Schneider D, Gannon R, Sweeney K, Shore E
Hartford Hospital, Department of Pharmacy Services, CT 06115.
Chest. 1990 Jan;97(1):84-7. doi: 10.1378/chest.97.1.84.
To determine a change in theophylline pharmacokinetics during concomitant thiabendazole or mebendazole therapy, we studied six normal, healthy male volunteers. Aminophylline was administered intravenously, followed by a 30-h blood sampling period. Subjects were randomized to receive thiabendazole or mebendazole, then crossed over to receive the other therapy. Theophylline concentrations were measured utilizing an HPLC technique and a one-compartment model was fit to the data. Theophylline pharmacokinetic parameters were significantly different during thiabendazole therapy. Mean theophylline half-life increased, clearance decreased and elimination rate constant decreased. Two subjects experienced severe nausea and vomiting during thiabendazole therapy. There were no significant differences in theophylline pharmacokinetic parameters during mebendazole therapy. Thiabendazole administration results in a significant decrease in theophylline clearance and beta elimination rate constant. The theophylline half-life increased significantly. Concomitant administration of theophylline and thiabendazole resulted in severe nausea and vomiting. Mebendazole administration did not seem to alter theophylline pharmacokinetics.
为了确定在同时使用噻苯达唑或甲苯达唑治疗期间茶碱药代动力学的变化，我们研究了6名正常、健康的男性志愿者。静脉注射氨茶碱，随后进行30小时的血样采集。受试者被随机分为接受噻苯达唑或甲苯达唑治疗，然后交叉接受另一种治疗。使用高效液相色谱技术测量茶碱浓度，并对数据拟合单室模型。在噻苯达唑治疗期间，茶碱药代动力学参数有显著差异。茶碱平均半衰期延长，清除率降低，消除速率常数降低。两名受试者在噻苯达唑治疗期间出现严重恶心和呕吐。在甲苯达唑治疗期间，茶碱药代动力学参数无显著差异。服用噻苯达唑导致茶碱清除率和β消除速率常数显著降低。茶碱半衰期显著延长。同时服用茶碱和噻苯达唑导致严重恶心和呕吐。服用甲苯达唑似乎并未改变茶碱的药代动力学。
