Pharmacology: Pharmacodynamics: Topical: The exact mechanism is not known. Adapalene exhibits some retinoic acid-like activity but it also has additional effects. It is thought that adapalene reduces important features of the pathology of acne vulgaris by normalizing the differentiation of follicular epithelial cells and keratinization to prevent microcomedone formation, similar to the mechanism of retinoic acid. Unlike retinoic acid, adapalene selectively binds to some nuclear retinoic acid receptors (RARs) and does not bind to cellular receptors called cytosolic retinoic acid binding proteins (CRABPs). It is hypothesized that by selectively binding to certain nuclear retinoic acid. Also, adapalene may help reduce cell-mediated inflammation, an effect demonstrated by in vitro studies. Adapalene decreases formation of comedones and inflammatory and non-inflammatory acne lesions.
Pharmacokinetics: Absorption: Topical bioavailability is low.
Elimination: Topical: Biliary route is major route of excretion.
The elimination half-life is 17.2 ± 10.2 hour.