ELOCON Lotion 0.1% contains mometasone furoate, USP, 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 Cl ₂ O ₆ , a molecular weight of 521.4 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 of ELOCON Lotion 0.1% contains: 1 mg of mometasone furoate, USP, in a lotion base of isopropyl alcohol, USP (40%); propylene glycol, USP; hydyroxypropyl cellulose, NF; sodium phosphate monobasic monohydrate, R; and purified water, USP. May also contain phosphoric acid NF to adjust the pH to approximately 4.5.

The corticosteroids are a class of compounds comprising steroid hormones secreted by the adrenal cortex and their synthetic analogs. In pharmacologic doses corticosteroids are used primarily for their anti-inflammatory and/or immunosuppressive effects.

Topical corticosteroids, such as mometasone furoate, are effective in the treatment of corticosteroid-responsive dermatoses primarily because of their anti-inflammatory, anti-pruritic, and vasoconstrictive actions. However, while the physiologic, pharmacologic, and clinical effects of the corticosteroids are well known, the exact mechanisms of their actions in each disease are uncertain. Mometasone furoate has been shown to have topical (dermatologic) and systemic pharmacologic and metabolic effects characteristic of this class of drugs.

The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings. (See DOSAGE AND ADMINISTRATION .) Topical corticosteroids can be absorbed from normal intact skin.

A study using a radio-labelled ³ H mometasone furoate ointment (0.1%) formulation was performed in man to measure systemic absorption and excretion. Results showed that approximately 0.7% of the steroid was absorbed during 8 hours of contact, without occlusion, with intact skin of normal volunteers. A similar minimal degree of absorption of the corticosteroid from the lotion formulation would be anticipated.

Inflammation and/or disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. (See DOSAGE AND ADMINISTRATION .)

Mometasone furoate lotion was applied at 15 mL twice daily (30 mL per day) to diseased skin (patients with scalp and body psoriasis) of four patients for seven days, to study its effects on the hypothalamic-pituitary-adrenal (HPA) axis. Plasma cortisol levels for each of the four patients remained well within the normal range and changed little from baseline.

Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

ELOCON Lotion is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

CONTRAINDICATIONS

ELOCON Lotion is contraindicated in patients who are hypersensitive to mometasone furoate, to other corticosteroids, or to any ingredient in this preparation.

PRECAUTIONS

General Systemic absorption of potent topical corticosteroids has produced reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing' syndrome, hyperglycemia, and glucosuria in some patients.

Conditions which augment systemic absorption include application of more potent steroids, use over large surface areas, prolonged use, use in areas where the epidermal barrier is disrupted, and the use of occlusive dressings. (See DOSAGE AND ADMINISTRATION .)

Patients receiving a large dose of a potent topical steroid applied to a large surface area or under an occlusive dressing should be evaluated periodically for evidence of HPA axis suppression by using the urinary free cortisol and ACTH stimulation tests. 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 steroid.

Recovery of HPA axis function is generally prompt and complete upon discontinuation of the drug. Infrequently, signs and symptoms of steroid withdrawal may occur, requiring supplemental systemic corticosteroids.

Children may absorb proportionally larger amounts of topical corticosteroids and thus be more susceptible to systemic toxicity. (See PRECAUTIONS --Pediatric Use .)

If irritation develops, topical corticosteroids should be discontinued and appropriate therapy instituted.

In the presence of dermatological infections, use of an appropriate antifungal or antibacterial agent should be instituted. If a favorable response does not occur promptly, the corticosteroid should be discontinued until the infection has been adequately controlled.

Information for Patients Patients using topical corticosteroids should receive the following information and instructions. This information is intended to aid in the safe and effective use of this medication. It is not a disclosure of all possible adverse or intended effects.

This medication is to be used as directed by the physician. It is for external use only. Avoid contact with the eyes.
Patients should be advised not to use this medication for any disorder other than that for which it was prescribed.
The treated skin area should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by the physician. (See DOSAGE AND ADMINISTRATION .)
Patients should report any signs of local adverse reactions.
Parents of pediatric patients should be advised not to use tight-fitting diapers or plastic pants on a child being treated in the diaper area, as these garments may constitute occlusive dressing. (See DOSAGE AND ADMINISTRATION .)

Laboratory Tests The following tests may be helpful in evaluating HPA axis suppression:

Urinary free cortisol test

ACTH stimulation test

Carcinogenesis, Mutagenesis, and Impairment of Fertility Long-term animal studies have not been performed to evaluate the carcinogenic potential or the effect on fertility of topical corticosteroids.

Genetic toxicity studies with mometasone furoate, which included the Ames test, mouse lymphoma assay, and a micronucleus test, did not reveal any mutagenic potential.

Pregnancy Category C Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. Corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. 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. Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods.

Nursing Mothers It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically administered corticosteroids are secreted into breast milk in quantities not likely to have a deleterious effect on the infant. Nevertheless, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use Pediatric patients may demonstrate greater susceptibility to topical corticosteroid-induced HPA axis suppression and Cushing' syndrome than mature patients because of a larger skin surface area to body weight ratio.

Hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing' syndrome, and intracranial hypertension have been reported in children receiving topical corticosteroids. Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol levels, and absence of response to ACTH stimulation. Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema. Administration of topical corticosteroids to children should be limited to the least amount compatible with an effective therapeutic regimen. Chronic corticosteroid therapy may interfere with the growth and development of children.

ADVERSE REACTIONS

The following local adverse reactions were reported with ELOCON Lotion during clinical studies with 209 patients: acneiform reaction, 2; burning, 4; and itching, 1. In an irritation/sensitization study with 156 normal subjects, folliculitis was reported in 4.

The following local adverse reactions have been reported infrequently when other topical dermatologic corticosteroids have been used as recommended. These reactions are listed in an approximate decreasing order of occurrence: burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria.

OVERDOSAGE

Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects. (See PRECAUTIONS .)

DOSAGE AND ADMINISTRATION

Apply a few drops of ELOCON Lotion to the affected areas once daily and massage lightly until it disappears. For the most effective and economical use, hold the nozzle of the bottle very close to the affected areas and gently squeeze.

HOW SUPPLIED

ELOCON Lotion 0.1% is supplied in 30 mL (27.5 g) (NDC 0085-0854-01) and 60 mL (55 g) (NDC 0085-0854-02) bottles; boxes of one.

Store ELOCON Lotion between 2° and 30°C (36° and 86°F).

Schering Corporation

Kenilworth, NJ 07033 USA

Rev. 1/99 17980912