Müller T, Kuhn W, Quack G, Przuntek H
Department of Neurology, University of Bochum, Federal Republic of Germany.
J Neural Transm Suppl. 1995;46:407-13.
The aim of this study was to estimate the pharmacokinetic properties of amantadine after infusion and subsequent peroral application of two galenic forms at a daily dose of 200 mg. In addition, the pharmacodynamics of the different treatment regimes evaluated by the motoric items of the UPDRS were investigated. Furthermore, the relationship between plasma levels and clinical efficacy was evaluated. To address these questions Parkinsonian patients were randomly assigned to 3 groups: infusion-tablet, infusion-capsule, infusion-infusion. Parenteral application of amantadine sulphate provided a rapid improvement in Parkinsonian patients within the first three days. This response could be stabilized and even improved further by peroral treatment for another 3 days. The change from intravenous to peroral tablet therapy was followed by a transient decrease in cmax and AUC(o-t) being not reflected by a reduction in clinical efficacy. Conversely, a persistent reduction of the plasma concentration after switching to the capsule therapy was paralleled by a somewhat unfavourable clinical response.
本研究的目的是评估在每日剂量为200mg时,两种剂型金刚烷胺静脉输注后再口服给药的药代动力学特性。此外,还研究了通过帕金森病统一评分量表(UPDRS)的运动项目评估的不同治疗方案的药效学。此外,还评估了血浆水平与临床疗效之间的关系。为解决这些问题,帕金森病患者被随机分为3组:静脉输注-片剂组、静脉输注-胶囊组、静脉输注-静脉输注组。硫酸金刚烷胺的肠外给药在头三天内使帕金森病患者迅速改善。通过口服治疗另外3天,这种反应可以稳定下来,甚至进一步改善。从静脉给药改为口服片剂治疗后,cmax和AUC(0-t)短暂下降,但临床疗效并未降低。相反,改用胶囊治疗后血浆浓度持续降低,同时临床反应略显不利。