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ELOCON® (mometasone furoate cream) Cream contains mometasone furoate for dermatologic use. Mometasone furoate is a synthetic corticosteroid with anti-inflammatory activity.
Chemically, mometasone furoate is 9(alpha),21-Dichloro-11(beta),17-dihydroxy-16(alpha)-methylpregna-1,4-diene-3,20-dione 17-(2-furoate), with the empirical formula C 27 H 30 CI 2 O 6 , a molecular weight of 521.4 and the following structural formula:
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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 of ELOCON Cream 0.1% contains: 1 mg mometasone furoate in a cream base of hexylene glycol, phosphoric acid, propylene glycol stearate, stearyl alcohol and ceteareth-20, titanium dioxide, aluminum starch octenylsuccinate, 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 A 2 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 A 2 .
The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle and the integrity of the epidermal barrier. Occlusive dressings with hydrocortisone for up to 24 hours have not been demonstrated to increase penetration; however, occlusion of hydrocortisone for 96 hours markedly enhances penetration. Studies in humans indicate that approximately 0.4% of the applied dose of ELOCON Cream 0.1% enters the circulation after 8 hours of contact on normal skin without occlusion. Inflammation and/or other disease processes in the skin may increase percutaneous absorption.
Studies performed with ELOCON Cream indicate that it is in the medium range of potency as compared with other topical corticosteroids.
In a pediatric trial, 24 atopic dermatitis patients, of which 19 patients were age 2 to 12 years, were treated with ELOCON Cream 0.1% once daily. The majority of patients cleared within 3 weeks.
ELOCON Cream 0.1% is a medium potency corticosteroid indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
ELOCON (mometasone furoate cream) Cream 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 ELOCON Cream have not been established in pediatric patients below 2 years of age, its use in this age group is not recommended.
ELOCON Cream is contraindicated in those patients with a history of hypersensitivity to any of the components in the preparation.
General Systemic absorption of topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal of treatment. Manifestations of Cushing' syndrome, hyperglycemia, and glucosuria can also be produced in some patients by systemic absorption of topical corticosteroids while on treatment.
Patients applying a topical steroid to a large surface area or to areas under occlusion should be evaluated periodically for evidence of HPA axis suppression. This may be done by using the ACTH stimulation, A.M. plasma cortisol, and urinary free cortisol tests.
In a study evaluating the effects of mometasone furoate cream on the hypothalamic-pituitary-adrenal (HPA) axis, 15 grams were applied twice daily for 7 days to six adult patients with psoriasis or atopic dermatitis. The cream was applied without occlusion to at least 30% of the body surface. The results show that the drug caused a slight lowering of adrenal corticosteroid secretion.
If HPA axis suppression is noted, an attempt should be made to withdraw the drug, to reduce the frequency of application, or to substitute a less potent corticosteroid. Recovery of HPA axis function is generally prompt upon discontinuation of topical corticosteroids. Infrequently, signs and symptoms of glucocorticosteroid insufficiency may occur requiring supplemental systemic corticosteroids. For information on systemic supplementation, see Prescribing Information for those products.
Pediatric patients may be more susceptible to systemic toxicity from equivalent doses due to their larger skin surface to body mass ratios (see PRECAUTIONS - Pediatric Use ).
If irritation develops, ELOCON Cream should be discontinued and appropriate therapy instituted. Allergic contact dermatitis with corticosteroids is usually diagnosed by observing a failure to heal rather than noting a clinical exacerbation as with most topical products not containing corticosteroids. Such an observation should be corroborated with appropriate diagnostic patch testing.
If concomitant skin infections are present or develop, an appropriate antifungal or antibacterial agent should be used. If a favorable response does not occur promptly, use of ELOCON Cream should be discontinued until the infection has been adequately controlled.
Information for Patients Patients using topical corticosteroids should receive the following information and instructions:
Laboratory Tests The following tests may be helpful in evaluating patients for HPA axis suppression:
Carcinogenesis, Mutagenesis, and Impairment of Fertility In studies of the effect of mometasone furoate on fertility, pregnancy, and postnatal development in rats and rabbits, 25 rats were treated with doses up to 1.2 mg/kg of drug topically, and 15 rabbits with doses up to 0.3 mg/kg of drug topically. The drugs were left on the skin for 6 hours daily during gestation. At the highest dosage, the rat dams lost weight. One of the rabbit dams at the highest dosage had wrinkled skin, muscle wasting and aborted 5 fetuses.
Genetic toxicity studies with mometasone furoate, which included the Ames test, mouse lymphoma assay, and a micronucleus test did not reveal any mutagenic potential.
Long term animal studies have not been performed to evaluate the carcinogenic potential of ELOCON (mometasone furoate cream) Cream.
Pregnancy Teratogenic effects: Pregnancy Category C 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.
Rat offspring of dams treated with 1.2 mg/kg of mometasone furoate topically (4 times the maximum dose in a 50 kg individual) displayed umbilical hernias, unossified sternebrae and vertebrae, and wavy ribs, as well as markedly depressed fetal growth. Rabbit offspring of dams treated with up to 0.3 mg/kg of mometasone furoate topically (the same dose as the maximum dose in a 50 kg individual) displayed flexed paws, umbilical hernias, and cleft palate. A 50 kg female using 1 gram of ELOCON Cream would apply approximately 0.023 mg/kg.
There are no adequate and well-controlled studies of the teratogenic potential of mometasone furoate in pregnant women. ELOCON Cream should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Because many drugs are excreted in human milk, caution should be exercised when ELOCON Cream is administered to a nursing woman.
Pediatric Use ELOCON Cream may be used with caution 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. Use of ELOCON Cream is supported by results from adequate and well-controlled studies in pediatric patients with corticosteroid-responsive dermatoses. Since safety and efficacy of ELOCON Cream have not been established in pediatric patients below 2 years of age, its use in this age group is not recommended. Because of a higher ratio of skin surface area to body mass, pediatric patients are at a greater risk than adults of HPA axis suppression and Cushing' syndrome when they are treated with topical corticosteroids. They are, therefore, also at greater risk of adrenal insufficiency during and/or after withdrawal of treatment. Pediatric patients may be more susceptible than adults to skin atrophy, including striae, when they are treated with topical corticosteroids. Pediatric patients applying topical corticosteroids to greater than 20% of body surface are at higher risk of HPA axis suppression.
HPA axis suppression, Cushing' syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension have been reported in pediatric patients receiving topical corticosteroids. Manifestations of adrenal suppression in children include low plasma cortisol levels, and an absence of response to ACTH stimulation. Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema.
ELOCON (mometasone furoate cream) Cream should not be used in the treatment of diaper dermatitis.
In controlled clinical studies involving 319 patients, the incidence of adverse reactions associated with the use of ELOCON Cream was 1.6%. Reported reactions included burning, pruritus, and skin atrophy. Reports of rosacea associated with the use of ELOCON Cream have also 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 ELOCON Cream was approximately 7%. Reported reactions included stinging, pruritus, and furunculosis.
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 listed 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 ELOCON Cream can be absorbed in sufficient amounts to produce systemic effects (see PRECAUTIONS ).
Apply a thin film of ELOCON Cream to the affected skin areas once daily. ELOCON Cream may be used in pediatric patients 2 years of age or older. Safety and efficacy of ELOCON Cream in pediatric patients for more than 3 weeks of use have not been established. Use in pediatric patients under 2 years of age is not recommended.
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.
ELOCON Cream should not be used with occlusive dressings unless directed by a physician. ELOCON Cream should not be applied in the diaper area if the child still requires diapers or plastic pants as these garments may constitute occlusive dressing.
ELOCON Cream 0.1% is supplied in 15 g (NDC 0085-0567-01) and 45 g (NDC 0085-0567-02) tubes; boxes of one.
Store ELOCON Cream between 2° and 25°C (36° and 77°F).
Schering Corporation
Kenilworth, NJ 07033 USA
Revised 8/95 14112839
18724308T
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