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Diprolene AF (Betamethasone Dipropionate Topical) - Description and Clinical Pharmacology

 
 



For Dermatologic Use Only – Not for Ophthalmic Use

PRODUCT INFORMATION

DESCRIPTION

DIPROLENE® AF Cream 0.05% contains betamethasone dipropionate, USP, a synthetic adrenocorticosteroid, for dermatologic use in an emollient base. Betamethasone, an analog of prednisolone, has a high degree of corticosteroid activity and a slight degree of mineralocorticoid activity. Betamethasone dipropionate is the 17,21-dipropionate ester of betamethasone.

Chemically, betamethasone dipropionate is 9-fluoro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21-dipropionate, with the empirical formula C28H37FO7, a molecular weight of 504.6, and the following structural formula:

Betamethasone dipropionate is a white to creamy white, odorless crystalline powder, insoluble in water.

Each gram of DIPROLENE AF Cream 0.05% contains: 0.643 mg betamethasone dipropionate, USP (equivalent to 0.5 mg betamethasone) in an emollient cream base of purified water, USP; chlorocresol; propylene glycol, USP; white petrolatum, USP; white wax, NF; cyclomethicone; sorbitol solution, USP; glyceryl oleate/propylene glycol; ceteareth-30; carbomer 940, NF; and sodium hydroxide R.

CLINICAL PHARMACOLOGY

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.

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 (see DOSAGE AND ADMINISTRATION).

Topical corticosteroids can be absorbed through normal intact skin. Inflammation and/or other disease processes in the skin may increase percutaneous absorption. Occlusive dressings substantially increase the percutaneous absorption of topical corticosteroids (see DOSAGE AND ADMINISTRATION).

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

DIPROLENE® AF Cream 0.05% was applied once daily at 7 grams per day for 1 week to diseased skin, in adult patients with psoriasis or atopic dermatitis, to study its effects on the hypothalamic-pituitary-adrenal (HPA) axis. The results suggested that the drug caused a slight lowering of adrenal corticosteroid secretion, although in no case did plasma cortisol levels go below the lower limit of the normal range.

Sixty-seven pediatric patients ages 1 to 12 years, with atopic dermatitis, were enrolled in an open-label, hypothalamic-pituitary-adrenal (HPA) axis safety study. DIPROLENE AF Cream 0.05% was applied twice daily for 2 to 3 weeks over a mean body surface area of 58% (range 35% to 95%). In 19 of 60 (32%) evaluable patients, adrenal suppression was indicated by either a ≤5 mcg/dL pre-stimulation cortisol, or a cosyntropin post-stimulation cortisol ≤18 mcg/dL and/or an increase of <7 mcg/dL from the baseline cortisol. Studies performed with DIPROLENE AF Cream 0.05% indicate that it is in the high range of potency as compared with other topical corticosteroids.

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