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  • Title: Ocular distribution after topical instillation and potential neuroprotective effect after intravitreal injection of the calcium channel blocker iganipidine.
    Author: Ohashi M, Saito S, Fukaya Y, Tomidokoro A, Araie M, Kashwagi K, Suzuki Y.
    Journal: Curr Eye Res; 2005 Apr; 30(4):309-17. PubMed ID: 16020261.
    Abstract:
    PURPOSE: To investigate the effects of iganidipine, a new calcium antagonist on glutamate agonist-induced retinal damage. METHODS: Iganidipine was injected with N-methyl-D-aspartate (NMDA) or kainic acid (KA) into the rat vitreous, and the retina was histologically examined. After co-injection with KA, the number of DiI-labeled retinal ganglion cells was also counted. Rabbits received unilateral instillation of 0.03% iganidipine twice daily for 14 days, and the iganidipine level in the posterior retina-choroid was determined by liquid chromatography/mass spectrometry. RESULTS: Coadministration of iganidipine had no significant effect on NMDA-induced thinning of the inner plexiform layer but partly suppressed KA-induced thinning at final intravitreous concentrations of 10(-8) M or higher, which was confirmed by counting the ganglion cell number. The iganidipine level in the posterior retina-choroid was approximately 6.2 x 10(-7) M in the instilled eye, which was higher than on the contralateral side by 5.2 x 10(-7) M (p = 0.035). CONCLUSIONS: Iganidipine suppressed KA-induced retinal damage in rats. This suppression was achieved with a lower concentration than that resulting from unilateral instillations of iganidipine in the ipsilateral posterior retina-choroid in rabbits.
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