MOMETASONE FUROATE OINTMENT USP, 0.1%

Rx only

For Dermatologic Use Only.
Not for Ophthalmic Use.

Mometasone Furoate Ointment USP, 0.1%, contains mometasone furoate, USP for dermatologic use. Mometasone furoate is a synthetic corticosteroid with anti-inflammatory activity.

Chemically, mometasone furoate is 9α,21-dichloro-11β,17-dihydroxy-16α,-methylpregna-1,4-diene-3,20-dione 17-(2-furoate), with the molecular formula C₂₇H₃₀CI₂O₆, a molecular weight of 521.43 and the following structural formula:

Mometasone furoate is a white to off-white powder practically insoluble in water, slightly soluble in octanol, and moderately soluble in ethyl alcohol. Each gram contains: 1 mg mometasone furoate in an ointment base of hexylene glycol; phosphoric acid; propylene glycol monostearate; white wax; white petrolatum; and purified water.

Like other topical corticosteroids, mometasone furoate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A₂ inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A₂.

Mometasone Furoate Ointment, 0.1%, is a medium potency corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

Mometasone furoate ointment, 0.1%, may be used in pediatric patients 2 years of age or older, although the safety and efficacy of drug use for longer than 3 weeks have not been established (see PRECAUTIONS - Pediatric Use). Since safety and efficacy of mometasone furoate ointment, 0.1% have not been adequately established in pediatric patients below 2 years of age, its use in this age group is not recommended.

Mometasone furoate ointment, 0.1% is contraindicated in those patients with a history of hypersensitivity to any of the components in the preparation.

Corticosteroids have been shown to be teratogenic in laboratory animals when administered systemically at relatively low dosage levels. Some corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. When administered to pregnant rats, rabbits, and mice, mometasone furoate increased fetal malformations. The doses that produced malformations also decreased fetal growth, as measured by lower fetal weights and/or delayed ossification. Mometasone furoate also caused dystocia and related complications when administered to rats during the end of pregnancy. In mice, mometasone furoate caused cleft palate at subcutaneous doses of 60 mcg/kg and above. Fetal survival was reduced at 180 mcg/kg. No toxicity was observed at 20 mcg/kg. (Doses of 20, 60 and 180 mcg/kg in the mouse are approximately 0.01, 0.02 and 0.05 times the estimated maximum clinical topical dose from mometasone furoate ointment, 0.1% on a mcg/m² basis). In rats, mometasone furoate produced umbilical hernias at topical doses of 600 mcg/kg and above. A dose of 300 mcg/kg produced delays in ossification, but no malformations. (Doses of 300 and 600 mcg/kg in the rat are approximately 0.2 and 0.4 times the estimated maximum clinical topical dose from mometasone furoate ointment, 0.1% on a mcg/m² basis). In rabbits, mometasone furoate caused multiple malformations (e.g., flexed front paws, gallbladder agenesis, umbilical hernia, hydrocephaly) at topical doses of 150 mcg/kg and above (approximately 0.2 times the estimated maximum clinical topical dose from mometasone furoate ointment, 0.1% on a mcg/m² basis). In an oral study, mometasone furoate increased resorptions and caused cleft palate and/or head malformations (hydrocephaly and domed head) at 700 mcg/kg. At 2800 mcg/kg most litters were aborted or resorbed. No toxicity was observed at 140 mcg/kg. (Doses of 140, 700 and 2800 mcg/kg in the rabbit are approximately 0.2, 0.9 and 3.6 times the estimated maximum clinical topical dose from mometasone furoate ointment, 0.1% on a mcg/m² basis).

When rats received subcutaneous doses of mometasone furoate throughout pregnancy or during the later stages of pregnancy, 15 mcg/kg caused prolonged and difficult labor and reduced the number of live births, birth weight and early pup survival. Similar effects were not observed at 7.5 mcg/kg. (Doses of 7.5 and 15 mcg/kg in the rat are approximately 0.005 and 0.01 times the estimated maximum clinical topical dose from mometasone furoate ointment, 0.1% on a mcg/m² basis).

There are no adequate and well-controlled studies of teratogenic effects from topically applied corticosteroids in pregnant women . Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

In controlled clinical studies involving 812 patients, the incidence of adverse reactions associated with the use of mometasone furoate ointment, 0.1% was 4.8%. Reported reactions included burning, pruritus, skin atrophy, tingling/stinging, and furunculosis. Reports of rosacea associated with the use of mometasone furoate ointment, 0.1% have been received. In controlled clinical studies (n=74) involving pediatric patients 2 to 12 years of age, the incidence of adverse experiences associated with the use of mometasone furoate cream is approximately 7%. Reported reactions included stinging, pruritus, and furunculosis. The following adverse reactions were reported to be possibly or probably related to treatment with mometasone furoate ointment, 0.1% during a clinical study, in 5% of 63 pediatric patients 6 months to 2 years of age: decreased glucocorticoid levels, 1; an unspecified skin disorder, 1; and a bacterial skin infection, 1. The following signs of skin atrophy were also observed among 63 patients treated with mometasone furoate ointment, 0.1% in a clinical study: shininess 4, telangiectasia 1, loss of elasticity 4, loss of normal skin markings 4, thinness 1. Striae and bruising were not observed in this study. The following additional local adverse reactions have been reported infrequently with topical corticosteroids, but may occur more frequently with the use of occlusive dressings. These reactions are uled in an approximate decreasing order of occurrence: irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, striae, and miliaria.

Topically applied mometasone furoate ointment, 0.1% can be absorbed in sufficient amounts to produce systemic effects (see PRECAUTIONS).

Apply a thin film of mometasone furoate ointment, 0.1% to the affected skin areas once daily. Mometasone furoate ointment, 0.1% may be used in pediatric patients 2 years of age or older. Since safety and efficacy of mometasone furoate ointment, 0.1% have not been adequately established in pediatric patients below 2 years of age, its use in this age group is not recommended (see PRECAUTIONS - Pediatric Use). As with other corticosteroids, therapy should be discontinued when control is achieved. If no improvement is seen within 2 weeks, reassessment of diagnosis may be necessary. Safety and efficacy of mometasone furoate ointment, 0.1% in pediatric patients for more than 3 weeks have not been established.

Mometasone furoate ointment, 0.1% should not be used with occlusive dressings unless directed by a physician. Mometasone furoate ointment, 0.1% should not be applied in the diaper area if the child still requires diapers or plastic pants as these garments may constitute occlusive dressing.

Mometasone Furoate Ointment USP, 0.1%, is supplied as follows:

NDC 0168-0271-15 15 gram tube
NDC 0168-0271-46 45 gram tube

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F)

[See USP Controlled Room Temperature].

E. FOUGERA & CO.
a division of Altana Inc.,
MELVILLE, NEW YORK 11747

I2271
R9/04
#121