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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.

DOI:10.1007/BF00315422
PMID:2076729
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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1
Protein binding of oxcarbazepine and its primary active metabolite, 10-hydroxycarbazepine, in patients with trigeminal neuralgia.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。
Eur J Clin Pharmacol. 1990;39(4):413-5. doi: 10.1007/BF00315422.
2
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4
Long-term cohort study comparing medical (oxcarbazepine) and surgical management of intractable trigeminal neuralgia.比较医学治疗(奥卡西平)和手术治疗顽固性三叉神经痛的长期队列研究。
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Gas chromatographic/mass spectrometric assays for oxcarbazepine and its main metabolites, 10-hydroxy-carbazepine and carbazepine-10,11-trans-diol.
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本文引用的文献

1
Carbamazepine therapy in trigeminal neuralgia: clinical effects in relation to plasma concentration.卡马西平治疗三叉神经痛:与血浆浓度相关的临床疗效
Arch Neurol. 1980 Nov;37(11):699-703. doi: 10.1001/archneur.1980.00500600047009.
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Factors influencing simultaneous concentrations of carbamazepine and its epoxide in plasma.影响血浆中卡马西平及其环氧化物同时浓度的因素。
Ther Drug Monit. 1981;3(1):63-70.
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Disposition of the antiepileptic oxcarbazepine and its metabolites in healthy volunteers.抗癫痫药物奥卡西平及其代谢产物在健康志愿者体内的处置情况。
Clin Drug Investig. 2004;24(4):185-203. doi: 10.2165/00044011-200424040-00001.
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Clinical pharmacokinetics of oxcarbazepine.奥卡西平的临床药代动力学
Clin Pharmacokinet. 2003;42(12):1023-42. doi: 10.2165/00003088-200342120-00002.
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Antiepileptic drugs. A review of clinically significant drug interactions.抗癫痫药物。具有临床意义的药物相互作用综述。
Drug Saf. 1993 Sep;9(3):156-84. doi: 10.2165/00002018-199309030-00003.
6
Newer antiepileptic drugs. Towards an improved risk-benefit ratio.新型抗癫痫药物。旨在改善风险效益比。
Drug Saf. 1994 Jul;11(1):37-67. doi: 10.2165/00002018-199411010-00005.
7
Place of newer antiepileptic drugs in the treatment of epilepsy.新型抗癫痫药物在癫痫治疗中的地位。
Drugs. 1993 Dec;46(6):1009-24. doi: 10.2165/00003495-199346060-00006.
8
Oxcarbazepine. A review of its pharmacology and therapeutic potential in epilepsy, trigeminal neuralgia and affective disorders.奥卡西平。对其在癫痫、三叉神经痛和情感障碍方面的药理学及治疗潜力的综述。
Drugs. 1992 Jun;43(6):873-88. doi: 10.2165/00003495-199243060-00007.
Eur J Clin Pharmacol. 1982;22(6):545-51. doi: 10.1007/BF00609629.
4
Use of saliva for monitoring oxcarbazepine therapy in epileptic patients.唾液用于监测癫痫患者的奥卡西平治疗情况。
Eur J Clin Pharmacol. 1986;31(1):91-4. doi: 10.1007/BF00870993.
5
Factors influencing simultaneous concentrations of total and free carbamazepine and carbamazepine-10, 11-epoxide in serum of children with epilepsy.
Ther Drug Monit. 1986;8(3):288-92. doi: 10.1097/00007691-198609000-00009.
6
Trigeminal neuralgia: its treatment with two new carbamazepine analogues.三叉神经痛:两种新型卡马西平类似物对其的治疗
Eur Neurol. 1987;26(2):73-83. doi: 10.1159/000116315.
7
Comparison of oxcarbazepine and carbamazepine: a double-blind study.奥卡西平与卡马西平的比较:一项双盲研究。
Epilepsy Res. 1987 Sep;1(5):284-9. doi: 10.1016/0920-1211(87)90003-9.
8
In vitro lymphocyte proliferation by carbamazepine, carbamazepine-10, 11-epoxide, and oxcarbazepine in the diagnosis of drug-induced hypersensitivity.
J Allergy Clin Immunol. 1988 Jul;82(1):110-5. doi: 10.1016/0091-6749(88)90059-0.
9
Oxcarbazepine (GP 47.680): a possible alternative to carbamazepine?奥卡西平(GP 47.680):卡马西平的一种可能替代药物?
Epilepsia. 1987 Nov-Dec;28(6):693-8. doi: 10.1111/j.1528-1157.1987.tb03702.x.
10
Oxcarbazepine: a new drug in the management of intractable trigeminal neuralgia.奥卡西平:治疗顽固性三叉神经痛的一种新药。
J Neurol Neurosurg Psychiatry. 1989 Apr;52(4):472-6. doi: 10.1136/jnnp.52.4.472.