Lomerizine 2HCl is an L- and T-typecalcium channel blocker used in the treatment of migraine.
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Lomerizine dihydrochloride (LOM) is a Ca2+ channel blocker used as an antimigraine drug, which is currently administered orally in Japan[3]. Lomerizine reduced the retinal damage induced by NMDA (N-methyl-D-aspartate) and partially prevented the transsynaptic neuronal degeneration within dLGN and SC on the contralateral side. Moreover, lomerizine reduced the intravitreal NMDA induced decrease in the light-induced expression of c-Fos in the contralateral dLGN (used in this study to evaluate residual vision). Thus, lomerizine affords some protection against transsynaptic neuronal degeneration within the visual center of the mouse brain[4]. Lomerizine may inhibit not only voltage-dependent Ca(2+) channels but also 5-HT(2A) receptors and so inhibit 5-HT-induced contraction in the basilar artery[5]. The inhibition of H(2)O(2)-induced Ca(2+) influx through T-type VDCC (voltage-dependent Ca(2+) channel) seems to be important in the protective effect of lomerizine against oxidative stress. It is possible that lomerizine may be a useful drug for prophylactic treatment of migraine, because migraine is a risk factor for ischemic stroke[6]. In healthy humans, lomerizine increased blood velocity in the optic nerve head, without significantly altering blood pressure or heart rate. Moreover, lomerizine reduced retinal damage in rats both in vitro and in vivo, presumably through a Ca(2+) channel blocking effect via an action that may involve a direct protection of retinal neurons as well as an improvement in the ocular circulation[7].
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