Mometasone Furoate

Description

Mometasone furoate anhydrous, USP, is the active ingredient in mometasone furoate nasal spray, delivering 50 mcg per dose. It is classified as an anti-inflammatory corticosteroid, with the chemical name 9,21-Dichloro-11ß,17-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione 17-(2-furoate). The compound has an empirical formula of C27H30Cl2O6 and a molecular weight of 521.43 g/mol.

Mometasone furoate anhydrous appears as a white to off-white powder and exhibits limited solubility characteristics; it is practically insoluble in water, slightly soluble in methanol, ethanol, and isopropanol, soluble in acetone and chloroform, and freely soluble in tetrahydrofuran. The partition coefficient between octanol and water exceeds 5,000, indicating a high lipophilicity.

The mometasone furoate nasal spray is formulated as a metered-dose, manual pump spray unit, containing an aqueous suspension of mometasone furoate, USP, in a medium that includes benzalkonium chloride, citric acid, glycerin, microcrystalline cellulose, carboxymethylcellulose sodium, polysorbate 80, and sodium citrate. The pH of the formulation is maintained between 4.3 and 4.9.

Uses and Indications

Mometasone furoate nasal spray is indicated for the prophylaxis of nasal symptoms associated with seasonal allergic rhinitis in adult and pediatric patients aged 12 years and older. Additionally, it is indicated for the treatment of chronic rhinosinusitis with nasal polyps in adult patients aged 18 years and older.

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

Dosage and Administration

For the prophylaxis of Seasonal Allergic Rhinitis in adult and pediatric patients aged 12 years and older, the recommended dosage is 2 sprays in each nostril once daily.

In the treatment of Chronic Rhinosinusitis with Nasal Polyps in adults aged 18 years and older, the recommended dosage is 2 sprays in each nostril twice daily. An alternative regimen of 2 sprays in each nostril once daily may also be effective for some patients.

The medication is intended for nasal use only and should be administered as a spray. It is important to adhere to the specified frequency of administration: once daily for prophylaxis and twice daily for treatment, with the option of once daily for certain patients with Chronic Rhinosinusitis.

Contraindications

Use of mometasone furoate nasal spray is contraindicated in patients with a known hypersensitivity to mometasone furoate or any of its components. This contraindication is essential to prevent potential allergic reactions that may occur in susceptible individuals.

Warnings and Precautions

Patients using mometasone furoate nasal spray should be monitored periodically for signs of adverse effects on the nasal mucosa, including epistaxis, nasal ulceration, Candida albicans infection, nasal septal perforation, and impaired wound healing. It is imperative to avoid the use of this medication in individuals with recent nasal ulcers, nasal surgery, or nasal trauma due to the heightened risk of complications.

Ocular health should also be a consideration, as there is a potential risk for the development of glaucoma and cataracts. Healthcare professionals should consider referring patients to an ophthalmologist if they exhibit ocular symptoms or if they are using mometasone furoate nasal spray for an extended period.

Caution is advised in patients with a history of tuberculosis or those with fungal, bacterial, viral, or parasitic infections, as well as in individuals with ocular herpes simplex. The use of mometasone furoate nasal spray may exacerbate these conditions, leading to a more serious or even fatal progression of infections such as chickenpox or measles in susceptible patients.

Additionally, the risk of hypercorticism and adrenal suppression increases with dosages that exceed the recommended levels or with regular dosages in susceptible individuals. Should any signs of these conditions arise, it is essential to discontinue the use of mometasone furoate nasal spray gradually.

In pediatric patients, there is a potential for reduced growth velocity associated with the use of mometasone furoate nasal spray. Therefore, routine monitoring of growth is recommended for children receiving this treatment to ensure any potential impacts on growth are identified and managed appropriately.

Side Effects

Patients receiving mometasone furoate nasal spray may experience a range of adverse reactions. Common adverse reactions reported include headache, viral infection, pharyngitis, epistaxis, and cough.

In addition to these common reactions, there are several important considerations regarding additional adverse effects. Epistaxis and nasal ulceration have been noted, along with Candida albicans infection, nasal septal perforation, and impaired wound healing. It is recommended that patients be monitored periodically for signs of adverse effects on the nasal mucosa, and the use of this medication should be avoided in individuals with recent nasal ulcers, nasal surgery, or nasal trauma.

Ocular complications such as glaucoma and cataracts have also been associated with the use of mometasone furoate nasal spray. Patients who develop ocular symptoms or require long-term treatment should be considered for referral to an ophthalmologist.

There is a potential risk for the worsening of existing infections, including tuberculosis, fungal, bacterial, viral, or parasitic infections, as well as ocular herpes simplex. In susceptible patients, there may be a more serious or even fatal course of chickenpox or measles. Caution is advised in patients with these conditions due to the potential for exacerbation.

Higher than recommended dosages or regular dosages in susceptible individuals may lead to hypercorticism and adrenal suppression. Should such changes occur, it is advised to discontinue the use of mometasone furoate nasal spray gradually.

In pediatric patients, there is a potential reduction in growth velocity associated with the use of mometasone furoate nasal spray. Routine monitoring of growth in children receiving this treatment is essential, as the potential for "catch up" growth following discontinuation has not been adequately studied. The growth effects of prolonged treatment should be carefully weighed against the clinical benefits and the availability of safe and effective non-corticosteroid alternatives. To minimize systemic effects, each patient should be titrated to the lowest effective dose. The possibility of growth suppression in susceptible patients or at higher doses cannot be ruled out.

Drug Interactions

Mometasone furoate nasal spray has not undergone formal drug-drug interaction studies. However, the following interactions have been identified, particularly concerning the metabolism of mometasone furoate.

Inhibitors of Cytochrome P450 3A4

Mometasone furoate is primarily metabolized in the liver, with cytochrome CYP3A4 playing a significant role in its metabolic pathway. The concomitant use of CYP3A4 inhibitors may lead to reduced metabolism of mometasone furoate, resulting in increased systemic exposure and a heightened risk of systemic corticosteroid side effects.

Caution is advised when co-administering mometasone furoate nasal spray with strong CYP3A4 inhibitors, including but not limited to:

• Ketoconazole (long-term use)

• Ritonavir

• Cobicistat-containing products

• Atazanavir

• Clarithromycin

• Indinavir

• Itraconazole

• Nefazodone

• Nelfinavir

• Saquinavir

• Telithromycin

When considering the co-administration of these agents, healthcare professionals should weigh the potential benefits against the risks of systemic corticosteroid effects. Patients receiving this combination should be closely monitored for any signs of systemic corticosteroid side effects.

Packaging & NDC

The table below lists all NDC Code configurations of Mometasone Furoate (mometasone), the U.S. brand-name prescription product. Columns show Packaging, Formulation Type, and Active Ingredient Strength.

Pediatric Use

The safety and effectiveness of mometasone furoate nasal spray for the prophylaxis of nasal symptoms associated with seasonal allergic rhinitis have been established in pediatric patients aged 12 years and older. This indication is supported by evidence from controlled trials involving both adult and pediatric populations aged 12 years and older.

However, the safety and effectiveness of mometasone furoate nasal spray for the treatment of chronic rhinosinusitis with nasal polyps in pediatric patients under 18 years of age have not been established. A clinical trial assessing its efficacy in pediatric patients aged 6 to 17 years did not demonstrate effectiveness in this indication. In this study, 127 patients were randomized to receive either placebo or mometasone furoate nasal spray at doses of 100 mcg once or twice daily for patients aged 6 to 11 years, and 200 mcg once or twice daily for those aged 12 to 17 years.

It is important to note that controlled clinical studies have indicated that nasal corticosteroids, including mometasone furoate, may lead to a reduction in growth velocity in pediatric patients. Therefore, routine monitoring of growth in pediatric patients receiving nasal corticosteroids is recommended, which can be conducted through stadiometry.

A specific clinical study evaluating the effect of mometasone furoate nasal spray (100 mcg total daily dose) on growth velocity in pediatric patients aged 3 to 9 years with allergic rhinitis showed no statistically significant effect on growth velocity compared to placebo after one year of treatment. Nonetheless, the potential for mometasone furoate nasal spray to cause growth suppression in susceptible patients or when administered at higher doses cannot be excluded.

Geriatric Use

Elderly patients, specifically those aged 65 years and older, have been treated with mometasone furoate nasal spray for conditions such as allergic rhinitis and chronic rhinosinusitis with nasal polyps. In clinical studies, a total of 280 patients above the age of 64, with an age range of 64 to 86 years, received treatment for durations of up to 3 or 4 months.

Clinical findings indicate that there are no observed differences in safety and effectiveness between geriatric patients and younger adult patients. Therefore, no specific dosage adjustments are necessary for elderly patients. However, it is advisable to monitor this population closely, as individual responses to treatment may vary.

Pregnancy

Mometasone is minimally absorbed systemically following nasal use, and maternal use is not expected to result in fetal exposure to the drug. However, available data from observational studies of mometasone use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes.

Animal reproduction studies have demonstrated that mometasone furoate can cause increased fetal malformations and decreased fetal survival and growth when administered to pregnant mice, rats, or rabbits at doses producing exposures approximately 1/3 to 8 times the maximum recommended human dose (MRHD) on a mcg/m² or AUC basis. Specifically, in an embryofetal development study with pregnant mice dosed throughout the period of organogenesis, mometasone furoate produced cleft palate at a dose less than the maximum recommended daily intranasal dose (MRDID) and decreased fetal survival at approximately 2 times the MRDID. In pregnant rats, similar studies revealed fetal umbilical hernia at exposures approximately 10 times the MRDID and delays in fetal ossification at a dose approximately 6 times the MRDID. Additionally, pregnant rats dosed with mometasone furoate throughout pregnancy or late in gestation experienced prolonged and difficult labor, fewer live births, lower birth weight, and reduced early pup survival at a dose less than the MRDID.

Embryofetal development studies conducted with pregnant rabbits dosed with mometasone furoate by either the topical dermal route or oral route throughout the period of organogenesis showed multiple malformations in fetuses at doses approximately 6 times the MRDID and increased fetal resorptions, cleft palate, and/or head malformations at a dose approximately 30 times the MRDID.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies carry a background risk of birth defects, loss, or other adverse outcomes. In the U.S. general population, the estimated risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Given the potential risks observed in animal studies, mometasone furoate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation

There are no available data on the presence of mometasone furoate nasal spray in human milk, nor on the effects on breastfed infants or milk production. However, it is noted that mometasone is minimally absorbed systemically by lactating mothers following nasal use. Therefore, breastfeeding is not expected to result in significant exposure of the infant to mometasone.

When considering the use of mometasone furoate nasal spray in lactating mothers, the developmental and health benefits of breastfeeding should be weighed against the mother's clinical need for the medication. Additionally, potential adverse effects on the breastfed infant from mometasone furoate nasal spray or from the underlying maternal condition should be taken into account.

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 patients with reduced kidney function, as the lack of information necessitates careful clinical judgment and monitoring.

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

There are currently no data available regarding the effects of acute or chronic overdosage with mometasone furoate nasal spray. Due to the low systemic bioavailability of the drug and the lack of acute drug-related systemic findings observed in clinical studies, it is unlikely that an overdose would necessitate any therapeutic intervention beyond observation.

However, it is important to note that chronic overdosage with any corticosteroid, including mometasone furoate, may lead to signs or symptoms of hypercorticism. Healthcare professionals should remain vigilant for these potential manifestations in patients who may have been exposed to excessive doses over an extended period.

In the event of suspected overdosage, monitoring the patient and providing supportive care as needed is recommended.

Nonclinical Toxicology

Mometasone furoate has been evaluated for its teratogenic effects in various animal models. In mice, subcutaneous administration of mometasone furoate at doses of 60 mcg/kg and above resulted in the occurrence of cleft palate, with fetal survival significantly reduced at a dose of 180 mcg/kg, which is approximately two times the maximum recommended daily inhalation dose (MRDID) in adults on a mcg/m² basis. In rabbits, topical dermal doses of 150 mcg/kg and above led to multiple malformations, including flexed front paws, gallbladder agenesis, umbilical hernia, and hydrocephaly, corresponding to approximately six times the MRDID in adults on a mcg/m² basis. An oral study indicated that at a dose of 700 mcg/kg, approximately thirty times the MRDID in adults on a mcg/m² basis, there was an increase in resorptions and the occurrence of cleft palate and/or head malformations such as hydrocephaly or domed head. At a higher dose of 2,800 mcg/kg, approximately 110 times the MRDID in adults on a mcg/m² basis, most litters were either aborted or resorbed. Additionally, when pregnant rats received subcutaneous doses of 15 mcg/kg throughout pregnancy or during the later stages, there were reports of prolonged and difficult labor, as well as a reduction in the number of live births, birth weight, and early pup survival; these effects were not observed at a lower dose of 7.5 mcg/kg.

In terms of non-teratogenic effects, no toxicity was noted at a dose of 20 mcg/kg, which is less than the MRDID in adults on a mcg/m² basis. A dose of 300 mcg/kg, approximately six times the MRDID in adults on a mcg/m² basis, resulted in delays in ossification without causing malformations. Similar effects were not observed at 7.5 mcg/kg. In reproductive studies conducted in rats, subcutaneous doses of mometasone furoate up to 15 mcg/kg did not impair fertility.

Carcinogenicity studies have shown that mometasone furoate does not induce a statistically significant increase in tumor incidence. In a two-year carcinogenicity study in Sprague Dawley rats, inhalation doses up to 67 mcg/kg, approximately one to two times the MRDID in adults and children, respectively, did not result in tumor formation. Similarly, a 19-month carcinogenicity study in Swiss CD-1 mice at inhalation doses up to 160 mcg/kg, approximately two times the MRDID in adults and children, also showed no significant increase in tumor incidence.

Mometasone furoate was found to increase chromosomal aberrations in an in vitro assay using Chinese hamster ovary cells, although it did not increase chromosomal aberrations in an in vitro assay using Chinese hamster lung cells. It was not 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. Furthermore, mometasone furoate did not induce unscheduled DNA synthesis in vivo in rat hepatocytes.

Postmarketing Experience

Mometasone furoate nasal spray has been associated with various adverse reactions reported voluntarily or through surveillance programs. Notable adverse events include epistaxis (nosebleed) and nasal septum perforation. Additionally, cases of Candida infection have been documented.

Long-term use of nasal and inhaled corticosteroids may elevate the risk of ocular complications, such as glaucoma and cataracts; therefore, regular eye examinations are recommended. Patients receiving immunosuppressive doses of corticosteroids should be advised to avoid exposure to chickenpox or measles.

Serious side effects associated with mometasone furoate may include thrush (Candida infection), nasal septal perforation, delayed wound healing, and ocular issues such as glaucoma, cataracts, and blurred vision. Other reported concerns encompass allergic reactions, including wheezing, immune system complications that may heighten infection risk, adrenal insufficiency, and potential growth suppression in children.

The most frequently reported side effects of mometasone furoate include headache, viral infections, sore throat, nosebleeds, and cough. Healthcare professionals and patients are encouraged to report any side effects to the FDA at 1-800-FDA-1088.

Patient Counseling

Advise patients to read the FDA-approved patient labeling, including the Patient Information and Instructions for Use, prior to starting treatment with mometasone furoate nasal spray and each time they receive a refill, as there may be new information.

Inform patients that treatment with mometasone furoate nasal spray may be associated with adverse reactions, including epistaxis (nosebleed) and nasal septum perforation. Additionally, patients should be made aware that Candida infections may occur.

Caution patients against using nasal corticosteroids if they have experienced recent nasal septum ulcers, nasal surgery, or nasal trauma due to the inhibitory effect of corticosteroids on wound healing. Advise them not to spray mometasone furoate nasal spray directly onto the nasal septum.

Patients should be informed that long-term use of nasal and inhaled corticosteroids may increase the risk of eye problems, such as glaucoma or cataracts, and that regular eye examinations should be considered. It is also important to caution patients not to spray mometasone furoate nasal spray into their eyes.

For patients on immunosuppressant doses of corticosteroids, warn them to avoid exposure to chickenpox or measles, and advise that they seek medical advice promptly if exposed.

Encourage patients to use mometasone furoate nasal spray regularly for optimal effect, as improvement in nasal symptoms of allergic rhinitis may occur within 1 to 2 days after initiation of dosing, with maximum benefit typically achieved within 1 to 2 weeks. Patients should not increase the prescribed dosage and should contact their physician if symptoms do not improve or if their condition worsens.

Administration of the nasal spray to young children should be supervised by an adult. If a patient misses a dose, they should be advised to administer the missed dose as soon as they remember, but not to exceed the recommended daily dose.

Remind patients to use mometasone furoate exactly as prescribed by their healthcare provider, emphasizing that this medicine is for nasal use only and should not be sprayed into the mouth or eyes. Patients should not use mometasone furoate more often than prescribed and should consult their healthcare provider with any questions.

Finally, encourage patients to see their healthcare provider regularly to monitor their symptoms while using mometasone furoate and to check for any potential side effects.

Storage and Handling

Mometasone furoate nasal spray, 50 mcg, is supplied in a protective cardboard container to safeguard against light exposure. It is essential to store the product at a temperature range of 20° to 25°C (68° to 77°F), with permissible excursions between 15° to 30°C (59° to 86°F) in accordance with USP Controlled Room Temperature guidelines.

Once the nasal spray is removed from its cardboard container, it is crucial to minimize prolonged exposure to direct light; however, brief exposure during normal use is acceptable. Prior to each use, the product must be shaken well to ensure proper administration. Additionally, it should be kept out of reach of children to ensure safety.

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 Amneal Pharmaceuticals LLC. It includes detailed information about indications, dosage, contraindications, warnings, and clinical pharmacology.

View full prescribing information (PDF)