Vree T B, Janssen T J, Hekster Y A, Termond E F, van de Dries A C, Wijnands W J
Ther Drug Monit. 1986;8(3):297-304. doi: 10.1097/00007691-198609000-00011.
In five cases of carbamazepine (CBZ) intoxication, the time curves of the plasma concentration and of the renal excretion rate of carbamazepine and its metabolites carbamazepine 10,11-epoxide (CBZ-epoxide) and trans-10,11-dihydro-10,11-dihydroxy-CBZ (CBZ-diol) were measured. Pseudo-steady-state or plateau-like plasma concentration-time curves were observed when doses of 12 or 18 g of CBZ were ingested. Hemoperfusion lowers the plasma concentration of CBZ and its metabolites by affecting the half-life. The effect of hemoperfusion is reduced by the continuous absorption from the gastrointestinal tract and redistribution from the tissues. The renal clearances of CBZ and of CBZ-epoxide are low (1 and 8 ml/min, respectively); both are flow dependent. The renal clearance of CBZ-diol is approximately 160-350 ml/min and is independent of the urine flow. Although urine stimulation increases the renal clearance of CBZ by 100%, the overall amount excreted increases only 1-2% of the dose. Protein binding of CBZ is approximately 80%, of CBZ-epoxide 50%, and of CBZ-diol 70%.
在5例卡马西平（CBZ）中毒病例中，测定了卡马西平及其代谢产物卡马西平10,11 - 环氧化物（CBZ - 环氧化物）和反式 - 10,11 - 二氢 - 10,11 - 二羟基 - 卡马西平（CBZ - 二醇）的血浆浓度时间曲线和肾脏排泄率时间曲线。当摄入12克或18克卡马西平时，观察到了伪稳态或类似平台的血浆浓度 - 时间曲线。血液灌流通过影响半衰期降低了卡马西平及其代谢产物的血浆浓度。胃肠道的持续吸收和组织的再分布降低了血液灌流的效果。卡马西平和CBZ - 环氧化物的肾脏清除率较低（分别为1和8毫升/分钟）；两者均与血流有关。CBZ - 二醇的肾脏清除率约为160 - 350毫升/分钟，且与尿流无关。尽管尿液刺激使卡马西平的肾脏清除率提高了100%，但排泄的总量仅增加了剂量的1 - 2%。卡马西平的蛋白结合率约为80%，CBZ - 环氧化物为50%，CBZ - 二醇为70%。
