Summary:
Adapalene is a useful new drug in the treatment of acne due to its tolerance and stability of effect.
It is suitable in combination with other local and systemic drugs, e.g. antimicrobial preparations or
benzoyl peroxide. After combined treatment and administration of adapalene alone the patients
collaboration improves due to more comfortable use and much weaker irritant potential of this new
substance. A number of authors confirm the reduced skin irritation.
In the treatment of skin diseases some natural and synthetic retinoids are used. E.g. retinoic acid
and one of its isomers, 13-cis retinoic acid (13-cis RA), are used as local and systemic drugs in acne.
Considerable skin irritation caused by retinoic acid is the reasonwhy retinoids with a better relation
between the therapeutic effect and side effects are sought. A modern chemical and pharmacological
programme led to the discovery of a new synthetic retinoid, adapalene, which is effective and
tolerated better by patients than retinoic acid.
Pharmacological studies in vitro and in vivo provided evidence of the activity of adapalene as
regards proliferation and differentiation of cells and tissues. Adapelene has also an anti-inflammatory
effect which is due to its anti-AP1 action. It enters selective interactions with nuclear receptors
RAR and RAR and its effect on proliferation and differentiation can be blocked by the antagonist
ofRAR-.AsRAR are not expressed inhumankeratinocytes, it is certain that the effect of adapalene
on this main cellular type of epidermis is mediated by interaction with RAR. The unique pharmacological
properties of adapalene explain - due to the improved tolerance - its better therapeutic
effect as compared with tretinoin.
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