Brands, Medical Use, Clinical Data
- Anti-Inflammatory Agents, Non-Steroidal
- Dermatologic Agents
- Gel (0.1%)
Brands / Synonyms
Adapaleno [INN-Spanish]; Adapalenum [INN-Latin]; Differin; Differin
For the topical treatment of comedo, papular and pustular acne (acne vulgaris) of the face, chest or back.
Adapalene is a chemically stable retinoid-like compound. 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.
Mechanism of Action
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 may normalize the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.
Absorption of adapalene through human skin is low. Only trace amounts (<0.25 ng/mL) of parent substance have been found in the plasma of acne patients following chronic topical application of adapalene in controlled clinical trials
The acute oral toxicity of adapalene 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.
Biotrnasformation / Drug Metabolism
Metabolized mainly by O-demethylation, hydroxylation and conjugation, and excretion is primarily by the biliary route.
DIFFERIN Gel should not be administered to individuals who are hypersensitive to adapalene or any of the
components in the vehicle gel.
As DIFFERIN Gel has the potential to produce local irritation in some patients, concomitant use of other
potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a
strong drying effect, and products with high concentrations of alcohol, astringents, spices or lime) should be
approached with caution. Particular caution should be exercised in using preparations containing sulfur, resorcinol,
or salicylic acid in combination with DIFFERIN Gel. If these preparations have been used it is advisable not to start
therapy with DIFFERIN Gel until the effects of such preparations in the skin have subsided.