Tateishi T, Ohashi K, Sudo T, Sakamoto K, Fujimura A, Ebihara A
Department of Clinical Pharmacology and Therapeutics, Jichi Medical School, Tochigi, Japan.
J Clin Pharmacol. 1993 Aug;33(8):738-40. doi: 10.1002/j.1552-4604.1993.tb05616.x.
To evaluate the influence of nifedipine on the pharmacokinetics and the pharmacodynamics of diltiazem, five healthy subjects received 60 mg diltiazem orally on two occasions, diltiazem alone or after nifedipine pretreatment (10 mg three times daily for 3 days). After nifedipine pretreatment, the maximum concentration (Cmax) of diltiazem was increased and the time of Cmax was shortened, and the area under the concentration curve (AUC) tended to be increased. Although heart rate was increased, the corrected PQ interval tended to be prolonged after the nifedipine pretreatment. Both a decreased hepatic clearance and an increased bioavailability of diltiazem probably accounts for the increase in the Cmax and AUC of diltiazem after nifedipine pretreatment, and that might affect the pharmacodynamics of diltiazem.
为评估硝苯地平对地尔硫䓬药代动力学和药效动力学的影响,5名健康受试者分两次口服60mg地尔硫䓬,一次单独服用地尔硫䓬,另一次在硝苯地平预处理后(每日3次,每次10mg,共3天)服用。硝苯地平预处理后,地尔硫䓬的最大浓度(Cmax)升高,达峰时间缩短,浓度曲线下面积(AUC)有增加趋势。虽然心率加快,但硝苯地平预处理后校正PQ间期有延长趋势。地尔硫䓬肝清除率降低和生物利用度增加可能是硝苯地平预处理后地尔硫䓬Cmax和AUC增加的原因,这可能会影响地尔硫䓬的药效动力学。