Ibraheem J J, Paalzow L, Tfelt-Hansen P
Eur J Clin Pharmacol. 1982;23(3):235-40. doi: 10.1007/BF00547560.
The kinetics of ergotamine has been investigated in migrainous patients using a new, specific, sensitive HPLC assay (detection limit 100 pg/ml plasma). 10 patients were given ergotamine tartrate 0.5 mg i.v. and 5 of them received the same dose i.m. 2-3 weeks later. Blood samples were collected for up to 54 h following administration and the plasma concentration were analysed. After intravenous administration the plasma ergotamine declined rapidly, with and initial distribution half-life of 3 min followed by a mean terminal half-life of 1.86 h (range 90-155 min). The mean total plasma clearance was 11.0 ml kg-1 min-1, and the volume of distribution (Vd beta) was 1847.6 ml kg-1. Individual t1/2 beta showed a positive linear correlation with the individual Vd beta. The intramuscular absorption of ergotamine was rapid and maximum plasma levels were usually obtained 10 min following administration. The biological availability was incomplete and variable at 46.6% (range 28.3-60.8%).
采用一种新的、特异的、灵敏的高效液相色谱法（血浆检测限为100 pg/ml），对偏头痛患者体内麦角胺的动力学进行了研究。10例患者静脉注射0.5 mg酒石酸麦角胺，其中5例在2至3周后肌肉注射相同剂量。给药后长达54小时采集血样并分析血浆浓度。静脉给药后，血浆麦角胺迅速下降，初始分布半衰期为3分钟，随后平均终末半衰期为1.86小时（范围90至155分钟）。平均总血浆清除率为11.0 ml·kg⁻¹·min⁻¹，分布容积（Vdβ）为1847.6 ml·kg⁻¹。个体t1/2β与个体Vdβ呈正线性相关。麦角胺的肌肉注射吸收迅速，给药后10分钟通常可达到血浆最高水平。生物利用度不完全且变化较大，为46.6%（范围28.3%至60.8%）。
