Adapalene
Encyclopedia
Adapalene is a third-generation topical retinoid
primarily used in the treatment of mild-moderate acne
and is also used (off-label
) to treat keratosis pilaris
as well as other skin conditions.
, adapalene is available under the brand name Differin in three different preparations: 0.1% cream, 0.1% gel, and 0.3% gel. As of June 2010, a 0.1% gel is also available under the generic name Teva. In Europe
, only the 0.1% cream and 0.1% gel are available. In Pakistan
, adapalene is available under the brand names Pimpal by Brookes Pharmaceuticals,and Gallet by Pharma Health Pakistan, Pimpal is in the form of 0.1% gel where as gallet is in cream. In India it is available under the trade name
Adelene with 0.1 % Adapalene and 1 % Clindamycin phosphate.
, although adverse effects are also increased. Application of adapalene gel to the skin 3–5 minutes before application of clindamycin enhances penetration of clindamycin into the skin, which may enhance the overall efficacy of the treatment as compared to clindamycin alone.
Unlike tretinoin
(Retin-A), adapalene has also been shown to retain its efficacy when applied at the same time as benzoyl peroxide
due to its more stable chemical structure.
, keratinization, and inflammatory processes. It has both exfoliating and anti-inflammatory effects. "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."
DIFFERIN®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."
Retinoid
The retinoids are a class of chemical compounds that are related chemically to vitamin A. Retinoids are used in medicine, primarily due to the way they regulate epithelial cell growth....
primarily used in the treatment of mild-moderate acne
Acne vulgaris
Acne vulgaris is a common human skin disease, characterized by areas of skin with seborrhea , comedones , papules , pustules , Nodules and possibly scarring...
and is also used (off-label
Off-label use
Off-label use is the practice of prescribing pharmaceuticals for an unapproved indication or in an unapproved age group, unapproved dose or unapproved form of administration...
) to treat keratosis pilaris
Keratosis pilaris
Keratosis pilaris is a common, autosomal dominant, genetic follicular condition that is manifested by the appearance of rough bumps on the skin...
as well as other skin conditions.
History
Adapalene was approved in 1996 by the U.S. Food and Drug Administration (FDA) for use in the treatment of acne.Available forms
In the United StatesUnited States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
, adapalene is available under the brand name Differin in three different preparations: 0.1% cream, 0.1% gel, and 0.3% gel. As of June 2010, a 0.1% gel is also available under the generic name Teva. In Europe
Europe
Europe is, by convention, one of the world's seven continents. Comprising the westernmost peninsula of Eurasia, Europe is generally 'divided' from Asia to its east by the watershed divides of the Ural and Caucasus Mountains, the Ural River, the Caspian and Black Seas, and the waterways connecting...
, only the 0.1% cream and 0.1% gel are available. In Pakistan
Pakistan
Pakistan , officially the Islamic Republic of Pakistan is a sovereign state in South Asia. It has a coastline along the Arabian Sea and the Gulf of Oman in the south and is bordered by Afghanistan and Iran in the west, India in the east and China in the far northeast. In the north, Tajikistan...
, adapalene is available under the brand names Pimpal by Brookes Pharmaceuticals,and Gallet by Pharma Health Pakistan, Pimpal is in the form of 0.1% gel where as gallet is in cream. In India it is available under the trade name
Adelene with 0.1 % Adapalene and 1 % Clindamycin phosphate.
Drug interactions
Adapalene has been shown to enhance the efficacy of topical clindamycinClindamycin
Clindamycin rINN is a lincosamide antibiotic. It is usually used to treat infections with anaerobic bacteria but can also be used to treat some protozoal diseases, such as malaria...
, although adverse effects are also increased. Application of adapalene gel to the skin 3–5 minutes before application of clindamycin enhances penetration of clindamycin into the skin, which may enhance the overall efficacy of the treatment as compared to clindamycin alone.
Unlike tretinoin
Tretinoin
Tretinoin is the acid form of vitamin A and is also known as all-trans retinoic acid or ATRA. It is a drug commonly used to treat acne vulgaris and keratosis pilaris. It is available as a cream or gel...
(Retin-A), adapalene has also been shown to retain its efficacy when applied at the same time as benzoyl peroxide
Benzoyl peroxide
Benzoyl peroxide is an organic compound in the peroxide family. It consists of two benzoyl groups bridged by a peroxide link. Its structural formula is [C6H5C]2O2. It is one of the most important organic peroxides in terms of applications and the scale of its production...
due to its more stable chemical structure.
Pharmacodynamics
Adapalene in small concentrations is a moderator of cellular differentiationCellular differentiation
In developmental biology, cellular differentiation is the process by which a less specialized cell becomes a more specialized cell type. Differentiation occurs numerous times during the development of a multicellular organism as the organism changes from a simple zygote to a complex system of...
, keratinization, and inflammatory processes. It has both exfoliating and anti-inflammatory effects. "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 DIFFERIN® Cream through human skin is low. In a pharmacokinetic study with six acne patients treated once daily for 5 days with 2 grams ofDIFFERIN®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."