Low Biological Availability of Ergotamine Tartrate After Oral Dosing in Cluster Headache
Low Biological Availability of Ergotamine Tartrate After Oral Dosing in Cluster Headache
复制标题
丛集性头痛口服给药后酒石酸麦角胺的生物利用度较低
DOI：
10.1046/j.1468-2982.1981.0104203.x
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发表时间：
1981
期刊：
影响因子：
4.9
通讯作者：
E. Waldenlind
中科院分区：
文献类型：
--
作者：
K. Ekbom;L. Paalzow;E. Waldenlind
本文试图测定9名男性丛集性头痛患者口服治疗剂量的酒石酸麦角胺（Cafergot（r））后15-600分钟的血浆麦角胺浓度。有些病人被研究了两次。5名患者接受了每天2-4 mg的恒定剂量，持续至少7天。4例患者每天给予1 mg 5次，3例患者单次口服2 mg。采用高效液相色谱-荧光检测法测定麦角胺，方法灵敏度高，特异性强，检出限小于100 pg/ml。在任何血浆样本中均未发现酒石酸麦角胺。在一名患者中，单次口服2 mg麦角胺后1小时，脑脊液中未检测到麦角胺。口服生物利用度小于1%，这是口服给药后原型麦角胺的最大有效分数。在我们的几名患者中观察到临床获益。药物的这些作用可能是由于活性代谢物的形成和/或麦角胺对颅血管的高亲和力。
An attempt was made to determine the plasma ergotamine concentrations in nine male patients with cluster headache 15–600 min after oral therapeutic doses of ergotamine tartrate (Cafergot(r)). Some of the patients were studied twice. Five patients received a constant dose of 2–4 mg daily for at least seven days. Four patients were given 1 mg five times on one day and three patients a single oral dose of 2 mg. Ergotamine was determined by means of high performance liquid chromatography with fluorescence detection-a new highly sensitive, specific method, the detection limit of which is less than 100 pg/ml for ergotamine. Ergotamine tartrate was not discovered in any of the plasma samples. In one patient ergotamine could not be detected in the cerebrospinal fluid one hour after a single oral dose of 2 mg. The oral biological availability is less than 1%, which is the maximal available fraction of unchanged ergotamine after oral administration. A clinical benefit was observed in several of our patients. These effects of the drug may be because of active metabolites being formed and/or to high affinity of ergotamine to cranial vessels.