Ocular toxicity of fluoroquinolones

Abstract

The ocular toxicity of fluoroquinolones and the risks of their use in the treatment of ocular infection were reviewed. Systematic identification, selection, review and synthesis of published English-language studies relating to fluoroquinolone use and safety in animals and humans was conducted. Although not free of complications, fluoroquinolones are generally safe when used to treat ocular infection. Ocular toxicity appears to be dose-dependent and results from class-effects and specific fluoroquinolone structures. Phototoxicity and neurotoxicity have been reported, and toxic effects on ocular collagen may be associated with Achilles tendinopathy. Corneal precipitation may provide an advantageous drug depot but delay healing and result in corneal perforation in approximately 10% of cases. Although human toxicity studies are limited, the current recommended dose for intracameral injection of ciprofloxacin is less than 25 microg. Intravitreal injections of ciprofloxacin 100 microg, ofloxacin 50 microg/mL, trovafloxacin 25 microg or less, moxifloxacin 160 microg/0.1 mL or less and pefloxacin 200 microg/0.1 mL are considered safe.

Cytotoxic effect of lomefloxacin in culture of human epidermal melanocytes

“…Phototoxicity is postulated to occur as a result of fluoroquinolones photodegradation and the molecules ability to generate free oxygen radicals. In turn, these oxidative radicals may attack cellular lipid membranes, initiating inflammatory processes, and cause mitochondria or DNA damage [42]. The study conducted by Marrot et al [26] on human skin cells, i.e., normal human fibroblasts, keratinocytes and Caucasian melanocytes, confirmed the ability of lomefloxacin to induce DNA damage such as strand breaks and pyrimidine dimers.…”

“…Halogenation (chlorine, fluorine) of position 8 in concert with fluorination of position 6 (the so-called double-halogenated quinolones) has demonstrated significant photototoxic potential [30]. Therefore, lomefloxacin and sparfloxacin have been reported to have relatively high phototoxic potential as compared with other fluoroquinolones, e.g., ciprofloxacin or norfloxacin [27,42]. UV-induced defluorination at the 8-position generates a highly reactive aromatic carbene intermediate.…”

“…Lomefloxacin is widely used in clinical practice to treat infections of the respiratory or urinary tracts, as well as in ophthalmology and dermatology [35,42]. Like other fluoroquinolones, lomefloxacin acts by inhibiting DNA topoisomerases, of which DNA gyrase and topoisomerase IV are particularly important [28,40].…”

Modification of Innervation Pattern by Fluoroquinolone Treatment in the Rat Salivary Glands

“…Another possible mechanism of the neurotoxic side effect of FQAs is their interaction with various neurotransmitter receptors (Thompson, 2007). For instance, the fluoroquinolone antagonism with the GABA receptors was found in the retina, and it was thought to be the explanation of retinal toxicity (Sakai et al, 1994).…”

Endophthalmitis, Prevention and Treatment

“…Experimental data suggests a Moxifloxacin dose of 160ug/0.1cc is probably safe. 32 The major limitation of intraocular antimicrobials is the short duration of action. Reinjection should be considered if the infection fails to stabilize or improve more than 48 hours after the first injection.…”