Zylber-Katz E, Granit L, Stessman J, Levy M
Department of Medicine A. Hadassah University Hospital, Jerusalem, Israel.
Eur J Clin Pharmacol. 1989;36(5):513-6. doi: 10.1007/BF00558078.
The pharmacokinetics of the dipyrone metabolite, 4-methylaminoantipyrine (MAA) was evaluated, following the administration of a single oral dose of dipyrone 1.0 g to 12 young (21-30 years) and 9 elderly (73-90 years) healthy volunteers. Maximal concentration, time to peak and absorption rate of MAA were similar for both groups. The elimination half-life was 2.6 (0.2) h for the young and 4.5 (0.5) h for the elderly subjects. Total clearance of MAA, corrected for lean body mass (LBM), was lower in the elderly than in the young 2.65 vs 3.97 ml.min-1.kg-1 LBM. There was no differences between the groups in the apparent volume of distribution. A good correlation was found between the total body clearance of MAA and the creatinine clearance, which was also reduced in the elderly (r = 0.61).
在向12名年轻(21 - 30岁)和9名老年(73 - 90岁)健康志愿者单次口服1.0 g安乃近后,对安乃近代谢产物4 - 甲基氨基安替比林(MAA)的药代动力学进行了评估。两组的MAA最大浓度、达峰时间和吸收速率相似。年轻受试者的消除半衰期为2.6(0.2)小时,老年受试者为4.5(0.5)小时。经去脂体重(LBM)校正后,老年组MAA的总清除率低于年轻组,分别为2.65 vs 3.97 ml·min⁻¹·kg⁻¹ LBM。两组间的表观分布容积无差异。发现MAA的全身清除率与肌酐清除率之间存在良好的相关性,肌酐清除率在老年人中也降低(r = 0.61)。