Waite N M, Rybak M J, Krakovsky D J, Steinberg J D, Warbasse L H, Edwards D J
College of Pharmacy & Allied Health Professions, Wayne State University, Detroit, Michigan 48202.
Antimicrob Agents Chemother. 1991 Jan;35(1):130-4. doi: 10.1128/AAC.35.1.130.
Case reports suggest that the magnitude of inhibition of oxidative metabolism produced by ciprofloxacin may be greater in elderly subjects. We examined the effect of oral ciprofloxacin on antipyrine disposition in 13 young (ages, 23 to 34 years) and 9 elderly (ages, 65 to 82 years) healthy volunteers. Ciprofloxacin decreased antipyrine oral clearance in young and elderly subjects (P less than 0.05), with the average decreases being similar in both groups (23.3% for the young subjects and 27.9% for the elderly subjects). Ciprofloxacin concentrations in serum were significantly higher (mean, 57%) in the elderly. The formation clearance of 4-hydroxyantipyrine and 3-hydroxymethylantipyrine was also significantly decreased in both groups of subjects; however, norantipyrine formation, accounting for 15 to 20% of antipyrine clearance, was reduced only in the elderly. These results suggest that elderly subjects are not more sensitive to the inhibitory effect of ciprofloxacin on antipyrine metabolism. However, careful clinical monitoring is necessary with all patients, irrespective of age, taking ciprofloxacin concomitantly with drugs primarily eliminated by the cytochrome P-450 system.
病例报告表明,环丙沙星对氧化代谢的抑制程度在老年受试者中可能更大。我们研究了口服环丙沙星对13名年轻(年龄23至34岁)和9名老年(年龄65至82岁)健康志愿者中安替比林处置的影响。环丙沙星降低了年轻和老年受试者的安替比林口服清除率(P小于0.05),两组的平均降低幅度相似(年轻受试者为23.3%,老年受试者为27.9%)。老年受试者血清中环丙沙星浓度显著更高(平均高57%)。两组受试者中4-羟基安替比林和3-羟甲基安替比林的生成清除率也显著降低;然而,占安替比林清除率15%至20%的去甲安替比林生成仅在老年受试者中降低。这些结果表明,老年受试者对环丙沙星对安替比林代谢的抑制作用并不更敏感。然而,所有同时服用环丙沙星和主要通过细胞色素P-450系统消除的药物的患者,无论年龄大小,都需要仔细的临床监测。