Prescription Drugs

CLINICAL PHARMACOLOGY Topical corticosteroids share anti-inflammatory, antipruritic and vasoconstrictive actions. The mechanism of anti-inflammatory activity of the topical corticoster­oids is unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man. Pharmacokinetics 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. Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticoster­oids. Thus, occlusive dressings may be a valuable therapeutic adjunct for treatment of resistant dermatoses. (See DOSAGE AND ADMINISTRATION.) 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. They 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.

Find Lowest Prices on ApexiCon® E Cream (diflorasone diacetate) Cream USP 0.05% [Emollient] Not For Ophthalmic Use DESCRIPTION Each gram of ApexiCon® E Cream (diflorasone diacetate cream USP 0.05% [emollient]) contains 0.5 mg diflorasone diacetate in a cream base for topical dermatological use. Chemically, diflorasone diacetate is: 6±,9-difluoro-11”,17,21-trihydroxy-16”-methylpregna-1,4-diene-3,20-dione 17,21-diacetate. The structural formula is represented below: Each gram of ApexiCon® E Cream (diflorasone diacetate cream USP 0.05% [emollient]) con­tains: 0.5 mg diflorasone diacetate in a hydrophilic vanishing cream base of propylene glycol, stearyl alcohol, cetyl alcohol, sorbitan monostearate, polysorbate 60, mineral oil and purified water.

INDICATIONS Topical corticosteroids are indicated for relief of the inflammatory and pruritic manifestations of corticosteroid responsive dermatoses. DOSAGE AND ADMINISTRATION ApexiCon® E Cream (diflorasone diacetate cream USP 0.05% [emollient]) should be applied to the affected areas as a thin film from one to three times daily depending on the severity or resistant nature of the condition. Occlusive dressings may be used for the management of psoriasis or recalcitrant conditions. If an infection develops, the use of occlusive dressings should be discontinued and appropriate antimicrobial therapy initiated. HOW SUPPLIED ApexiCon® E Cream (diflorasone diacetate cream USP 0.05% [emollient]) is available in the following size tubes: NDC 0462-0395-30 30 gram tube NDC 0462-0395-60 60 gram tube Store at controlled room temperature 20° - 25°C (68° -77°F) [see USP]. PharmaDerm.,  A division of Nycomed US Inc.Melville, NY 11747, USA. www.pharmaderm.com. Rev: 1/08

OVERDOSE Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects. (See PRECAUTIONS). CONTRAINDICATIONS Topical steroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.

SIDE EFFECTS The following local adverse reactions have been reported 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: burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria. DRUG INTERACTIONS No information provided.

WARNINGS No information provided. PRECAUTIONS General Systemic absorption of topical corticosteroids has produced reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some patients. Conditions which augment systemic absorption include the application of the more potent steroids, use over large surface areas, prolonged use, and the addition of occlusive dressings. Therefore, 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. Pediatric patients 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, the 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. Laboratory Tests The following tests may be helpful in evaluating the 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. Studies to determine mutagenicity with prednisolone and hydrocortisone have revealed nega­tive results. Pregnancy Category C Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels.The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids. 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 of time. 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, caution should be exercised when topical corti­costeroids are administered to a nursing woman. Pediatric Use Safety and effectiveness of diflorasone diacetate emollient cream in pediatric patients have not been established. 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 when they are treated with topical corticosteroids. They are, therefore, also at greater risk of glucocor­ticosteroid insufficiency after withdrawal of treatment and of Cushing's syndrome while on treatment. Adverse effects including striae have been reported with inappropriate use of topical corticosteroids in pediatric patients. HPA axis suppression, Cushing's syndrome, and intracranial hypertension have been reported in pediatric patients receiving topical corticosteroids. Manifestations of adrenal suppression in pediatric patients 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 pediatric patients should be limited to the least amount compatible with an effective therapeutic regimen. Chronic corticosteroid therapy may interfere with the growth and development of pediatric patients.