Wurzinger L J, Schmid-Schönbein H
Abteilung Physiologie der Medizinischen Fakultät der Rheinisch-Westfälischen Technischen Hochschule Aachen, Fed. Rep. of Germany.
Arzneimittelforschung. 1987 Oct;37(10):1113-5.
The effect of buflomedil (4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone) in vitro and ex vivo after intravenous and oral administration was tested upon epinephrine-enhanced platelet aggregation (PA) in platelet-rich plasma (PRP) prepared from heparinized blood of healthy volunteers. In vitro incubation of PRP with buflomedil in concentrations above 10 mumol/l resulted in a significant depression of PA to approximately one-third of the control. 30 min after a single intravenous dose of 2.5 mg/kg buflomedil a depression of epinephrine-enhanced PA to about 60% of the value before injection of the drug was observed. This effect wore off during a few hours and was no longer present 24 h thereafter. Oral ingestion of 600 mg/d buflomedil depressed PA to approximately two-thirds within 2 days, with a further decrease to some 50% after 6 days of intake. 2 days after termination of treatment epinephrine-enhanced PA had returned to premedication values. Unlike nonsteroidal antiinflammatory drugs buflomedil does not act through an inhibition of prostaglandin synthesis.
在由健康志愿者肝素化血液制备的富血小板血浆（PRP）中，测试了丁咯地尔（4-(1-吡咯烷基)-1-(2,4,6-三甲氧基苯基)-1-丁酮）在静脉内和口服给药后对肾上腺素增强的血小板聚集（PA）的体外和离体作用。将PRP与浓度高于10μmol/L的丁咯地尔进行体外孵育，导致PA显著降低至对照值的约三分之一。单次静脉注射2.5mg/kg丁咯地尔30分钟后，观察到肾上腺素增强的PA降低至注射药物前值的约60%。这种作用在数小时内逐渐消失，24小时后不再存在。口服600mg/d丁咯地尔在2天内将PA降低至约三分之二，摄入6天后进一步降至约50%。治疗终止2天后，肾上腺素增强的PA已恢复至用药前值。与非甾体抗炎药不同，丁咯地尔不是通过抑制前列腺素合成起作用。
