Gammans R E, Pfeffer M, Westrick M L, Faulkner H C, Rehm K D, Goodson P J
Pharmacotherapy. 1987;7(3):72-9. doi: 10.1002/j.1875-9114.1987.tb03521.x.
Simultaneous administration of cimetidine and many benzodiazepine anxiolytics has resulted in decreased body clearance and marked prolongation of the half-life of these agents. The pharmacokinetic interaction of buspirone, a new nonbenzodiazepine anxiolytic, and cimetidine was studied in 10 healthy male volunteers. Each received, in order, buspirone 45 mg/day (days 1-7), no drug (days 8-14), cimetidine 1 g/day (days 15-21), buspirone 45 mg/day plus cimetidine 1 g/day (days 22-28), and cimetidine 1 g/day (days 29-31). Buspirone and 1-pyrimidinyl piperazine (1-PP), an active metabolite, pharmacokinetics, urinary excretion of cimetidine, a manual dexterity test, the Stroop color-word interference test, and a visual analog mood scale were evaluated on each treatment. There were no significant (p greater than 0.05) differences among treatments for any measurement except for a slight (31%) but significant (p less than 0.05) increase in the 1-PP Cmax value. These results suggest that within the normal therapeutic dosage ranges for both drugs, it is unlikely that a clinically significant interaction between them will occur.
西咪替丁与多种苯二氮䓬类抗焦虑药同时使用已导致这些药物的体内清除率降低,半衰期显著延长。在10名健康男性志愿者中研究了新型非苯二氮䓬类抗焦虑药丁螺环酮与西咪替丁的药代动力学相互作用。每位志愿者依次接受以下治疗:丁螺环酮45毫克/天(第1 - 7天)、不服用药物(第8 - 14天)、西咪替丁1克/天(第15 - 21天)、丁螺环酮45毫克/天加西咪替丁1克/天(第22 - 28天)以及西咪替丁1克/天(第29 - 31天)。对每种治疗方案评估了丁螺环酮及其活性代谢物1 - 嘧啶基哌嗪(1 - PP)的药代动力学、西咪替丁的尿排泄、一项手工灵巧度测试、Stroop颜色 - 文字干扰测试以及视觉模拟情绪量表。除1 - PP的Cmax值有轻微(31%)但显著(p < 0.05)升高外,各治疗方案之间的任何测量结果均无显著(p > 0.05)差异。这些结果表明,在两种药物的正常治疗剂量范围内,它们之间不太可能发生具有临床意义的相互作用。