Suzuki H, Sawada Y, Sugiyama Y, Iga T, Hanano M
J Pharmacobiodyn. 1985 Jan;8(1):73-6. doi: 10.1248/bpb1978.8.73.
Cimetidine, a histamine H2 receptor antagonist, is known to have some effects on central nervous system, and is reported to emerge in the cerebrospinal fluid (CSF). We evaluated the elimination of cimetidine from CSF by the method of ventriculo-cisternal perfusion in rats. The extraction ratio of cimetidine at the low perfusate concentration (14 nM) was 0.190 +/- 0.023 (n = 3), while that significantly (p less than 0.02) decreased to 0.0916 +/- 0.081 (n = 3) at the high concentration (4 mM). No significant difference was observed in the production rate of CSF between these two concentrations. These findings suggest that cimetidine is excreted from CSF to blood by a saturable transport system.
西咪替丁是一种组胺H2受体拮抗剂，已知对中枢神经系统有一定作用，据报道可出现在脑脊液（CSF）中。我们采用脑室-脑池灌注法在大鼠中评估了西咪替丁从脑脊液中的消除情况。低灌注液浓度（14 nM）时西咪替丁的提取率为0.190±0.023（n = 3），而在高浓度（4 mM）时显著（p<0.02）降至0.0916±0.081（n = 3）。这两种浓度下脑脊液的生成速率未观察到显著差异。这些发现表明西咪替丁通过一个可饱和转运系统从脑脊液排泄到血液中。
