Adapalene Cream

In controlled clinical trials, local cutaneous irritation was monitored in 285 acne patients who used DIFFERIN® Cream once daily for 12 weeks. The frequency and severity of erythema, scaling, dryness, pruritus and burning were assessed during these studies. The incidence of local cutaneous irritation with DIFFERIN® Cream from the controlled clinical studies is provided in the following table:

Other reported local cutaneous adverse events in patients who used DIFFERIN® Cream once daily included: sunburn (2%), skin discomfort-burning and stinging (1%) and skin irritation (1%). Events occurring in less than 1% of patients treated with DIFFERIN® Cream included: acne flare, dermatitis and contact dermatitis, eyelid edema, conjunctivitis, erythema, pruritus, skin discoloration, rash, and eczema.

Rx Only

For topical use only. Not for ophthalmic, oral or intravaginal use.

Adapalene Cream, 0.1%, contains adapalene 0.1% in an aqueous cream emulsion consisting of carbomer 934P, cyclomethicone, edetate disodium, glycerin, methyl glucose sesquistearate, methylparaben, PEG-20 methyl glucose sesquistearate, phenoxyethanol, propylparaben, purified water, squalane, and trolamine.

The chemical name of adapalene is 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid. It is a white to off-white powder which is soluble in tetrahydrofuran, sparingly soluble in ethanol, and practically insoluble in water. The molecular formula is C28H28O3 and molecular weight is 412.52. Adapalene is represented by the following structural formula:

Mechanism of Action:

Adapalene acts on retinoid receptors. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization, and inflammatory processes all of which represent important features in the pathology of acne vulgaris.

Mechanistically, adapalene binds to specific retinoic acid nuclear receptors but does not bind to the cytosolic receptor protein. Although the exact mode of action of adapalene is unknown, it is suggested that topical adapalene normalizes the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.

Pharmacokinetics:

Absorption of adapalene from Adapalene Cream through human skin is low. In a pharmacokinetic study with six acne patients treated once daily for 5 days with 2 grams of Adapalene Cream applied to 1000 cm2 of acne involved skin, there were no quantifiable amounts (limit of quantification = 0.35 ng/mL) of adapalene in the plasma samples from any patient. Excretion appears to be primarily by the biliary route.

Adapalene Cream is indicated for the topical treatment of acne vulgaris.

Adapalene Cream is intended for cutaneous use only. If the medication is applied excessively, no more rapid or better results will be obtained and marked redness, scaling, or skin discomfort may occur. The acute oral toxicity of Adapalene Cream in mice and rats is greater than 10 mL/kg. Chronic ingestion of the drug may lead to the same side effects as those associated with excessive oral intake of Vitamin A.

Adapalene Cream should be applied to affected areas of the skin, once daily at nighttime. A thin film of the cream should be applied to the skin areas where acne lesions appear, using enough to cover the entire affected areas lightly. A mild transitory sensation of warmth or slight stinging may occur shortly after the application of Adapalene Cream.

NDC 0168-0424-46

Adapalene Cream 0.1%

For topical use only.
Not for ophthalmic, oral or intravaginal use.

NET WT 45 grams