Mometasone furoate

Description

Mometasone Furoate Topical Solution USP, 0.1% contains mometasone furoate, a synthetic corticosteroid with 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 521.4.

Mometasone furoate appears as a white to off-white powder that is insoluble in water, freely soluble in acetone and methylene chloride, and sparingly soluble in heptane. Each gram of the topical solution contains 1 mg of mometasone furoate in a clear to translucent, colorless solution base comprising 40% isopropyl alcohol, hexylene glycol, hydroxypropyl cellulose, sodium phosphate monobasic anhydrous, purified water, glycerin, and oleic acid. Phosphoric acid may also be included to adjust the pH to approximately 4.5.

Uses and Indications

Mometasone Furoate Topical Solution 0.1% 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

Mometasone Furoate Topical Solution, 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 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.

Side Effects

Patients using Mometasone Furoate Topical Solution, 0.1% may experience a range of adverse reactions. Common adverse reactions reported include acneiform reactions, burning, itching, and folliculitis.

Serious adverse reactions associated with the use of this medication include 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 occlusive dressings should be monitored periodically for signs of HPA axis suppression. If such suppression is detected, it is advised to modify the treatment regimen accordingly.

Pediatric patients are particularly susceptible to systemic toxicity, with studies indicating that approximately 29% of pediatric subjects aged 6 to 23 months experienced HPA axis suppression despite having normal adrenal function prior to treatment. Follow-up testing revealed suppressed HPA axis function in one subject. The risk of HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension is heightened in pediatric patients receiving topical corticosteroids. Symptoms of adrenal suppression in children may include low plasma cortisol levels and a lack of response to ACTH stimulation, while manifestations of intracranial hypertension can present as bulging fontanelles, headaches, and bilateral papilledema.

Additionally, the use of Mometasone Furoate Topical Solution may increase 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 Topical Solution 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 Topical Solution 0.1%. Therefore, the potential for drug interactions remains undefined. Clinicians are advised to exercise caution and monitor patients for any unexpected effects when Mometasone Furoate is used concurrently with other medications.

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 0.1% have not been established in pediatric patients under 12 years of age; therefore, its use in this population is not recommended. In a study involving pediatric subjects aged 6 to 23 months, HPA axis suppression occurred in approximately 29% of those with normal adrenal function prior to treatment. These subjects were treated for about 3 weeks, covering a mean body surface area of 40% (range 16%-90%).

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. Additionally, they 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 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. Signs of adrenal suppression may manifest as low plasma cortisol levels and a lack of response to ACTH stimulation. Symptoms of intracranial hypertension can include bulging fontanelles, headaches, and bilateral papilledema. Mometasone Furoate Topical Solution 0.1% is contraindicated for the treatment of diaper dermatitis.

Geriatric Use

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

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 with mometasone furoate lotion.

Pregnancy

Mometasone Furoate Topical Solution 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 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, resulted in increased 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 exposed to mometasone furoate at topical doses of 150 mcg/kg and above exhibited multiple malformations, including flexed front paws, gallbladder agenesis, umbilical hernia, and hydrocephaly. In oral studies, doses of 700 mcg/kg resulted in increased resorptions and cleft palate or head malformations, while at 2800 mcg/kg, most litters were aborted or resorbed. No toxicity was observed at 140 mcg/kg.

When administered subcutaneously throughout pregnancy or during the later stages, a dose of 15 mcg/kg of mometasone furoate in rats caused prolonged and difficult labor, as well as a reduction in the number 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 potential 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 for topical administration of corticosteroids to result in sufficient systemic absorption to produce detectable quantities in human milk is not known. Therefore, caution should be exercised when Mometasone Furoate Topical Solution 0.1% is administered to lactating mothers.

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 monitoring of renal function may be warranted to ensure patient safety and therapeutic 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 Topical Solution 0.1% 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 possibility of systemic effects necessitates careful monitoring of the patient.

Management of overdosage should focus on 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 where systemic effects are suspected, discontinuation of the topical solution and symptomatic treatment may be warranted.

Healthcare professionals are advised to report any adverse effects or unusual symptoms to the appropriate regulatory authorities to contribute to the ongoing safety monitoring of Mometasone Furoate Topical Solution.

Nonclinical Toxicology

Long-term animal studies have not been conducted to assess the carcinogenic potential of mometasone furoate lotion. However, long-term carcinogenicity studies have been performed via the inhalation route in both rats and mice. In a 2-year carcinogenicity study involving Sprague Dawley rats, mometasone furoate did not show 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 mcg/m². Similarly, a 19-month carcinogenicity study in Swiss CD-1 mice revealed 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 with Chinese hamster lung cells. The compound was not found to be mutagenic in the Ames test or the mouse lymphoma assay, nor was it clastogenic 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 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 mcg/m².

Postmarketing Experience

Postmarketing experience with Mometasone Furoate Topical Solution, 0.1% has identified several adverse events reported voluntarily or through surveillance programs. The most frequently reported side effects include burning, itching, and inflammation of the hair follicle (folliculitis).

Serious side effects have also been noted, particularly concerning vision. There is a potential risk for developing vision problems, such as cataracts and glaucoma, associated with the use of topical corticosteroids. Patients are advised to inform their healthcare provider if they experience blurred vision or other vision-related issues during treatment.

Skin-related adverse events have been documented, including allergic reactions (contact dermatitis) and skin infections at the site of application. Patients should discontinue use and consult their healthcare provider if they experience any skin reactions, such as pain, tenderness, swelling, or difficulties with healing.

Healthcare professionals are encouraged to report any side effects to the FDA at 1-800-FDA-1088 for further monitoring and evaluation.

Patient Counseling

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

Patients must be informed that Mometasone Furoate Topical Solution 0.1% should not be applied to the face, underarms, or groin areas. It is critical to use this medication solely for the specific disorder for which it was prescribed. Additionally, patients should not bandage, cover, or wrap the treated skin area in a manner that is occlusive unless directed by their physician.

Healthcare providers should specifically instruct patients not to use Mometasone Furoate Topical Solution 0.1% for the treatment of diaper dermatitis and to avoid applying it 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.

It is important to advise patients against using other corticosteroid-containing products concurrently with Mometasone Furoate Topical Solution 0.1% without prior consultation with their physician. Patients should be encouraged to inform their healthcare provider about all medications they are taking, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Special attention should be given to informing the healthcare provider if they are taking other corticosteroid medicines by mouth or using other topical corticosteroid products.

Patients should be instructed to apply a few drops of Mometasone Furoate Topical Solution 0.1% to the affected skin area once daily, rubbing it in lightly until it disappears. They should continue using the solution until the affected area improves and should notify their healthcare provider if there is no improvement after two weeks of treatment.

After application, patients should wash their hands thoroughly. They should be advised to seek medical advice regarding any side effects and may report side effects to the FDA at 1-800-FDA-1088. Lastly, healthcare providers should remind patients that medications are sometimes prescribed for purposes other than those listed in the Patient Information leaflet, and Mometasone Furoate Topical Solution 0.1% should not be used for any condition other than that for which it was prescribed. It should not be shared with others, even if they exhibit similar symptoms, as it may cause harm.

Storage and Handling

Mometasone Furoate Topical Solution, 0.1% is supplied in a suitable container that ensures product integrity. It should be stored at a temperature range of 20°-25°C (68°-77°F), in accordance with USP Controlled Room Temperature guidelines. Proper storage conditions are essential to maintain 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, emphasizing the importance of avoiding contact of Mometasone Furoate Topical Solution, 0.1% with the eyes.

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)