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环丙沙星及其他氟喹诺酮类药物的药物相互作用。

Drug-drug interactions with ciprofloxacin and other fluoroquinolones.

作者信息

Polk R E

机构信息

Department of Pharmacy, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0581.

出版信息

Am J Med. 1989 Nov 30;87(5A):76S-81S. doi: 10.1016/0002-9343(89)90028-4.

Abstract

Early investigational trials with new quinolone antibiotics revealed two important drug-drug interactions: decreased fluoroquinolone absorption when co-administered with magnesium-aluminum antacids and inhibition of theophylline metabolism. Subsequent studies have investigated the mechanisms of these interactions. With respect to the effect of antacids, the absorption of all quinolones appears to be significantly reduced by antacids containing magnesium and/or aluminum, and concomitant administration must be avoided. Other cations, such as calcium, iron, and probably zinc, appear to interact in a similar manner. Chelation between the quinolone and cation is the most likely mechanism. With respect to the effect on theophylline metabolism, quinolones inhibit specific cytochrome P-450 isozymes responsible for metabolism of methylxanthines, although there are major differences between the quinolones. Enoxacin is the most potent inhibitor, followed by ciprofloxacin, pefloxacin, norfloxacin, and ofloxacin. Caffeine metabolism is also inhibited, although the clinical significance is uncertain. Case reports describe renal failure associated with concomitant administration of cyclosporine and ciprofloxacin, although controlled trials have not demonstrated an interaction. Enoxacin has little effect on warfarin metabolism, suggesting that other quinolones may not affect warfarin disposition. Case reports of central nervous system toxicity from administration of nonsteroidal anti-inflammatory agents and quinolones need confirmation. Patients should be monitored closely when potential interacting agents are used; it is probable that not all interactions have been identified.

摘要

早期针对新型喹诺酮类抗生素开展的研究性试验揭示了两种重要的药物相互作用

与镁铝抗酸剂合用时氟喹诺酮类药物的吸收减少,以及对茶碱代谢的抑制作用。后续研究对这些相互作用的机制进行了探究。关于抗酸剂的影响,含镁和/或铝的抗酸剂似乎会显著降低所有喹诺酮类药物的吸收,必须避免同时给药。其他阳离子,如钙、铁,可能还有锌,似乎也以类似方式相互作用。喹诺酮类药物与阳离子之间的螯合作用是最可能的机制。关于对茶碱代谢的影响,喹诺酮类药物会抑制负责甲基黄嘌呤代谢的特定细胞色素P - 450同工酶,不过喹诺酮类药物之间存在重大差异。依诺沙星是最强的抑制剂,其次是环丙沙星、培氟沙星、诺氟沙星和氧氟沙星。咖啡因代谢也会受到抑制,尽管其临床意义尚不确定。病例报告描述了环孢素与环丙沙星同时给药导致肾衰竭的情况,不过对照试验并未证实存在相互作用。依诺沙星对华法林代谢影响很小,这表明其他喹诺酮类药物可能不会影响华法林的处置。关于非甾体抗炎药与喹诺酮类药物联合给药导致中枢神经系统毒性的病例报告需要得到证实。当使用可能存在相互作用的药物时,应对患者进行密切监测;很可能并非所有相互作用都已被识别出来。

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