Groeneveld G J, van Kan H J, Toraño J S, Veldink J H, Guchelaar H J, Wokke J H, van den Berg L H
Neuromuscular Center Utrecht, University Medical Center Utrecht, PO Box 85500, 3508 GA, Utrecht, The Netherlands.
J Neurol Sci. 2001 Oct 15;191(1-2):121-5. doi: 10.1016/s0022-510x(01)00613-x.
All patients with amyotrophic lateral sclerosis (ALS) are treated with the same dose of riluzole: 50 mg twice daily. Reasonably large interindividual differences in clearance of the drug have been reported. The relatively small group of patients with high blood concentrations of riluzole has probably primarily influenced the efficacy and the incidence of side-effects in the previously conducted clinical trials with riluzole. Individual dosing of the drug may, in the case of large interindividual differences in serum concentrations of the drug, be necessary in the future. Exact data concerning the plasma and serum concentrations of riluzole in patients with ALS, after standardized intake of the drug, diet and blood sampling are unknown so far. In this study, inter- and intraindividual variability of serum and plasma levels of riluzole in 21 patients with "probable" or "definite" ALS were determined. The interindividual variability of peak serum levels (coefficient of variation=74%) was significantly larger than intraindividual variability (p<0.001). Serum levels were not correlated with age or smoking status. The determination of a correlation between riluzole serum concentrations and survival of patients with ALS will be the aim of further studies.
所有肌萎缩侧索硬化症（ALS）患者均接受相同剂量的利鲁唑治疗：每日两次，每次50毫克。据报道，该药物的清除率存在相当大的个体间差异。在先前进行的利鲁唑临床试验中，利鲁唑血药浓度较高的相对少数患者可能主要影响了疗效和副作用发生率。如果药物血清浓度存在较大个体间差异，未来可能需要进行个体化给药。目前尚无关于ALS患者在标准化摄入药物、饮食和采血后利鲁唑血浆和血清浓度的确切数据。在本研究中，测定了21例“可能”或“确诊”ALS患者血清和血浆中利鲁唑水平的个体间和个体内变异性。血清峰值水平的个体间变异性（变异系数=74%）显著大于个体内变异性（p<0.001）。血清水平与年龄或吸烟状况无关。进一步研究的目的将是确定利鲁唑血清浓度与ALS患者生存率之间的相关性。
