Mometasone furoate

Description

Mometasone Furoate Topical Solution USP, 0.1% (Lotion) is formulated for topical application and contains mometasone furoate, a synthetic corticosteroid exhibiting 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.

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 the topical solution contains 1 mg of mometasone furoate, suspended in a clear to translucent lotion base composed of hydroxypropyl cellulose, isopropyl alcohol (40% v/v), phosphoric acid, propylene glycol, purified water, and sodium phosphate monobasic.

Uses and Indications

Mometasone Furoate Topical Solution USP, 0.1% (Lotion) is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses in patients aged 12 years and older.

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

Dosage and Administration

Healthcare professionals are advised to apply a few drops of the medication to the affected skin areas once daily. The application should be followed by a light massage until the product is fully absorbed.

Therapy should be discontinued once adequate control of the condition is achieved. In cases where no improvement is observed within 2 weeks of initiating treatment, a reassessment of the diagnosis is recommended.

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

Contraindications

Momentasone furoate topical solution (lotion) 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 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 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 the medication may experience a range of adverse reactions. Common adverse reactions reported include acneiform reactions, burning sensations, itching, and folliculitis.

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. Additionally, Cushing's syndrome and hyperglycemia may occur due to systemic absorption, particularly in patients applying a 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 identified.

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.

Furthermore, the use of this medication may elevate the risk of cataracts and glaucoma. Should any visual symptoms arise, a referral to an ophthalmologist should be considered for further evaluation.

Drug Interactions

Mometasone furoate topical solution (lotion) has not undergone any drug-drug interaction studies. As a result, there is currently no available data regarding potential interactions with other medications. Clinicians are advised to exercise caution when prescribing this medication alongside other treatments, as the absence of interaction studies limits the understanding of its safety profile in combination with other drugs. Monitoring for any unexpected effects is recommended when mometasone furoate is used concurrently with other therapies.

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

The safety and efficacy of mometasone furoate topical solution (lotion) have not been established in pediatric patients below 12 years of age; therefore, its use in this age group is not recommended. In a study involving pediatric subjects aged 6 to 23 months, approximately 29% experienced hypothalamic-pituitary-adrenal (HPA) axis suppression after treatment for about 3 weeks, with a mean body surface area of 40% (ranging from 16% to 90%).

Due to a higher ratio of skin surface area to body mass, pediatric patients are at an increased risk of HPA axis suppression and Cushing's syndrome when treated with topical corticosteroids. Additionally, they may be more susceptible to skin atrophy, including striae. Those applying topical corticosteroids to more than 20% of their body surface area are at an elevated risk for HPA axis suppression.

Adverse effects associated with topical corticosteroid use in pediatric patients 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 an absence of response to ACTH stimulation. Symptoms of intracranial hypertension can include bulging fontanelles, headaches, and bilateral papilledema.

Mometasone furoate topical solution (lotion) is contraindicated for the treatment of diaper dermatitis.

Geriatric Use

Clinical trials of mometasone furoate topical solution (lotion) did not include a sufficient number of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, other reported clinical experience has not identified significant differences in responses between elderly patients and younger patients.

In general, dose selection for geriatric patients should be approached with caution. It is advisable to start at the low end of the dosing range to minimize the risk of adverse effects and to ensure safety in this population. Regular monitoring may be warranted to assess efficacy and tolerability in elderly patients receiving treatment.

Pregnancy

Mometasone furoate topical solution (lotion) is classified as a Pregnancy Category C medication. There are no adequate and well-controlled studies in pregnant women; therefore, the use of mometasone furoate during pregnancy should only be considered if the potential benefits justify the potential risks to the fetus.

Corticosteroids, including mometasone furoate, have demonstrated teratogenic effects in laboratory animals when administered systemically at relatively low doses. In studies involving pregnant rats, rabbits, and mice, mometasone furoate was associated with increased fetal malformations, which were accompanied by 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.

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. 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 led to delays in ossification without causing 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. Oral administration at 700 mcg/kg resulted in increased resorptions and cleft palate, with most litters aborted or resorbed at 2800 mcg/kg. No toxicity was noted at 140 mcg/kg.

Given these findings, healthcare professionals should carefully weigh the potential risks and benefits when considering the use of 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 topical solution (lotion) to lactating mothers.

Renal Impairment

There is no specific information 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 topical solution (lotion) has the potential for systemic absorption, which may lead to significant systemic effects in cases of overdosage.

In the event of an overdose, healthcare professionals should be vigilant for symptoms that may arise due to excessive exposure. While specific symptoms of overdosage are not detailed, the systemic effects could include manifestations typical of corticosteroid overexposure, such as adrenal suppression, Cushing's syndrome, or other related complications.

Management of overdosage should focus on supportive care and symptomatic treatment. It is recommended that healthcare providers monitor the patient closely for any adverse effects and initiate appropriate interventions as necessary. If systemic effects are suspected, further evaluation and management may be warranted, including consultation with a specialist in toxicology or endocrinology.

In summary, while the risk of overdosage with mometasone furoate topical solution is low when used as directed, awareness of the potential for systemic absorption and the associated risks is essential for effective patient management.

Nonclinical Toxicology

There are no adequate and well-controlled studies in pregnant women; therefore, mometasone furoate topical solution (lotion) 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, administration of mometasone furoate at 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 a dose of 20 mcg/kg. In rats, topical doses of 600 mcg/kg and above led to the occurrence of umbilical hernias, while a dose of 300 mcg/kg caused delays in ossification without producing 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 mometasone furoate increased resorptions and caused cleft palate and/or head malformations (hydrocephaly and domed head) at 700 mcg/kg, 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 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 topical solution (lotion). However, long-term carcinogenicity studies conducted via inhalation in rats and mice showed no statistically significant increase in tumor incidence. In a 2-year carcinogenicity study in Sprague Dawley rats, mometasone furoate demonstrated no significant increase in tumors at inhalation doses up to 67 mcg/kg. Similarly, a 19-month carcinogenicity study in Swiss CD-1 mice revealed no 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 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

Mometasone furoate topical solution (lotion) has been associated with various postmarketing experiences reported voluntarily or through surveillance programs.

It is noted that the formulation can permeate 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 linked to an increased risk of vision-related complications, 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 reported, including allergic reactions (contact dermatitis) and localized skin infections at the application site. Patients should discontinue use and consult their healthcare provider if they notice any skin reactions, such as pain, tenderness, swelling, or impaired healing.

Common side effects associated with mometasone furoate topical solution (lotion) include burning, itching, and inflammation of hair follicles (folliculitis).

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

Patient Counseling

Healthcare providers should advise patients to read the FDA-approved patient labeling (Patient Information) thoroughly to understand the proper use of mometasone furoate topical solution (lotion). It is essential to inform patients that this medication is intended for external use only and should be applied as directed by their physician.

Patients should be cautioned to avoid contact with the eyes and to report any visual symptoms to their healthcare provider immediately. It is important to instruct patients not to use mometasone furoate topical solution (lotion) on sensitive areas such as the face, underarms, or groin. Additionally, patients should be made aware that this medication should only be used for the specific disorder for which it was prescribed.

Healthcare providers should emphasize that patients must not bandage or cover the treated skin area in a manner that creates an occlusive dressing unless specifically directed by their physician. Patients should also be encouraged to report any signs of local adverse reactions to their healthcare provider.

Furthermore, it is crucial to inform patients that mometasone furoate topical solution (lotion) should not be used for the treatment of diaper dermatitis, as applying it in the diaper area may lead to occlusion due to diapers or plastic pants. Patients should be advised to discontinue therapy once control is achieved and to contact their physician if no improvement is observed within two weeks.

Lastly, healthcare providers should remind patients not to use other corticosteroid-containing products in conjunction with mometasone furoate topical solution (lotion) without prior consultation with 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), 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

No further data are available.

FDA Insert (PDF)

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

View full prescribing information (PDF)