Kragballe K, Jansén C T, Geiger J M, Bjerke J R, Falk E S, Gip L, Hjorth N, Lauharanta J, Mork N J, Reunala T
Department of Dermatology, Marselisborg Hospital, Aarhus, Denmark.
Acta Derm Venereol. 1989;69(1):35-40.
Acitretin, the free acid of etretinate, is less lipophilic and has a much shorter terminal half-life than the parent compound. The present double-blind, randomized study compared the therapeutic effectiveness and the tolerability of acitretin (n = 127) and etretinate (n = 41) in psoriasis. Patients were treated with 40 mg daily for the first 4 weeks and with an individually adjusted dose for the subsequent 8 weeks. The average daily doses of acitretin (0.54 mg/kg/day) and etretinate (0.65 mg/kg/day) were similar. The PASI (Psoriasis Area and Severity Index) scores improved in parallel in the 2 treatment groups. At the completion of the study, the PASI score improvement was 75.8% for acitretin and 70.8% for etretinate. Both acitretin and etretinate resulted in mucocutaneous side effects. Assessments of tolerability by investigators and patients showed a statistically significant difference in favour of etretinate. These results demonstrate that acitretin and etretinate have similar therapeutic effectiveness in psoriasis. Although the tolerance to acitretin was lower than to etretinate, acitretin offers the important advantage of a much shorter period of potential teratogenicity and is, therefore, to be preferred in women of childbearing potential.
阿维A,即依曲替酯的游离酸,亲脂性较低,终末半衰期比母体化合物短得多。本双盲随机研究比较了阿维A(n = 127)和依曲替酯(n = 41)治疗银屑病的疗效和耐受性。患者在最初4周每天服用40 mg,随后8周根据个体情况调整剂量。阿维A(0.54 mg/kg/天)和依曲替酯(0.65 mg/kg/天)的平均日剂量相似。两个治疗组的银屑病面积和严重程度指数(PASI)评分平行改善。研究结束时,阿维A组的PASI评分改善率为75.8%,依曲替酯组为70.8%。阿维A和依曲替酯均导致了皮肤黏膜副作用。研究者和患者对耐受性的评估显示,依曲替酯在统计学上有显著优势。这些结果表明,阿维A和依曲替酯在治疗银屑病方面具有相似的疗效。尽管阿维A的耐受性低于依曲替酯,但阿维A具有潜在致畸期短得多的重要优势,因此,对于有生育潜力的女性而言更值得选用。