flunarizine

Flunarizine is a selective calcium-entry blocker classified as a calcium channel antagonist. It is primarily used for the prophylaxis of migraine, especially in patients with severe and frequent episodes who have not responded to more common treatments. Flunarizine also has calmodulin binding properties and histamine H1 blocking activity. Its mechanism of action involves inhibiting the influx of extracellular calcium through voltage-dependent P/Q-type and T-type calcium channels, leading to reduced intracellular calcium levels. This results in relaxation of smooth muscle cells, vasodilation (especially in cerebral arteries), decreased peripheral resistance, and reduced blood pressure[1][4][6]. Flunarizine is also used for vertigo (of central or peripheral origin), occlusive peripheral vascular disease, and as an adjunctive therapy in epilepsy resistant to conventional drugs[4][5]. The drug is well absorbed orally (>80%), highly protein-bound (>99%), metabolized mainly by CYP2D6 in the liver, and excreted mostly via bile/feces[4].

Brand names

SibeliumApo-Flunarizine

Other names

flunarizine1-[bis(4-fluorophenyl)methyl]-4-[(E)-3-phenylprop-2-enyl]piperazine