Optimal Routes of Administration of Ergotamine Tartrate in Cluster Headache Patients. A Pharmacokinetic Study*

Optimal Routes of Administration of Ergotamine Tartrate in Cluster Headache Patients. A Pharmacokinetic Study*
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丛集性头痛患者酒石酸麦角胺的最佳给药途径。

DOI:
10.1046/j.1468-2982.1983.0301015.x
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发表时间:
1983
期刊:
影响因子:
4.9
通讯作者:
E. Waldenlind
E. Waldenlind
中科院分区:
医学2区
文献类型:
--
作者:
K. Ekbom;A. Krabbe;G. Paalzow;L. Paalzow;P. Tfelt;E. Waldenlind

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在八名丛集性头痛发作之外的患者中研究了麦角胺的生物利用度和吸收率。在交叉设计中,大约 2 mg 酒石酸麦角胺以泡腾片、栓剂和吸入装置的形式给药,并以 0.25 mg 静脉注射作为参考。通过高效液相色谱法和荧光检测器在 5 至 420 分钟内测量血浆中的麦角胺。对于所有三种给药途径,估计麦角胺的生物利用度均较低(0.5-4.2%)。仅吸入麦角胺会导致血浆中麦角胺的浓度提前(5 分钟)达到峰值,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,我们建议改进吸入装置的方法。
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.