Yisak W, Farde L, von Bahr C, Nilsson L B, Fredriksson G, Ogenstad S
Department of Clinical Pharmacology, Astra Arcus AB, Södertälje, Sweden.
Psychopharmacology (Berl). 1993;111(1):27-32. doi: 10.1007/BF02257403.
Twelve healthy male volunteers took part in a double-blind randomised cross-over study composed of three treatment sessions: remoxipride 100 mg; remoxipride 100 mg plus biperiden 4 mg; and biperiden 4 mg. Plasma and urine concentrations of remoxipride and biperiden, plasma prolactin levels, salivary flow and adverse events were recorded to assess pharmacodynamic interactions. Remoxipride and biperiden had no effect on each other's plasma concentrations. Biperiden did not affect the urinary recovery or renal clearance of remoxipride. Prolactin levels were unaffected by biperiden but increased following remoxipride administration. Differences in prolactin Cmax and tmax following remoxipride versus concomitant (remoxipride + biperiden) treatment were not statistically significant. However, a slight but statistically significant (P = 0.04) increase in prolactin AUC was observed after concomitant treatment. No significant differences could be observed between the recorded salivary flow in all the treatment sessions. Single doses of remoxipride and biperiden showed no pharmacokinetic or pharmacodynamic interaction.
12名健康男性志愿者参与了一项双盲随机交叉研究，该研究由三个治疗阶段组成：瑞莫必利100毫克；瑞莫必利100毫克加比哌立登4毫克；以及比哌立登4毫克。记录瑞莫必利和比哌立登的血浆及尿液浓度、血浆催乳素水平、唾液流量和不良事件，以评估药效学相互作用。瑞莫必利和比哌立登对彼此的血浆浓度均无影响。比哌立登不影响瑞莫必利的尿回收率或肾脏清除率。催乳素水平不受比哌立登影响，但在给予瑞莫必利后升高。瑞莫必利治疗与联合（瑞莫必利+比哌立登）治疗后催乳素Cmax和tmax的差异无统计学意义。然而，联合治疗后观察到催乳素AUC有轻微但具有统计学意义（P = 0.04）的升高。在所有治疗阶段记录的唾液流量之间未观察到显著差异。单剂量的瑞莫必利和比哌立登未显示药代动力学或药效学相互作用。
