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Journal of Antimicrobial Chemotherapy (1987) 20, 729-734
© 1987 The British Society for Antimicrobial Chemotherapy


research-article

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

Wolfgang Stillea,, Sebastian Harderb, Sylvia Miekeb, Christian Beerb, Pramod M. Shaha, Karin Frecha and A. Horst Staibb

aZentrum der Inneren Medizin, Infektiologie, Klinikum der Johann Wolfgang Goethe-Universität Frankfurt D-6000 Frankfurt 70, Federal Republic of Germany bAbteilung für Klinische Pharmakologie, Klinikum der Johann Wolfgang Goethe-Universität Frankfurt D-6000 Frankfurt 70, Federal Republic of Germany

accepted 3 June 1987


Correspondence to: Prof. Dr W. Stille, Zentrum der Inneren Medizin, Infektiologie, Klinikum der Johann Wolfgang Goethe- Universität Frankfurt, Theodor- Stern- Kai 7, D-6000 Frankfurt 70, F.R.G.

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 (T1/2cl), Cmax, total body clearance (Cl{omega}t) and the volume of distribution ({alpha}Vd) of caffeine were noticeably altered by administration of ofloxacin. Striking changes were observed, however, after administration of enoxacin: the T1/2cl was prolonged by as much as 260%, the Cmax increased by 41%; the aVd was reduced by 20% and Cl{omega}t by 78% (mean values). Treatment with ciprofloxacin led to a prolongation of T1/2cl by 15%, to a decrease of aVd by 25% and to a 33% decrease of Cl{omega}t. 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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