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Clinical Trial
. 1988;35(6):651-6.
doi: 10.1007/BF00637602.

4-quinolones inhibit biotransformation of caffeine

S Harder  1 , A H Staib, C Beer, A Papenburg, W Stille, P M Shah
Affiliations
Clinical Trial

4-quinolones inhibit biotransformation of caffeine

S Harder et al. Eur J Clin Pharmacol. 1988.

Erratum in

  • Eur J Clin Pharmacol 1989;36(1):100

Abstract

The pharmacokinetics of caffeine, including formation of its major metabolite paraxanthine in plasma, has been investigated in 12 healthy males (age 20-40 years) alone and during co-administration of the 4-quinolones ofloxacin, norfloxacin, pipemidic acid, ciprofloxacin, and enoxacin; ciprofloxacin and enoxacin were given in 3 different dose levels. The naphthyridine derivative enoxacin and the pyrido-pyrimidine derivative pipemidic acid had caused marked inhibition of caffeine and paraxanthine metabolism, whereas the genuine quinolone derivatives norfloxacin and ciprofloxacin had little effect, and the pyrido-benzoxacine derivative ofloxacin had no detectable effect. The different molecular and spatial structures of the compounds appear to be responsible for the differences in inhibitory potency.

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