Gaska J A, Tietze K J, Rocci M L, Vlasses P H
Philadelphia College of Pharmacy and Science, Pennsylvania 19104-4495.
J Clin Pharmacol. 1991 Jul;31(7):668-72. doi: 10.1002/j.1552-4604.1991.tb03754.x.
The comparative effects of continuous versus intermittent cimetidine infusion on theophylline pharmacokinetics were evaluated in 12 nonsmoking healthy male volunteers. Each subject received aminophylline 0.9 mg/kg/hr over 6 hours alone (control) and in random order at 1 week intervals, in combination with intermittent cimetidine (300 mg IV over 15 minutes every 6 hours) and continuous cimetidine (50 mg/hr IV) infusions. Both cimetidine regimens were administered for a total of 50 hours. Serial plasma samples were obtained and assayed for theophylline by HPLC. No significant differences existed in mean theophylline clearance and mean volume of distribution among control, intermittent or continuous cimetidine regimens; the power was greater than 80% to detect a 30% change in clearance. Only a minor difference in theophylline half-life between control and continuous cimetidine infusion (7.59 +/- 2.52 vs. 9.05 +/- 3.17 hr; P less than .05) was observed. These findings do not support a clinically significant interaction between IV aminophylline and cimetidine administered IV either as a low dose continuous infusion or as an intermittent infusion.
在12名不吸烟的健康男性志愿者中评估了西咪替丁持续输注与间歇输注对茶碱药代动力学的比较效应。每位受试者在单独接受氨茶碱0.9mg/kg/小时，持续6小时（对照）后，以随机顺序，每隔1周接受一次，同时联合间歇西咪替丁（每6小时静脉注射300mg，持续15分钟）和持续西咪替丁（50mg/小时静脉输注）。两种西咪替丁给药方案均持续给药50小时。采集系列血浆样本，并用高效液相色谱法测定茶碱。对照、间歇或持续西咪替丁给药方案之间的平均茶碱清除率和平均分布容积无显著差异；检测清除率30%变化的效能大于80%。仅观察到对照与持续西咪替丁输注之间茶碱半衰期存在微小差异（7.59±2.52对9.05±3.17小时；P<0.05）。这些发现不支持静脉注射氨茶碱与静脉注射西咪替丁（无论是低剂量持续输注还是间歇输注）之间存在具有临床意义的相互作用。
