Acitretin in Dermatology: A Review

July 2011 | Volume 10 | Issue 7 | Original Article | 772 | Copyright © 2011

Abstract

Introduction: Acitretin is a systemic retinoid drug used in the treatment of severe psoriasis. It has also been used for a spectrum of other difficult-to-treat dermatoses, including hyperkeratotic and inflammatory dermatoses and non-melanoma skin cancers. Here we review the available data regarding both FDA-approved and off-label uses of acitretin, clinically relevant adverse events, precautions and monitoring.
Methods: A PubMed literature search was conducted utilizing the search term "acitretin," which yielded 714 hits. Results were further limited to English language clinical trials in human subjects. Of 78 articles evaluated for relevance, 60 were included for review.
Results: Acitretin is effective as monotherapy and in multidrug therapeutic regimens for the treatment of psoriasis and other hyperkeratotic and inflammatory disorders, as well as for malignancy chemoprevention. Its use is limited by its teratogenic potential and other adverse effects, including mucocutaneous effects and hepatotoxicity. Potential adverse effects may be reduced or avoided by using lower doses of acitretin or in combination with other therapies.
Limitations: The reviewed studies include many small trials and case reports of the use of acitretin for psoriasis. Studies of acitretin therapy for the treatment of other cutaneous disorders are limited.
Conclusion: Acitretin is a beneficial treatment for psoriasis, and should be considered when not contraindicated. Particularly when used in combination with ultraviolet (UV) phototherapy, is a safe and cost effective therapeutic strategy.

J Drugs Dermatol.2011;10(7):772-782.

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INTRODUCTION

Acitretin is a second-generation aromatic retinoid. It is an active metabolite of the precursor drug, etretinate (Tegison, Hoffmann-La Roche, Nutley, NJ), which was widely used in the United States (U.S.) as a systemic psoriasis therapy until 1998 when it was withdrawn from the market and replaced by acitretin. Etretinate is 50 times more lipophilic than acitretin and is sequestered in fatty tissues, leading to a mean terminal half-life of 120 days.1-3 Compared to etretinate, acitretin has a wider therapeutic index and improved pharmacokinetic profile. It is relatively water-soluble and has a half-life of 50 to 60 days. Etretinate and acitretin have nearly identical therapeutic profiles, with similar levels of efficacy and toxicity. Acitretin is effective for the treatment of psoriasis and a number of other keratinizing disorders.4

Acitretin is approved by the U.S. Food and Drug Administration (FDA) for the treatment of severe recalcitrant psoriasis. It is useful as monotherapy and has increased efficacy when used in combination with other topical and systemic therapies, as well as with phototherapy. Acitretin has also been used off-label in the treatment of severe keratinization disorders and other dermatoses, but the data are limited.5,6 We reviewed the current literature including the safety and efficacy of acitretin in clinical trials for the treatment of psoriasis and other disorders of keratinization, inflammatory disorders and in the chemoprevention of malignancies.

METHODS

We conducted a PubMed literature search for the term "acitretin" which yielded 714 results. The results were further limited to English language, clinical trials in human subjects. The 78 articles returned were evaluated for relevance and 60 were included in this review (Figure 1). Here, we present clinical efficacy data for acitretin as a therapy for psoriasis, other keratinization and inflammatory disorders and the chemoprevention of malignancy, as well as safety, tolerability, dosing and cost.

RESULTS

Pharmacokinetics

Acitretin is an orally administered therapy with variable absorption, which increases with high-fat meals. It has a bioavailability of approximately 60 percent, with 99 percent of the circulating

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