Treatment of atopic dermatitis with pimecrolimus - impact on quality of life.

Allergy-Center-Charité (CCM), Department of Dermatology and Allergy, Charité - Universitätsmedizin Berlin Germany.
Therapeutics and Clinical Risk Management 01/2008; 3(6):1021-6.
Source: PubMed

ABSTRACT Atopic dermatitis (AD) is a multifactorial chronic remittent skin disease which requires long-term treatment. Pimecrolimus cream 1% is a nonsteroid selective inhibitor of inflammatory cytokines and effective in the treatment of AD. Various clinical trials have shown its long-term safety and efficacy in pediatric and adult patients suffering from mild to moderate AD. In this article we discuss data which has assessed the impact of AD on the patient's quality of life, and the consequent role of topical anti-inflammatory therapy for long-term AD treatment.

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    ABSTRACT: For treatment of skin diseases with topical drugs, penetration of the agents into the relevant layers of the skin is required. Permeation through the skin should, however, be kept to a minimum, in order to avoid the risk of systemic side effects. Here we compared the in vitro skin penetration and permeation of two novel drugs used in the therapy of atopic eczema (pimecrolimus and tacrolimus) and three representative corticosteroids (betamethasone-17-valerate, clobetasol-17-propionate, and diflucortolon-21-valerate). Drug concentrations of pimecrolimus and corticosteroids in human skin were found to be in the same order of magnitude. Permeation of pimecrolimus through human skin was, however, lower by factors of 70-110 as compared to the steroids. When pimecrolimus was compared with tacrolimus in human, pig, or rat skin, similar concentrations of the two compounds were measured in the skin, whereas permeation of pimecrolimus through skin was consistently lower by factors of 9-10. Lipophilicity was found to be highest for pimecrolimus, its octanol-water distribution coefficient being higher by factors of 8 and 25-450 than that of tacrolimus and the corticosteroids, respectively. The low permeation of pimecrolimus may be explained by its higher lipophilicity (compared to tacrolimus and the corticosteroids) and higher molecular weight (compared to steroids). In conclusion, pimecrolimus appears to have a favourable skin penetration/permeation profile, featuring a low degree of percutaneous absorption.
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