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儿童微粒体酶诱导:卡马西平治疗对安替比林动力学、6β-羟基皮质醇排泄及血浆γ-谷氨酰转肽酶活性的影响

Microsomal enzyme induction in children: the influence of carbamazepine treatment on antipyrine kinetics, 6 beta-hydroxycortisol excretion and plasma gamma-glutamyltranspeptidase activity.

作者信息

Moreland T A, Park B K, Rylance G W

出版信息

Br J Clin Pharmacol. 1982 Dec;14(6):861-5. doi: 10.1111/j.1365-2125.1982.tb02050.x.

Abstract

1 The influence of carbamazepine (CBZ) therapy on saliva antipyrine kinetics, urinary 6 beta-hydroxycortisol excretion and plasma gamma-glutamyltranspeptidase activity was determined in nine children aged 6-14 years. 2 During 5 weeks of CBZ therapy the mean (+/- s.d.) antipyrine clearance increased from 65 +/- 12 ml kg-1 h-1 to 143 +/- 34 ml kg-1 h-1 (P less than 0.001) and the mean half-life declined from 6.24 +/- 1.23 h to 2.78 +/- 0.59 h (P less than 0.001). The apparent volume of distribution of antipyrine did not change during CBZ treatment. 3 Urinary 6 beta-hydroxycortisol excretion increased markedly during the study period from 5.10 +/- 1.77 micrograms day-1 kg-1 to 17.85 +/- 6.75 micrograms day-1 kg-1 (P less than 0.01). 4 Plasma gamma-glutamyltranspeptidase activity increased in eight out of nine children during CBZ therapy but the change was not statistically significant. 5 CBZ appears to have a marked enzyme inducing effect in young epileptics as indicated by antipyrine kinetics and 6 beta-hydroxycortisol excretion.

摘要
  1. 测定了9名6至14岁儿童服用卡马西平(CBZ)治疗对唾液中安替比林动力学、尿6β-羟基皮质醇排泄及血浆γ-谷氨酰转肽酶活性的影响。2. 在CBZ治疗的5周期间,安替比林清除率均值(±标准差)从65±12 ml·kg⁻¹·h⁻¹增至143±34 ml·kg⁻¹·h⁻¹(P<0.001),平均半衰期从6.24±1.23小时降至2.78±0.59小时(P<0.001)。CBZ治疗期间安替比林的表观分布容积未发生变化。3. 研究期间尿6β-羟基皮质醇排泄显著增加,从5.10±1.77μg·day⁻¹·kg⁻¹增至17.85±6.75μg·day⁻¹·kg⁻¹(P<0.01)。4. CBZ治疗期间9名儿童中有8名血浆γ-谷氨酰转肽酶活性升高,但变化无统计学意义。5. 如安替比林动力学及6β-羟基皮质醇排泄所示,CBZ对年轻癫痫患者似乎有显著的酶诱导作用。

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