Hoffman W H, Miceli J N
Department of Pediatrics, Wayne State University School of Medicine, Detroit, Mich.
Dev Pharmacol Ther. 1988;11(2):73-81. doi: 10.1159/000457669.
The pharmacokinetics of propylthiouracil (PTU) was studied in 7 patients having Graves' disease when they were hyperthyroid and then again when they were euthyroid. Two additional euthyroid patients were also studied. The t1/2, Ke, Ka, apparent Vd, AUC and clearance were calculated. Serum T3 and T4 were also measured. PTU had an immediate effect in reducing T3 levels. Although there were intraindividual variations, the mean PTU elimination half-time did not change from the hyperthyroid state (1.47 h) to the euthyroid state (1.53 h). The mean Ka when hyperthyroid (2.12 h-1) was significantly increased (p less than 0.005) compared to when euthyroid (1.00 h-1). The calculated kinetic information indicates that the disposition of PTU in children is similar to that reported in adults.
对7例格雷夫斯病患者在甲状腺功能亢进期和甲状腺功能正常期进行了丙硫氧嘧啶(PTU)的药代动力学研究。另外还研究了2例甲状腺功能正常的患者。计算了t1/2、Ke、Ka、表观分布容积、AUC和清除率。同时测定了血清T3和T4。PTU对降低T3水平有即刻作用。尽管存在个体差异,但PTU消除半衰期的均值从甲状腺功能亢进状态(1.47小时)到甲状腺功能正常状态(1.53小时)并未改变。甲状腺功能亢进时的平均Ka(2.12 h-1)与甲状腺功能正常时(1.00 h-1)相比显著升高(p<0.005)。计算得到的动力学信息表明,PTU在儿童体内的处置情况与成人报道的相似。