説明
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.
