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J. E. Roberts, C. F. Chignell, U. P. Andley, B. Zhao; Screening for Ocular Phototoxicity of Fluoroquinolone Antibiotics. Invest. Ophthalmol. Vis. Sci. 2010;51(13):1187.
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To determine the potential ocular phototoxicity of fluoroquinolone antibiotics (FLQ) used for ocular infections.
Human lens epithelial cells were exposed to 0.125-1 mM FLQs [ciprofloxacin (Cipro), lomefloxacin (Lome), nalidixic acid (Nalid), norfloxacin (Nor) and ofloxacin (Ofl)] and UVA radiation (2.5 J/cm2). Uptake and subcellularlocalization of the FLQ drugs was determined by confocal microscopy and staining with mitochondrial (MitoTracker Orange CMTMRos) and lysosomal (LysoTraker Red DND-99) probes. Cell viability was measured by MTS and membrane damage as determined by the LDH assay. Flow cytometry was used to determine the extent of necrosis and apoptosis. Binding of the FLQs was determined by shifts in the UV-vis absorption spectrum of the drugs in the presence of alpha crystallin.
All FLQs tested absorbed light in the UV-A region (320-340 nm). Neither FLQ drugs exposure alone nor UVA exposure alone reduced cell viability. In contrast, cells exposed to UVA and FLQs underwent necrosis and apoptosis and loss of cell viability as measured by MTS and membrane damage as determined by the LDH assay in the order: Cipro > Nor > Lome > Ofl > Nalid. None of the drugs tested were found to bind to alpha crystallin.
FLQs are potentially phototoxic to the eye. However since these antibiotics do not bind to lens proteins, permanent damage to the eye can be prevented if patients protect their eyes from intense sunlight by wearing wrap-around UV filtering sunglasses while taking these medications.
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