Furst D E, Gupta N, Paulus H E
J Clin Invest. 1977 Jul;60(1):32-42. doi: 10.1172/JCI108766.
To evaluate the contribution of genetic influences on the individual variation in plateau serum salicylate levels, salicylate metabolism was studied in seven pairs of identical and six pairs of fraternal twins.Under the conditions of this study, after a single i.v. dose (40 mg/kg) of sodium salicylate, the serum salicylate concentration versus time curve approximated a straight line on linear coordinates (appeared approximately zero order). The slopes of the decay curves ranged between 0.64 and 1.02. The intrapair variation for identical twin pairs was significantly less than for fraternal twin pairs (P = 0.044). Likewise pleateau serum salicylic acid concentrations (milligrams/deciliter) and total salicylic acid excretion rate after multiple doses demonstrated significantly less intrapair variation for identical twins than for fraternal twins (P = 0.043 and 0.006). Plateau salicylurate excretion (milligram/kilogram per hour) differences after multiple dosing had a P = 0.067. Michaelis-Menton constant for salicylurate formation and hours to 50% excretion after the i.v. dose were not different when comparing identical and nonidentical twins. Salicylurate formation rates were increased after 3 days of oral therapy, and this induction phenomenon may account for much of the apparent discrepancy between genetic influences on salicylurate formation rates observed after single and multiple dose salicylate administration. This study suggests that the plateau concentration of serum salicylate varies among individuals given the same weight-adjusted dose in part because of genetically determined variations in their metabolism of salicylate.
为评估遗传因素对高原血清水杨酸盐水平个体差异的影响,对7对同卵双胞胎和6对异卵双胞胎的水杨酸盐代谢进行了研究。在本研究条件下,静脉注射单剂量(40mg/kg)水杨酸钠后,血清水杨酸盐浓度-时间曲线在直角坐标上近似一条直线(近似为零级动力学)。衰减曲线的斜率在0.64至1.02之间。同卵双胞胎对之间的配对内差异显著小于异卵双胞胎对(P = 0.044)。同样,多次给药后,同卵双胞胎的高原血清水杨酸浓度(毫克/分升)和总水杨酸排泄率的配对内差异也显著小于异卵双胞胎(P = 0.043和0.006)。多次给药后高原水杨尿酸排泄(毫克/千克每小时)差异的P值为0.067。比较同卵和非同卵双胞胎时,水杨尿酸形成的米氏常数和静脉注射给药后至50%排泄的时间并无差异。口服治疗3天后水杨尿酸形成率增加,这种诱导现象可能是单次和多次剂量水杨酸盐给药后观察到的遗传因素对水杨尿酸形成率影响存在明显差异 的主要原因。本研究表明,给予相同体重调整剂量后,个体间血清水杨酸盐的高原浓度存在差异,部分原因是其水杨酸盐代谢的遗传决定差异。