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Retinal toxicity and ocular kinetics of 1-β-D-arabinofuranosyl-E-5-(2-bromovinyl)uracil in rabbits

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Abstract

The intraocular penetration of 1-β-d-arabinofuranosyl-E-5-(2-bromovinyl)uracil (BV-araU), a new antiviral drug, after oral administration, the effects of non-toxic intravitreal doses of BV-araU, and the intraocular kinetics of BV-araU after intraocular injection were studied in rabbits. The intravitreal penetration of BV-araU after oral administration was very poor: 0.11 ± 0.13 μg/ml and 0.20 ±0.02 μg/ml respectively in albino and pigmented rabbits 2 h after 30 mg/kg. An intravitreal injection of 200 μg BV-araU caused transient electroretinographic (ERG) changes, whereas a 100-μg injection and intravitreal irrigation with 20 μg/ml BV-araU caused no ERG and histologic changes over the 4-week follow-up period. The half-life of the intravitreal concentration of BV-araU after an intravitreal injection was short (2.4 h). The results suggest that an intravitreal injection of 100 μg BV-araU or an intravitreal irrigating solution containing 20 μg/ml BV-araU is nontoxic to the retina and may be used for treatment of retinitis caused by varicella-zoster virus or herpes simplex virus type 1.

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Authors and Affiliations

  1. Department of Ophthalmology, Kanazawa University School of Medicine, 13-1 Takara-machi, Kanazawa, 920, Ishikawa, Japan

    Kiyofumi Mochizuki, Makoto Torisaki, Yohko Yamashita, Masaki Komatsu & Toshiro Tanahashi

  2. Research & Development Division, Yamasa Corporation, Choshi, Japan

    Katsushi Ijichi & Haruhiko Machida

Authors
  1. Kiyofumi Mochizuki
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  2. Makoto Torisaki
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  3. Yohko Yamashita
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  4. Masaki Komatsu
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  5. Toshiro Tanahashi
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  6. Katsushi Ijichi
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  7. Haruhiko Machida
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Mochizuki, K., Torisaki, M., Yamashita, Y. et al. Retinal toxicity and ocular kinetics of 1-β-D-arabinofuranosyl-E-5-(2-bromovinyl)uracil in rabbits. Graefe's Arch Clin Exp Ophthalmol 232, 503–508 (1994). https://doi.org/10.1007/BF00195362

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  • DOI: https://doi.org/10.1007/BF00195362

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