Burns R S, Gopinathan G, Hümpel M, Dorow R, Calne D B
Clin Pharmacol Ther. 1984 Apr;35(4):548-56. doi: 10.1038/clpt.1984.76.
The single and multiple oral dose plasma kinetics of lisuride were followed by a recently developed radioimmunoassay method in 11 patients with Parkinson's disease. A very wide range of plasma drug concentrations resulted from a single dose of 300 micrograms, as reflected in large interindividual differences in peak concentration (0.27 to 3.30 ng/ml) and AUC after the initial dose (43.1 to 617 ng X min/ml). Absorption was rapid, with a mean time to peak of 39 min. Only 0.05% of the dose was excreted unchanged in urine in 24 hr. There was a 110% increase in apparent oral clearance after 2 to 4 wk of treatment.
采用最近开发的放射免疫分析法,对11例帕金森病患者进行了利苏瑞单次及多次口服给药后的血浆动力学研究。单次给予300微克剂量后,血浆药物浓度范围非常宽,初始剂量后的峰浓度(0.27至3.30纳克/毫升)和AUC(43.1至617纳克·分钟/毫升)存在很大的个体间差异。吸收迅速,平均达峰时间为39分钟。24小时内仅有0.05%的剂量以原形经尿液排泄。治疗2至4周后,表观口服清除率增加了110%。