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酒石酸麦角胺在丛集性头痛患者中的最佳给药途径。一项药代动力学研究。

Optimal routes of administration of ergotamine tartrate in cluster headache patients. A pharmacokinetic study.

作者信息

Ekbom K, Krabbe A E, Paalzow G, Paalzow L, Tfelt-Hansen P, Waldenlind E

出版信息

Cephalalgia. 1983 Mar;3(1):15-20. doi: 10.1046/j.1468-2982.1983.0301015.x.

Abstract

Bioavailability and rate of absorption of ergotamine were studied in eight cluster headache patients outside attacks. In a cross-over design, approximately 2 mg ergotamine tartrate was administered as effervescent tablets, suppositories, and from an inhalation device, with 0.25 mg intravenously as the reference. Ergotamine in plasma was measured by high performance liquid chromatography with fluorescence detection from 5 to 420 min. For all three routes of administration, a similar low (0.5-4.2%) bioavailability of ergotamine was estimated. Only inhalation of ergotamine resulted in early (at 5 min) peak concentrations of ergotamine in plasma and is therefore most likely to relieve the short-lived attacks of cluster headache. The inhalation route for ergotamine poses problems, however, and we suggest ways of improving the inhalation device.

摘要

在八名非发作期丛集性头痛患者中研究了麦角胺的生物利用度和吸收速率。采用交叉设计,分别以泡腾片、栓剂和吸入装置给予约2mg酒石酸麦角胺,静脉注射0.25mg作为对照。采用高效液相色谱荧光检测法在5至420分钟内测定血浆中的麦角胺。对于所有三种给药途径,估计麦角胺的生物利用度都较低(0.5-4.2%)。只有吸入麦角胺会导致血浆中麦角胺在早期(5分钟时)达到峰值浓度,因此最有可能缓解丛集性头痛的短暂发作。然而,麦角胺的吸入途径存在问题,我们提出了改进吸入装置的方法。

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