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. 1987 Nov;20(5):729-34.
doi: 10.1093/jac/20.5.729.

Decrease of caffeine elimination in man during co-administration of 4-quinolones

W Stille  1 , S Harder, S Mieke, C Beer, P M Shah, K Frech, A H Staib
Affiliations

Decrease of caffeine elimination in man during co-administration of 4-quinolones

W Stille et al. J Antimicrob Chemother. 1987 Nov.

Abstract

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.

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