儿童体内的卡马西平10,11 - 环氧化物
Carbamazepine 10,11-epoxide in children.
作者信息
Rylance G W, Edwards C, Gard P R
出版信息
Br J Clin Pharmacol. 1984 Dec;18(6):935-9. doi: 10.1111/j.1365-2125.1984.tb02566.x.
Concentrations of carbamazepine (CBZ) and its 10,11-epoxide metabolite (CBZ-E) were measured in simultaneously collected plasma and mixed saliva samples from 15 children (aged 1-13 years). Saliva concentrations of CBZ and CBZ-E were measured in hourly samples taken from six of these children during dose intervals whilst on different dose or dose-frequency regimens. Saliva and plasma CBZ (r = 0.91; P less than 0.001) and CBZ-E (r = 0.91; P less than 0.001) concentrations were significantly correlated. The mean +/- s.d. steady state CBZ-E/CBZ concentration ratio in the six children was 0.40 +/- 0.21 and was similar at all times within the 12 h dose interval. The mean +/- s.d. percentage fluctuation of the combined CBZ + CBZ-E (103.0 +/-28.9) was significantly less than that of CBZ-E (145.5 +/- 52.8) but not CBZ (109.6 +/- 31.1). If CBZ and CBZ-E have equipotent anticonvulsant activity in man, the contribution of CBZ-E approximates to 30% of total anticonvulsant effect in children taking CBZ alone.
在同时采集的15名儿童（年龄1至13岁）的血浆和混合唾液样本中，测定了卡马西平（CBZ）及其10,11 - 环氧化物代谢物（CBZ - E）的浓度。在不同剂量或给药频率方案下，对其中6名儿童在给药间隔期间每小时采集的样本测定了CBZ和CBZ - E的唾液浓度。唾液和血浆中CBZ（r = 0.91；P < 0.001）和CBZ - E（r = 0.91；P < 0.001）浓度显著相关。6名儿童中CBZ - E/CBZ浓度比值的平均值±标准差为0.40±0.21，在12小时给药间隔内的所有时间均相似。CBZ + CBZ - E组合的平均±标准差波动百分比（103.0±28.9）显著低于CBZ - E（145.5±52.8），但不低于CBZ（109.6±31.1）。如果CBZ和CBZ - E在人体中具有等效的抗惊厥活性，那么在单独服用CBZ的儿童中，CBZ - E对总抗惊厥作用的贡献约为30%。
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