ointment 0.1%. Therefore, the potential for drug interactions remains undefined. Clinicians are advised to exercise caution when prescribing this medication 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, USP ointment 0.1% may be used with caution in pediatric patients aged 2 years and older. However, its safety and efficacy for use beyond 3 weeks have not been established. The use of this medication is not recommended in pediatric patients under 2 years of age.

Pediatric patients are at an increased risk of hypothalamic-pituitary-adrenal (HPA) axis suppression and Cushing's syndrome when treated with topical corticosteroids. In a study, HPA axis suppression was observed in approximately 27% of pediatric subjects aged 6 to 23 months who were treated for about 3 weeks. Additionally, those applying topical corticosteroids to more than 20% of their body surface area are at a higher risk for HPA axis suppression.

Manifestations of adrenal suppression in children may include low plasma cortisol levels and an absence of response to adrenocorticotropic hormone (ACTH) stimulation. Furthermore, signs of intracranial hypertension in this population can present as bulging fontanelles, headaches, and bilateral papilledema. Mometasone furoate, USP ointment 0.1% should not be used for the treatment of diaper dermatitis.

Geriatric Use

Clinical trials of mometasone furoate, USP ointment 0.1% included a total of 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 drug in some older individuals cannot be ruled out. Therefore, healthcare providers should exercise caution when prescribing mometasone furoate to elderly patients, considering the potential for increased sensitivity. Monitoring for adverse effects and therapeutic efficacy is recommended to ensure optimal treatment outcomes in this population.

Pregnancy

There are no adequate and well-controlled studies in pregnant women regarding the use of mometasone furoate, USP ointment 0.1%. Therefore, this medication should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Mometasone furoate is classified as a Pregnancy Category C drug, indicating that teratogenic effects have been observed in laboratory animals.

Corticosteroids, including mometasone furoate, have demonstrated teratogenic effects in laboratory animals when administered systemically at relatively low dosage levels. Specifically, studies have shown that mometasone furoate, when administered to pregnant rats, rabbits, and mice, increased the incidence of fetal malformations. The doses that produced these malformations were also associated with decreased fetal growth, as evidenced by lower fetal weights and/or delayed ossification. Additionally, dystocia and related complications were observed in rats treated with 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 application of mometasone furoate at doses of 600 mcg/kg and above led to the development of umbilical hernias, while a dose of 300 mcg/kg caused delays in ossification without producing malformations.

Rabbits treated with mometasone furoate exhibited multiple malformations, including flexed front paws, gallbladder agenesis, umbilical hernia, and hydrocephaly, at topical doses of 150 mcg/kg and above. In oral studies, doses of 700 mcg/kg resulted in increased resorptions and cleft palate, as well as head malformations such as hydrocephaly and domed head. At 2800 mcg/kg, most litters were either aborted or resorbed, while 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 was associated with prolonged and difficult labor, as well as a reduction in the number of live births, birth weight, and early pup survival. These 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 and monitor for potential adverse fetal outcomes.

Lactation

There are no specific statements regarding the use of this medication in lactating mothers or its effects on breastfed infants. Healthcare professionals should consider the absence of data when advising lactating mothers about the use of this medication.

Renal Impairment

Patients with renal impairment have no specific information regarding dosage adjustments, special monitoring, or safety considerations provided in the text. Therefore, healthcare professionals should exercise caution and consider individual patient factors when prescribing to this population. Regular assessment of renal function may be warranted to ensure safe and effective use of the medication in patients with reduced kidney function.

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, USP ointment 0.1% has the potential for systemic absorption, which may lead to significant systemic effects in cases of overdosage.

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

Management of overdosage primarily involves supportive care. It is recommended that healthcare providers assess the patient's clinical status and provide appropriate interventions based on the severity of symptoms observed. In cases of significant systemic effects, discontinuation of the topical treatment may be necessary, and further evaluation may be warranted to address any complications arising from the overdosage.

Healthcare professionals are advised to report any adverse events or significant reactions to the appropriate regulatory authorities to ensure ongoing safety monitoring of mometasone furoate.

Nonclinical Toxicology

Long-term animal studies have not been performed to evaluate the carcinogenic potential of mometasone furoate, USP ointment 0.1%. However, long-term carcinogenicity studies have been 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 based 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.

In terms of mutagenicity, mometasone furoate increased chromosomal aberrations in an in vitro assay using Chinese hamster ovary cells; however, it did not increase chromosomal aberrations in an in vitro assay using Chinese hamster lung cells. Mometasone furoate was not found to be mutagenic in the Ames test or the mouse lymphoma assay, nor was it clastogenic in an in vitro mouse micronucleus assay, a rat bone marrow chromosomal aberration assay, or a mouse male germ-cell chromosomal aberration assay. Additionally, it did not induce unscheduled DNA synthesis in vivo in rat hepatocytes.

Reproductive studies in rats indicated that mometasone furoate did not impair fertility 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 based on a mcg/m² basis.

Postmarketing Experience

Postmarketing experience with mometasone furoate, USP ointment 0.1% has identified several adverse events reported voluntarily or through surveillance programs.

Mometasone furoate, USP ointment 0.1% is known to penetrate the skin, and excessive absorption may lead to adrenal gland dysfunction. Healthcare providers may conduct blood tests to monitor for potential adrenal issues in patients using this medication.

Additionally, the use of topical corticosteroids, including mometasone furoate, has been associated with an increased risk of vision-related complications, such as cataracts and glaucoma. Patients are advised to report any occurrences of blurred vision or other visual disturbances to their healthcare provider during treatment.

Skin-related adverse events have also been reported, including allergic reactions (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, USP ointment 0.1% include burning, itching, skin atrophy, tingling, stinging, and the formation of boils.

Patient Counseling

Patients should be advised to read the FDA-approved patient labeling (Patient Information) prior to using mometasone furoate, USP ointment 0.1%. It is essential that patients use the ointment strictly as directed by their physician, emphasizing that it is for external use only.

Healthcare providers should instruct patients to avoid contact with the eyes and to report any visual symptoms that may arise during treatment. Additionally, patients must be informed that mometasone furoate, USP 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.

Patients should be cautioned against bandaging or covering the treated skin area in a manner that could be occlusive, unless specifically directed by their physician. They should also be encouraged to report any signs of local adverse reactions to their healthcare provider promptly.

It is important to inform patients that mometasone furoate, USP 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 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 advised not to use other corticosteroid-containing products in conjunction with mometasone furoate, USP ointment 0.1% without prior consultation with their physician.

Storage and Handling

Mometasone furoate, USP ointment 0.1% is available in two package configurations: 15 gram tubes and 45 gram tubes, each supplied in boxes containing one tube.

This product should be stored at a controlled room temperature of 25°C (77°F), with permissible excursions between 15-30°C (59-86°F) in accordance with USP guidelines for controlled room temperature. Proper storage conditions are essential to maintain the integrity and efficacy of the ointment.

Additional Clinical Information

No further data are available.

FDA Insert (PDF)

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

View full prescribing information (PDF)