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Published on: February 15, 2020
Photochemical toxicity of drugs intended for ocular use
Abstract:
The present investigation was undertaken to evaluate the possible ocular phototoxicity of drugs used in ophthalmic formulations. Sulphacetamide, ketoconazole, voriconazole, diclofenac, and ketorolac were assessed in the concentrations available in the market for their ocular use. The suitable models viz Hen's Egg Test Chorioallantoic Membrane (HET-CAM) test, Isolated Chicken Eye (ICE) test, and Red Blood Cell (RBC) haemolysis test as recommended by ECVAM, ICCVAM, and OECD guidelines were performed. Results of HET-CAM and ICE tests suggest that sulphacetamide is moderately toxic in the presence of light/UV-A and very slightly irritant without irradiation. Ketoconazole and voriconazole were found slightly irritant in presence of light/UV-A and non-irritant in dark. Diclofenac and ketorolac demonstrated slight irritancy in the light and were found to be non-irritant in dark. The results suggest that some of the drugs have potential toxic effect in the presence of light. The extent of phototoxicity might get extended when used for longer time. The recommendation is that these drugs should be stored and used in the dark for a specified time and be labelled with specific instructions for patients, especially for those working longer in the sunlight.
Insights
Ophthalmic drugs like sulphacetamide can be phototoxic, causing moderate toxicity with UV-A light exposure. Patients should use these medications in the dark and follow specific labeling instructions to minimize risks.
Area of Science:
- Ophthalmology
- Photobiology
- Toxicology
Background:
- Ophthalmic drug formulations contain various active ingredients.
- Phototoxicity is a potential adverse effect of some medications.
- Evaluating ocular phototoxicity is crucial for patient safety.
Purpose of the Study:
- To assess the ocular phototoxicity of commonly used ophthalmic drugs.
- To determine the safety of sulphacetamide, ketoconazole, voriconazole, diclofenac, and ketorolac under light exposure.
Main Methods:
- Utilized Hen's Egg Test Chorioallantoic Membrane (HET-CAM), Isolated Chicken Eye (ICE), and Red Blood Cell (RBC) haemolysis tests.
- Assessed drugs at market concentrations, following ECVAM, ICCVAM, and OECD guidelines.
- Evaluated effects in the presence and absence of UV-A irradiation.
Main Results:
- Sulphacetamide showed moderate toxicity with UV-A light and slight irritation without.
- Ketoconazole and voriconazole were slightly irritant with UV-A light, non-irritant in dark.
- Diclofenac and ketorolac exhibited slight irritancy in light, non-irritant in dark.
Conclusions:
- Several ophthalmic drugs possess phototoxic potential, particularly under UV-A light exposure.
- Prolonged use may exacerbate phototoxic effects.
- Recommendations include dark storage, light avoidance during use, and clear patient labeling.
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