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三叉神经痛患者中奥卡西平及其主要活性代谢物10-羟基奥卡西平的蛋白结合情况。

Protein binding of oxcarbazepine and its primary active metabolite, 10-hydroxycarbazepine, in patients with trigeminal neuralgia.

作者信息

Patsalos P N, Elyas A A, Zakrzewska J M

机构信息

University Department of Clinical Neurology, National Hospital, London, UK.

出版信息

Eur J Clin Pharmacol. 1990;39(4):413-5. doi: 10.1007/BF00315422.

Abstract

Oxcarbazepine, a new drug with antineuralgic properties has been evaluated in a long-term follow-up of 6 patients (2 males, 4 females; aged 42-77 years; mean 61 years), previously reported on with trigeminal neuralgia. Daily oral oxcarbazepine dose correlated significantly with both total oxcarbazepine (r = 0.851) and 10-OH-carbazepine (r = 0.958) serum concentrations. Mean percent free oxcarbazepine and 10-OH-carbazepine was 41 and 61% respectively and there was no significant difference in binding between male and female patients. Free serum concentrations of oxcarbazepine and 10-OH-carbazepine correlated significantly with total serum oxcarbazepine and 10-OH-carbazepine respectively, indicating that binding capacity of both are essentially constant within the respective ranges of 0.2-11.4 mumol.l-1 and 20-150 mumol.l-1 observed in the present study.

摘要

奥卡西平是一种具有抗神经痛特性的新药,我们对6例患者(2例男性,4例女性;年龄42 - 77岁,平均61岁)进行了长期随访评估,这些患者之前曾报道患有三叉神经痛。每日口服奥卡西平剂量与奥卡西平总血清浓度(r = 0.851)和10 - 羟基奥卡西平血清浓度(r = 0.958)均显著相关。奥卡西平游离百分比均值和10 - 羟基奥卡西平分别为41%和61%,男性和女性患者之间的蛋白结合率无显著差异。奥卡西平游离血清浓度和10 - 羟基奥卡西平分别与奥卡西平总血清浓度和10 - 羟基奥卡西平显著相关,表明在本研究观察到的各自0.2 - 11.4 μmol·L⁻¹和20 - 150 μmol·L⁻¹范围内,两者的蛋白结合能力基本恒定。

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