Description
Lomerizine hydrochloride was introduced as Teranas and Migsis in
Japan for the treatment of migraine. It is the first in its class of dual sodium and
calcium channel blockers to be marketed for this indication. It can be
synthetically obtained by reductive amination of 2,3,4-trimethoxybenzaldehyde
with the appropiate benzhydryl piperazine. In dogs, Lomerizine exerts a potent,
selective and long-lasting vasodilation of cerebral arteries related to a
combination of mechanisms, especially a functional block of L-type voltagesensitive
calcium channels (L-VSCCs). Lomerizine increases cerebral blood flow
compared to peripheral blood flow with only weak effects on systemic arterial
blood pressure. Other mechanisms involved could be blockade of other VSCC
and sodium channels, 5-HT2 and alpha-1 receptors. As a reducing agent of
cortical spreading depression and neurogenic inflammation, Lomerizine was
shown to be useful in migraine. In an open clinical study, it demonstrated
efficacy in the treatment of cluster headache. Moreover, it may have utility in
other neurological diseases such as cerebrovascular ischemia or cerebral
infarction.
Chemical Properties
Colourless Crystalline Solid
Originator
Akzo Nobel (Netherlands)
Uses
A diphenylpiperazine calcium channel blocker. A selective cerebral vasodilator. Antimigraine.
Brand name
Teranas;Migsis
References
1) Ishii?et al. (2009), Inhibitory effect of lomerizine, a prophylactic drug for migraines, on serotonin-induced contraction of the basilar artery; ?J. Pharmacol. Sci. 111 221
2)?Hara et al. (2004), Clinical potential of lomerizine, a Ca2+ channel blocker as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage; Cardiovasc.Drug Rev. 22 199
3)?Ishii et al. (2011), Neuroprotection by lomerizine, a prophylactic drug for migraine, against hydrogen peroxide-induced hippocampal neurotoxicity; Mol. Cell Biochem. 358 1
4) Savigni?et al. (2013), Three Ca2+ channel inhibitors in combination limit chronic secondary degeneration following neurotrauma; ?Neuropharmacology 75 380
5) Tran?et al. (2014), The voltage-gated calcium channel blocker lomerizine is neuroprotective in motor neurons expressing mutant SOD, but not TDP-43; ?J. Neurochem. 130 455
6) O’Hare?et al. (2016), Specific combinations of ion channel inhibitors reduce excessive Ca2+ influx as a consequence of oxidative stress and increase neuronal and glial cell viability in vitro; ?Neuroscience 339 450
