Janknegt R
Department of Clinical Pharmacology and Toxicology, Maasland Hospital, Sittard, The Netherlands.
J Antimicrob Chemother. 1990 Nov;26 Suppl D:7-29. doi: 10.1093/jac/26.suppl_d.7.
The pharmacodynamic and pharmacokinetic drug interactions and pharmaceutical compatibilities of fluoroquinolones are reviewed. Incompatibilities are observed between quinolones and penicillins such as flucloxacillin and amoxicillin and with clindamycin when mixed in an administration set. Fluoroquinolones, especially enoxacin, and to a lesser extent ciprofloxacin and pefloxacin, inhibit the metabolic clearance of theophylline and caffeine. It is advisable to use non-interacting quinolones such as ofloxacin or norfloxacin or to measure theophylline levels and reduce caffeine intake where appropriate. A potential interaction with midazolam needs further study. The absorption of fluoroquinolones is markedly reduced by antacids, calcium carbonate, ferrous sulphate and sucralfate. Although quantitative differences between fluoroquinolones exist, these combinations should be avoided whenever possible. Cimetidine reduces the metabolic clearance of pefloxacin. More studies are needed on the possible reduction of absorption of fluoroquinolones by opiates. Several case reports of a pharmacodynamic interaction between fluoroquinolones and cyclosporin or oral anticoagulants exist. No pharmacokinetic interaction has been observed and more, controlled studies are needed to assess the significance of the pharmacodynamic interaction. A high incidence of convulsions has been observed in patients receiving the combination enoxacin and fenbufen, an NSAID. A synergistic inhibitory effect of fluoroquinolones and several NSAIDs has been observed on the binding of the neurotransmitter GABA. Although the relevance of this interaction is probably not great, except with fenbufen, a possible epileptogenic effect of the combination cannot be excluded.
本文综述了氟喹诺酮类药物的药效学、药代动力学药物相互作用及药物配伍性。喹诺酮类药物与氟氯西林、阿莫西林等青霉素类药物以及与克林霉素在给药装置中混合时会出现配伍禁忌。氟喹诺酮类药物，尤其是依诺沙星，其次是环丙沙星和培氟沙星，会抑制茶碱和咖啡因的代谢清除。建议使用相互作用小的喹诺酮类药物，如氧氟沙星或诺氟沙星，或者在适当情况下测定茶碱水平并减少咖啡因摄入量。与咪达唑仑的潜在相互作用需要进一步研究。抗酸剂、碳酸钙、硫酸亚铁和硫糖铝会显著降低氟喹诺酮类药物的吸收。尽管氟喹诺酮类药物之间存在定量差异，但应尽可能避免这些组合。西咪替丁会降低培氟沙星的代谢清除率。关于阿片类药物可能降低氟喹诺酮类药物吸收的情况，还需要更多研究。有几例关于氟喹诺酮类药物与环孢素或口服抗凝剂之间药效学相互作用的病例报告。尚未观察到药代动力学相互作用，需要更多对照研究来评估药效学相互作用的重要性。在接受依诺沙星和非甾体抗炎药芬布芬联合治疗的患者中观察到惊厥发生率较高。已观察到氟喹诺酮类药物与几种非甾体抗炎药对神经递质γ-氨基丁酸（GABA）结合具有协同抑制作用。尽管这种相互作用的相关性可能不大，除了与芬布芬联合外，但不能排除该组合可能产生的致癫痫作用。
