Stille W, Harder S, Mieke S, Beer C, Shah P M, Frech K, Staib A H
Zentrum der Inneren Medizin, Infektiologie, Klinikum der Johann Wolfgang Goethe-Universität Frankfurt, Federal Republic of Germany.
J Antimicrob Chemother. 1987 Nov;20(5):729-34. doi: 10.1093/jac/20.5.729.
The single dose pharmacokinetics of caffeine (220-230 mg per dose) were investigated in 12 healthy male volunteers before and during treatment with ofloxacin (200 mg bd), ciprofloxacin (250 mg bd) and enoxacin (400 mg bd) with a cross-over study design. None of the parameters: mean elimination half-life (T1/2el), Cmax, total body clearance (Cltot) and the volume of distribution (aVd) of caffeine were noticeably altered by administration of ofloxacin. Striking changes were observed, however, after administration of enoxacin: the T1/2el was prolonged by as much as 260%, the Cmax increased by 41%; the aVd was reduced by 20% and Cltot by 78% (mean values). Treatment with ciprofloxacin led to a prolongation of T1/2el by 15%, to a decrease of aVd by 25% and to a 33% decrease of Cltot. The results of this intra-individual comparison of caffeine pharmacokinetic data demonstrate that treatment with ciprofloxacin and enoxacin may have a significant inhibitory effect on caffeine elimination.
采用交叉研究设计，在12名健康男性志愿者中研究了咖啡因（每剂220 - 230毫克）的单剂量药代动力学，研究时间为服用氧氟沙星（200毫克，每日两次）、环丙沙星（250毫克，每日两次）和依诺沙星（400毫克，每日两次）之前及期间。氧氟沙星给药后，咖啡因的各项参数：平均消除半衰期（T1/2el）、Cmax、总体清除率（Cltot）和分布容积（aVd）均未出现明显改变。然而，服用依诺沙星后观察到显著变化：T1/2el延长多达260%，Cmax增加41%；aVd降低20%，Cltot降低78%（平均值）。环丙沙星治疗导致T1/2el延长15%，aVd降低25%，Cltot降低33%。咖啡因药代动力学数据的个体内比较结果表明，环丙沙星和依诺沙星治疗可能对咖啡因消除有显著抑制作用。
