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DIPROSONE products contain betamethasone dipropionate, USP, a synthetic adrenocorticosteroid, for dermatologic use. Betamethasone, an analog of prednisolone, has high corticosteroid activity and slight mineralocorticoid activity. Betamethasone dipropionate is the 17, 21-dipropionate ester of betamethasone.
Chemically, betamethasone dipropionate is 9-Fluoro-11(beta),17,21-trihydroxy-16(beta)-methylpregna-1,4-diene-3,20-dione 17,21-dipropionate, with the empirical formula C 28 H 37 FO 7 , a molecular weight of 504.6, and the following structural formula:
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Betamethasone dipropionate is a white to creamy white, odorless crystalline powder, insoluble in water.
Each gram of DIPROSONE Cream 0.05% contains: 0.643 mg betamethasone dipropionate, USP (equivalent to 0.5 mg betamethasone) in a hydrophilic emollient cream consisting of purified water, USP; mineral oil, USP; white petrolatum, USP; ceteareth-30; cetearyl alcohol 70/30 (7.2%); sodium phosphate monobasic monohydrate R; and phosphoric acid, NF; chlorocresol, NF; and propylene glycol, USP as preservatives. May also contain sodium hydroxide R to adjust pH to approximately 5.0.
Each gram of DIPROSONE Lotion 0.05% w/w contains: 0.643 mg betamethasone dipropionate, USP (equivalent to 0.5 mg betamethasone) in a lotion base of isopropyl alcohol, USP (39.25%); and purified water, USP; slightly thickened with carbomer 974P; the pH is adjusted to approximately 4.7 with sodium hydroxide.
Each gram of DIPROSONE Ointment 0.05% contains: 0.643 mg betamethasone dipropionate, USP (equivalent to 0.5 mg betamethasone) in an ointment base of mineral oil, USP; and white petrolatum, USP.
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 betamethasone dipropionate, are effective in the treatment of corticosteroid-responsive dermatoses primarily because of their anti-inflammatory, antipruritic, 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. Betamethasone dipropionate, a corticosteroid, 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. Inflammation and/or other disease processes in the skin increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids. (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. 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.
DIPROSONE products are indicated for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
DIPROSONE products are contraindicated in patients who are hypersensitive to betamethasone dipropionate, to other corticosteroids, or to any ingredient in these preparations.
General Systemic absorption of 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 the application of the more potent steroids, use over large surface areas, prolonged use, and the addition of occlusive dressings. (See DOSAGE AND ADMINISTRATION .)
Therefore, patients receiving a large dose of a potent topical steroid applied to a large surface area 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.
Information for Patients 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.
Patients using topical corticosteroids should receive the following information and instructions:
1.This medication is to be used as directed by the physician. It is for external use only. Avoid contact with the eyes.
2.Patients should be advised not to use this medication for any disorder other than that for which it was prescribed.
3.The treated skin area should not be bandaged or otherwise covered or wrapped as to be occlusive. (See DOSAGE AND ADMINISTRATION .)
4.Patients should report any signs of local adverse reactions.
5.Parents of pediatric patients should be advised not to use tight-fitting diapers or plastic pants on a patient 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:
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 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 prescribed for a nursing woman.
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 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.
The following local adverse reactions are reported infrequently when DIPROSONE products are used as recommended in the DOSAGE AND ADMINISTRATION section. 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.
Systemic absorption of topical corticosteroids has produced reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing' syndrome, hyperglycemia, and glucosuria in some patients.
Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects. (See PRECAUTIONS .)
DIPROSONE Cream Apply a thin film of DIPROSONE Cream 0.05% to the affected skin areas once daily. In some cases, a twice-daily dosage may be necessary.
DIPROSONE Lotion: Apply a few drops of DIPROSONE Lotion to the affected area and massage lightly until it disappears. Apply twice daily, in the morning and at night. For the most effective and economical use, apply nozzle very close to affected area and gently squeeze bottle.
DIPROSONE Ointment Apply a thin film of DIPROSONE Ointment to the affected skin areas once daily. In some cases, a twice-daily dosage may be necessary.
DIPROSONE products are not to be used with occlusive dressings.
DIPROSONE Cream 0.05% is supplied in 15-g (NDC 0085-0853-02) and 45-g (NDC 0085-0853-03) tubes; boxes of one.
DIPROSONE Lotion 0.05% w/w is available in 20-mL (18.7-g) (NDC 0085-0028-04) and 60-mL (56.2-g) (NDC 0085-0028-06) plastic squeeze bottles; boxes of one. Protect from light. Store in carton until contents are used.
DIPROSONE Ointment 0.05% is supplied in 15-g (NDC 0085-0510-04) and 45-g (NDC 0085-0510-06) tubes; boxes of one.
Store all DIPROSONE preparations between 2° and 30°C (36° and 86°F).
Schering Corporation
Kenilworth, NJ 07033 USA
Rev. 2/99
20860510T
Copyright © 1974, 1991, 1999,
Schering Corporation. All rights reserved.