Harder S, Staib A H, Beer C, Papenburg A, Stille W, Shah P M
Department of Clinical Pharmacology, University Hospital, Frankfurt/Main, Federal Republic of Germany.
Eur J Clin Pharmacol. 1988;35(6):651-6. doi: 10.1007/BF00637602.
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.
已对12名健康男性（年龄20 - 40岁）单独以及在同时服用4 - 喹诺酮类药物氧氟沙星、诺氟沙星、吡哌酸、环丙沙星和依诺沙星的情况下咖啡因的药代动力学进行了研究，包括其主要代谢产物对黄嘌呤在血浆中的形成；环丙沙星和依诺沙星给予了3种不同剂量水平。萘啶衍生物依诺沙星和吡啶 - 嘧啶衍生物吡哌酸对咖啡因和对黄嘌呤的代谢有显著抑制作用，而真正的喹诺酮衍生物诺氟沙星和环丙沙星影响较小，吡啶 - 苯并恶嗪衍生物氧氟沙星则未检测到有影响。这些化合物不同的分子和空间结构似乎导致了抑制效力的差异。
