(Mometasone Furoate Ointment, USP) 0.1% (w/w) Corticosteroid Taro Pharmaceuticals Inc. Date of Initial Preparation: Brampton, Ontario February 08, 2005 L6T 1C1 Control Number: 104582 June 16, 2006
Table of Contents
SUMMARY PRODUCT INFORMATION 3 INDICATIONS AND CLINICAL USE. 3 WARNINGS AND PRECAUTIONS. 3 ADVERSE REACTIONS. 5 DRUG INTERACTIONS. 6 DOSAGE AND ADMINISTRATION. 6 OVER DOSAGE. 6 ACTION AND CLINICAL PHARMACOLOGY. 7 STORAGE AND STABILITY. 7 DOSAGE FORMS, COMPOSITION AND PACKAGING. 8
PHARMACEUTICAL INFORMATION. 9 CLINICAL TRIALS. 10 DETAILED PHARMACOLOGY. 13 TOXICOLOGY. 14 REFERENCES. 16
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(Mometasone Furoate Ointment, USP) 0.1% (w/w)
| Route of Administration | Dosage Form/Strength | Clinically Relevant Nonmedicinal Ingredients |
| Topical | Ointment / 0.1% (w/w) | For a complete listing see Dosage Forms, Composition and Packaging section. |
Taro-Mometasone (mometasone furoate) Ointment 0.1% (w/w) is indicated for: the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses such as psoriasis and atopic dermatitis.
Taro-Mometasone (mometasone furoate) Ointment 0.1 % (w/w) is contraindicated in patients who are sensitive to mometasone furoate, to other corticosteroids or to any component of these preparations. For a complete listing, see the Dosage Forms, Composition, and Packaging section of the product monograph. Topical steroids are contraindicated in untreated fungal, bacterial and viral (i.e. herpes simplex, chicken pox and vaccinia) infections involving the skin.
General
Systemic absorption of topical corticosteroids will be increased if extensive body surface areas are treated or if the occlusive technique is used. Suitable precautions should be taken under these conditions or when long-term use is anticipated, particularly in infants and children. Pediatric patients may demonstrate greater susceptibility to topical corticosteroid-induced HPA axis suppression and Cushing's syndrome than mature patients because of a larger skin surface area to body weight ratio. Use of topical corticosteroids in children should be limited to the least amount compatible with an effective therapeutic regimen. Chronic corticosteroid therapy may interfere with growth and development of children. Patients should be advised to inform subsequent physicians of the prior use of glucocorticoids.
Endocrine and Metabolism
Any of the side effects that have been reported following systemic use of corticosteroids, including adrenal suppression, may also occur with topical corticosteroids, especially in infants and children. Although mometasone furoate ointment is poorly absorbed, nevertheless, application of corticosteroids over extensive lesions, or exceeding the dosage schedule may result in significant systemic absorption producing hypercorticism manifesting itself by adrenal suppression, moon facies, striae and suppression of growth.
Immune
During the use of topical corticosteroids, infections may occur. If an overt infection is present, appropriate antimicrobial treatment is indicated. If symptomatic response is not noted within a few days to a week, the local application of corticosteroids should be discontinued and the patient re-evaluated.
Ophthalmologic
Mometasone furoate ointment is not formulated for ophthalmic use and should not be used in or near the eyes.
Skin
If irritation or sensitization develops with the use of mometasone furoate products, treatment should be discontinued and appropriate therapy instituted. Prolonged use of corticosteroid preparations may produce striae or atrophy of the skin or subcutaneous tissues. If this occurs, treatment should be discontinued.
Special Populations
Since safety of topical corticosteroid use in pregnant women has not been established, drugs of this class 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 in large amounts or for prolonged periods of time in pregnant patients.
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.
Evidence from clinical studies and experience suggests that use in the pediatric population is associated with differences in safety or effectiveness and a brief discussion can be found in the appropriate section.
Suitable precautions should be taken in using topical glucocorticoids in patients with impaired circulation suffering from stasis dermatitis and other skin diseases.
Adverse Drug Reaction Overview
Local adverse reactions rarely reported with mometasone furoate ointment 0.1 % include burning, pruritus, tingling/stinging and signs of skin atrophy. In <1 % of patients, adverse reactions reported with mometasone furoate ointment 0.1 % include aggravated allergy, dermatitis, erythema, furunculosis, increased lesion size, nausea (one patient) and vaginal discharge (one patient). The following local adverse reactions have been reported infrequently with the use of other topical corticosteroids: irritation, hypertrichosis, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, striae and miliaria.
Clinical Trial Adverse Drug Reactions
Because clinical trials are conducted under very specific conditions the adverse reaction rates observed in the clinical trials may not reflect the rates observed in practice and should not be compared to the rates in the clinical trials of another drug. Adverse drug reaction information from clinical trials is useful for identifying drug-related adverse events and for approximating rates.
The following local adverse reactions have been reported with mometasone furoate ointment: During clinical studies in 812 patients: burning - 13, pruritus - 8, skin atrophy - 8, tingling/stinging - 7, and furunculosis - 3. 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. Adrenal suppression has also been reported following topical corticosteroid therapy. Posterior subcapsular cataracts have been reported following systemic use of corticosteroids. The overall incidence of side effects was 4.9%, i.e. 40 of 812 subjects reported treatment-related adverse experiences. Side effects were mild to moderate and were those typically associated with topical corticosteroid formulations after seven days of treatment. No systemic treatment-related adverse experiences were seen.
Drug-Drug Interactions
Interactions with other drugs have not been established.
Drug-Food Interactions
Interaction with food has not been established.
Drug-Herb Interactions
Interaction with herbs has not been established.
Drug-Laboratory Interactions
Interaction with laboratory testing has not been established.
Drug- Lifestyle Interactions
Interaction with lifestyle has not been established.
Apply a thin film of Taro-Mometasone ointment to the affected skin areas once daily. Do not use occlusive dressings.
No specific antidote is available and treatment should be symptomatic.
Symptoms:
Excessive, prolonged use of topical corticosteroids can suppress pituitary-adrenal function resulting in secondary adrenal insufficiency, which may present with any combination of the following symptoms: fatigue, weakness, decreased appetite, constipation, nausea, vomiting, diarrhea, abdominal pain, skin colour darkening (especially on scars, elbows, knees, knuckles, toes, lips, and mucous membranes).
Percutaneous absorption of corticosteroids can occur when large amounts of corticosteroids are applied. Toxic effects may include ecchymosis of skin, peptic ulceration, hypertension, aggravation of infection, hirsutism, acne, edema and muscle weakness due to protein depletion.
Treatment:
Appropriate symptomatic treatment is indicated. Acute hypercorticoid symptoms are virtually reversible. Treat electrolyte imbalance, if necessary. In cases of chronic toxicity, slow withdrawal of corticosteroids is advised.
Treatment of a patient with systemic toxic manifestations consists of assuring and maintaining a patent airway and supporting ventilation using oxygen and assisted or controlled respiration as required. This will be sufficient in the management of most reactions. Should circulatory depression occur, vasopressors such as ephedrine or metaraminol and intravenous fluids may be used. Should a convulsion persist despite oxygen therapy, small increments of an ultra-short acting barbiturate (pentobarbital or secobarbital) may be given intravenously. Allergic reactions are characterized by cutaneous lesions, urticaria, edema or anaphylactoid reactions.
Mechanism of Action
Mometasone furoate has anti-inflammatory, antipruritic and vasoconstrictive actions. The exact mechanism, however, of corticosteroids in each disease is uncertain. Mometasone furoate, has been shown to have topical (dermatologic) and systemic pharmacologic and metabolic effects characteristic of this class of drugs.
Pharmacokinetics
A percutaneous absorption study with radio-labeled 3H-mometasone furoate ointment was conducted in adult male volunteers with intact skin. Based on the amounts of radioactivity excreted after an eight-hour application of the active ointment and analysis of urine and feces, approximately 0.7% of the applied dose was absorbed systemically without occlusion.
Store at room temperature between 15/ and 30/C. Taro-Mometasone Ointment is stable for 24 months when stored between 15/ and 30/C.
Each gram of Taro-Mometasone (mometasone furoate) Ointment 0.1% (w/w) contains 1 mg mometasone furoate. Non medicinal ingredients include: white wax, white petrolatum, hexylene glycol and propylene glycol stearate. Taro-Mometasone (mometasone furoate) Ointment 0.1% (w/w) is supplied in 15 g and 50 g tubes, boxes of one.