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氟喹诺酮类药物:在眼部治疗中的应用

Fluoroquinolones: place in ocular therapy.

作者信息

Smith A, Pennefather P M, Kaye S B, Hart C A

机构信息

St. Paul's Eye Unit, Royal Liverpool University Hospital, England.

出版信息

Drugs. 2001;61(6):747-61. doi: 10.2165/00003495-200161060-00004.

Abstract

The fluoroquinolones have become widely used antibacterial agents in the treatment of ocular infections, with topical, intravitreal and systemic routes of administration being used. In general, fluoroquinolones (such as ciprofloxacin, ofloxacin, lomefloxacin and norfloxacin) have good activity against gram-negative and gram-positive bacteria. Therapeutic concentrations are achieved in the cornea after topical administration so that the fluoroqinolones have largely replaced combination therapy for the treatment of bacterial keratitis. However, a second line agent is needed when resistance is likely, such as in disease caused by streptococcal species. Reversal of resistance to quinolones may not occur with withdrawal of the antibacterial. This stresses the importance of prudent prescribing to reduce the occurrence of resistance to quinolones. When used in therapeutic topical dosages, corneal toxicity does not occur. Similarly, retinal toxicity is not seen when fluoroquinolones are used at therapeutic dosages, systemically or topically. Corneal precipitation occurs, particularly with ciprofloxacin and to a lesser extent norfloxacin, but does not appear to interfere with healing. In the treatment of endophthalmitis there is reasonable penetration of systemic fluoroquinolones into the vitreous but sufficiently high concentrations to reach the minimum inhibitory concentration for 90% of isolates (MIC90) of all important micro-organisms may not be guaranteed. Systemic administration may be useful for prophylaxis after ocular trauma.

摘要

氟喹诺酮类药物已成为治疗眼部感染广泛使用的抗菌剂,给药途径包括局部、玻璃体内和全身给药。一般来说,氟喹诺酮类药物(如环丙沙星、氧氟沙星、洛美沙星和诺氟沙星)对革兰氏阴性菌和革兰氏阳性菌都有良好的活性。局部给药后角膜可达到治疗浓度,因此氟喹诺酮类药物在很大程度上已取代联合疗法用于治疗细菌性角膜炎。然而,在可能出现耐药的情况下,如由链球菌属引起的疾病,需要使用二线药物。停用抗菌药物后,对喹诺酮类药物的耐药性可能不会逆转。这凸显了谨慎用药以减少喹诺酮类药物耐药性发生的重要性。以治疗性局部剂量使用时,不会出现角膜毒性。同样,全身或局部以治疗剂量使用氟喹诺酮类药物时,也不会出现视网膜毒性。角膜会出现沉淀,尤其是环丙沙星,诺氟沙星的沉淀程度较轻,但似乎不会干扰愈合。在治疗眼内炎时,全身使用的氟喹诺酮类药物可合理渗透到玻璃体中,但可能无法保证达到所有重要微生物90%分离株的最低抑菌浓度(MIC90)的足够高浓度。全身给药可能对眼外伤后的预防有用。

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