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卡马西平及其代谢产物在神经痛中的浓度-效应关系

Carbamazepine and its metabolites in neuralgias: concentration-effect relations.

作者信息

Moosa R S, McFadyen M L, Miller R, Rubin J

机构信息

Department of Pharmacology, University of Durban-Westville, South Africa.

出版信息

Eur J Clin Pharmacol. 1993;45(4):297-301. doi: 10.1007/BF00265944.

DOI:10.1007/BF00265944
PMID:8299659
Abstract

The aim of this study was to investigate the use of carbamazepine in the treatment of neuralgic pain and to determine a therapeutic plasma concentration range for carbamazepine in neuralgias. The relation between plasma concentration and the response to treatment (reduction in pain) was examined by logistic regression analysis of carbamazepine and its metabolites, the epoxide, the diol, and 2-hydroxycarbamazepine. The plasma concentrations of carbamazepine, the epoxide, and the diol were significantly related to the probability of a 25% reduction in pain. Only carbamazepine was significantly related to the probability of 50% and 75% pain reduction. However, multiple regression analysis with backward elimination of the data showed a significant correlation between both carbamazepine and the epoxide with regard to the probability of 50% and 75% reductions in pain. This confirms the previous finding that the epoxide has antineuralgic properties [Tomson and Bertilsson 1984]. The therapeutic plasma concentration range for carbamazepine in neuralgias, defined as the range of concentrations that would be expected to provide a 25-75% reduction in pain in 50% of patients, was 2-7 micrograms.ml-1 (HPLC) or 5-17 micrograms.ml-1 (EMIT).

摘要

本研究的目的是调查卡马西平在治疗神经痛中的应用,并确定卡马西平在神经痛中的治疗血浆浓度范围。通过对卡马西平及其代谢产物环氧化物、二醇和2-羟基卡马西平进行逻辑回归分析,研究了血浆浓度与治疗反应(疼痛减轻)之间的关系。卡马西平、环氧化物和二醇的血浆浓度与疼痛减轻25%的概率显著相关。只有卡马西平与疼痛减轻50%和75%的概率显著相关。然而,对数据进行向后排除的多元回归分析表明,卡马西平和环氧化物在疼痛减轻50%和75%的概率方面均存在显著相关性。这证实了先前的发现,即环氧化物具有抗神经痛特性[汤姆森和贝蒂尔松,1984年]。神经痛中卡马西平的治疗血浆浓度范围定义为预计能使50%的患者疼痛减轻25%-75%的浓度范围,为2-7微克·毫升-1(高效液相色谱法)或5-17微克·毫升-1(酶放大免疫测定技术)。

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Carbamazepine and its metabolites in neuralgias: concentration-effect relations.卡马西平及其代谢产物在神经痛中的浓度-效应关系
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2
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Estimation of carbamazepine and carbamazepine-10,11-epoxide concentrations in plasma using mathematical equations generated with two carbamazepine immunoassays.应用两种卡马西平免疫分析法建立的数学方程估算血浆中卡马西平和卡马西平-10,11-环氧化物的浓度。
Am J Clin Pathol. 2010 May;133(5):728-36. doi: 10.1309/AJCPFAHVB26VVVTE.
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Potent therapeutic effect of carbamazepine-10,11-epoxide in trigeminal neuralgia.卡马西平-10,11-环氧化物在三叉神经痛中的显著治疗效果。
Arch Neurol. 1984 Jun;41(6):598-601. doi: 10.1001/archneur.1984.04210080006004.
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Determination of total and free plasma carbamazepine concentrations by enzyme multiplied immunoassay: interference with the 10,11-epoxide metabolite.采用酶放大免疫分析法测定血浆中卡马西平的总浓度和游离浓度:与10,11 - 环氧化代谢物的相互干扰
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Measurement of carbamazepine and its epoxide metabolite by high-performance liquid chromatography, and a comparison of assay techniques for the analysis of carbamazepine.
Clin Chem. 1977 Dec;23(12):2283-7.

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本文引用的文献

1
Potent therapeutic effect of carbamazepine-10,11-epoxide in trigeminal neuralgia.卡马西平-10,11-环氧化物在三叉神经痛中的显著治疗效果。
Arch Neurol. 1984 Jun;41(6):598-601. doi: 10.1001/archneur.1984.04210080006004.
2
Factors influencing the relationship between carbamazepine plasma concentration and its clinical effects in patients with epilepsy.影响癫痫患者卡马西平血药浓度与其临床疗效关系的因素。
Clin Neuropharmacol. 1985;8(2):141-9. doi: 10.1097/00002826-198506000-00003.
3
Determination of total and free plasma carbamazepine concentrations by enzyme multiplied immunoassay: interference with the 10,11-epoxide metabolite.
采用酶放大免疫分析法测定血浆中卡马西平的总浓度和游离浓度:与10,11 - 环氧化代谢物的相互干扰
Ther Drug Monit. 1985;7(1):46-50. doi: 10.1097/00007691-198503000-00007.
4
Carbamazepine toxicity: comparison of measurement of drug levels by HPLC and EMIT and model of carbamazepine kinetics.卡马西平毒性:高效液相色谱法和酶放大免疫测定技术测定药物水平的比较及卡马西平动力学模型
J Toxicol Clin Toxicol. 1986;24(4):281-94. doi: 10.3109/15563658608992593.
5
Plasma concentrations of alfentanil required to supplement nitrous oxide anesthesia for general surgery.
Anesthesiology. 1986 Oct;65(4):362-73. doi: 10.1097/00000542-198610000-00004.
6
Carbamazepine drug interactions.卡马西平的药物相互作用。
Ther Drug Monit. 1986;8(3):305-17. doi: 10.1097/00007691-198609000-00012.
7
Clinical pharmacokinetics 1990.临床药代动力学,1990年
Clin Pharmacokinet. 1990 Jan;18(1):1-19. doi: 10.2165/00003088-199018010-00001.
8
Interaction of propoxyphene with carbamazepine.丙氧芬与卡马西平的相互作用。
Lancet. 1977 Sep 3;2(8036):509. doi: 10.1016/s0140-6736(77)91637-3.