Bernard N, Fauvel J P, Pozet N, Ferry N, Cuisinaud G, Haond P, Chapuy P, Sassard J
Department of Physiology and Clinical Pharmacology, Faculty of Pharmacy, Lyon, France.
Eur J Clin Pharmacol. 1991;41(6):603-7. doi: 10.1007/BF00314993.
The pharmacokinetics of Chlormezanone (CM) has been determined after a single oral dose of 400 mg CM in 5 young volunteers (28 y) and in 8 elderly patients (79 y). In the young subjects, CM was rapidly absorbed and distributed, and was slowly eliminated with a half-life of 38 h major metabolites were not detected in plasma or urine. Only 3% of CM was excreted unchanged in urine. In elderly patients absorption was delayed but not reduced; the Cmax and AUC did not differ from those in younger subjects, the elimination rate was reduced compared to the younger subjects (mean 54 h). The increase was in part related to the reduction in renal function and metabolism observed in aging. However, the change in pharmacokinetics was moderate and no adjustment in dosage seems necessary for treatments of limited duration in elderly patients.
在5名年轻志愿者(28岁)和8名老年患者(79岁)单次口服400毫克氯美扎酮(CM)后,测定了氯美扎酮的药代动力学。在年轻受试者中,CM吸收和分布迅速,消除缓慢,半衰期为38小时,血浆或尿液中未检测到主要代谢物。仅3%的CM以原形经尿液排泄。在老年患者中,吸收延迟但未减少;Cmax和AUC与年轻受试者无差异,与年轻受试者相比消除率降低(平均54小时)。这种增加部分与衰老过程中观察到的肾功能和代谢降低有关。然而,药代动力学变化适中,对于老年患者的短期治疗似乎无需调整剂量。