DiGiovanna J J, Zech L A, Ruddel M E, Gantt G, Peck G L
Dermatology Branch, National Institutes of Health, Bethesda, MD 20892.
Arch Dermatol. 1989 Feb;125(2):246-51. doi: 10.1001/archderm.125.2.246.
In 47 patients who received long-term etretinate therapy, we measured serum etretinate concentrations from one to 244 weeks after the discontinuation of therapy. The earliest posttreatment, nondetectable serum concentration of etretinate was observed at five weeks after treatment. Detectable serum concentrations (0.05 to 1.2 micrograms/dL) were observed more than two years (108, 111, 131, 136, and 150 weeks) following the discontinuation of therapy. Sequential serum concentrations obtained on eight individual patients were used to determine half-lives for this late-phase elimination. The median half-life for the 12 curves obtained was 12.5 weeks (range, 5.3 to 24.8 weeks). Since etretinate is stored in fat, we compared each patient's deviation from ideal body weight as a measure of excess body fat with various pharmacokinetic factors of etretinate elimination. Overweight patients tended to have slower elimination, maintain higher serum concentrations, and clear etretinate later.
在47例接受长期阿维A酯治疗的患者中,我们在治疗中断后1至244周测量了血清阿维A酯浓度。治疗后最早在治疗后5周观察到血清阿维A酯浓度低于检测限。在治疗中断两年多(108、111、131、136和150周)后观察到可检测的血清浓度(0.05至1.2微克/分升)。利用8例个体患者的连续血清浓度来确定这种晚期消除的半衰期。所获得的12条曲线的中位半衰期为12.5周(范围为5.3至24.8周)。由于阿维A酯储存在脂肪中,我们将每位患者相对于理想体重的偏差作为过量体脂的指标,与阿维A酯消除的各种药代动力学因素进行比较。超重患者往往消除较慢,维持较高的血清浓度,且阿维A酯清除较晚。