不同稳态血清苯妥英浓度下癫痫患者示踪剂量苯妥英消除率。
Rate of elimination of tracer doses of phenytoin at different steady-state serum phenytoin concentrations in epileptic patients.
机构信息
Department of Clinical Pharmacology, St Bartholomew's Hospital, London.
出版信息
Br J Clin Pharmacol. 1974 Apr;1(2):155-61. doi: 10.1111/j.1365-2125.1974.tb00225.x.
1 Serum phenytoin concentration, the serum half-life of a tracer dose of carbon-labelled phenytoin, and the ratio of the major metabolite of phenytoin to unchanged drug in urine (p-HPPH: DPH ratio) were measured in epileptic patients on chronic anticonvulsant therapy. 2 A significant correlation was found between serum phenytoin concentration and half-life, the slope of the regression line being dose dependent. 3 A significant negative correlation was found between serum phenytoin concentration and p-HPPH: DPH ratio. 4 Increasing the daily dose of phenytoin lead to a lengthening of the half-life and a reduction in the p-HPPH: DPH ratio. The reverse occurred on lowering the dose. 5 These changes indicate that phenytoin hydroxylation is saturable. 6 Difficulty in achieving a stable serum phenytoin concentration within the therapeutic range may result.
在接受慢性抗惊厥治疗的癫痫患者中，测定了血清苯妥英钠浓度、放射性标记苯妥英的血清半衰期、以及尿中苯妥英主要代谢物与未改变药物的比值（p-HPPH:DPH 比值）。
发现血清苯妥英钠浓度与半衰期之间存在显著相关性，回归线斜率呈剂量依赖性。
发现血清苯妥英钠浓度与 p-HPPH:DPH 比值之间存在显著负相关。
增加苯妥英钠的日剂量会导致半衰期延长和 p-HPPH:DPH 比值降低。降低剂量则反之。
这些变化表明苯妥英羟基化是饱和的。
可能导致难以在治疗范围内达到稳定的血清苯妥英浓度。
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