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癫痫患儿的卡马西平和卡马西平-10,11-环氧化物血清浓度

Carbamazepine and carbamazepine-10,11-epoxide serum concentrations in epileptic children.

作者信息

Furlanut M, Montanari G, Bonin P, Casara G L

出版信息

J Pediatr. 1985 Mar;106(3):491-5. doi: 10.1016/s0022-3476(85)80689-2.

DOI:10.1016/s0022-3476(85)80689-2
PMID:3973787
Abstract

Carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZ-epox) steady-state serum concentrations were measured in 82 children who had generalized tonic-clonic, or partial seizures. There was no correlation between a given dose and serum concentrations, whether other anticonvulsant drugs were used or not. Epileptic children receiving polytherapy (CBZ associated with one or more of the following drugs: phenobarbital, primidone, phenytoin, ethosuximide) had significantly different CBZ clearance values and percent CBZ-epox than did patients given CBZ alone. Even though given lower doses, girls had higher CBZ concentrations and lower CBZ clearance values than did boys. Older girls had lower serum concentrations of CBZ-epox than did younger girls. Seizure-free children had higher CBZ serum levels and lower CBZ clearance values than did those with uncontrolled seizures. The percentage of CBZ-epox in children with uncontrolled seizures was significantly higher than in children without seizures. These data indicate that serum levels of CBZ and CBZ-epox correlate more with factors such as associated drugs, age, and sex than with administered dose. Therefore, CBZ serum level monitoring represents an essential means of individualization of anticonvulsant drug therapy.

摘要

对82例患有全身性强直阵挛发作或部分性发作的儿童测定了卡马西平(CBZ)和卡马西平 - 10,11 - 环氧化物(CBZ - epox)的稳态血清浓度。无论是否使用其他抗惊厥药物,给定剂量与血清浓度之间均无相关性。接受联合治疗(CBZ与以下一种或多种药物联合使用:苯巴比妥、扑米酮、苯妥英、乙琥胺)的癫痫儿童与单独使用CBZ的患者相比,其CBZ清除率值和CBZ - epox百分比有显著差异。尽管女孩服用的剂量较低,但其CBZ浓度较高,CBZ清除率值较低。年龄较大的女孩的CBZ - epox血清浓度低于年龄较小的女孩。无癫痫发作的儿童的CBZ血清水平较高,CBZ清除率值较低,而癫痫未得到控制的儿童则相反。癫痫未得到控制的儿童中CBZ - epox的百分比显著高于无癫痫发作的儿童。这些数据表明,CBZ和CBZ - epox的血清水平与联合用药、年龄和性别等因素的相关性比与给药剂量的相关性更大。因此,监测CBZ血清水平是抗惊厥药物治疗个体化的重要手段。

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