Lomaestro B M, Bailie G R
Albany Medical Center Hospital, Pharmacy Department, New York, USA.
Drug Saf. 1995 May;12(5):314-33. doi: 10.2165/00002018-199512050-00004.
The utility of the fluoroquinolone class of antibiotics is rapidly expanding due to their favourable pharmacokinetic profile and the continuing development of new compounds. These agents are often used for indications not successfully treated with other orally available antimicrobials in the past, or for 'step-down' therapy in patients originally treated with intravenous agents. As the usage of these agents expands for serious systemic infections, knowledge of absorptive interactions with fluoroquinolones becomes paramount. Fluoroquinolones are often utilised in dosages and against modestly susceptible pathogens which allow a narrow margin for acceptable decreases in bioavailability. Chelation interactions with multivalent cations can result in inactivation of the fluoroquinolone with ramifications in vitro and in vivo. Chelation interactions have been reported to occur in between 22 and 76% of patients prescribed fluoroquinolones. Concurrent administration of magnesium-aluminum antacids and sucralfate has the greatest effect on the bioavailability of quinolones followed by iron, calcium and zinc. Spacing doses of fluoroquinolones and interactants has been suggested as a method of ensuring adequate quinolone absorption, but this can make optimal administration of the cation interactant difficult, if not impossible.
由于氟喹诺酮类抗生素具有良好的药代动力学特性以及新化合物的不断研发,其应用范围正在迅速扩大。这些药物常用于过去其他口服抗菌药物治疗失败的适应症,或用于最初接受静脉用药治疗的患者的“降阶梯”治疗。随着这些药物在严重全身感染中的应用不断增加,了解与氟喹诺酮类药物的吸收相互作用变得至关重要。氟喹诺酮类药物通常以一定剂量使用,针对的是敏感性一般的病原体,这使得生物利用度可接受的降低幅度很小。与多价阳离子的螯合相互作用可导致氟喹诺酮类药物失活,在体外和体内均会产生影响。据报道,在使用氟喹诺酮类药物的患者中,有22%至76%会发生螯合相互作用。同时服用镁铝抗酸剂和硫糖铝对喹诺酮类药物的生物利用度影响最大,其次是铁、钙和锌。有人建议将氟喹诺酮类药物与相互作用物质的给药时间错开,作为确保喹诺酮类药物充分吸收的一种方法,但这可能会使阳离子相互作用物质的最佳给药变得困难,甚至无法实现。