Dual L/N-Type Ca Channel Blocker: Cilnidipine as a New Type of Antihypertensive Drug

Cilnidipine is a unique dihydropyridine derivative Ca2+ channel blocker with an inhibitory action on the sympathetic N-type Ca2+ channels (Uneyama et al., 1999a). It has been clarified that cilnidipine exerts antisympathetic actions in various examinations from cell to human levels. Furthermore, its renoprotective, neuroprotective and cardioprotective effects have been demonstrated in clinical practice or animal examinations. After the introduction of nifedipine, many Ca2+ channel blockers with long-lasting action have been synthesized to decline sympathetic reflex during antihypertensive therapy. Based on each pharmacokinetic profile, Ca2+ channel blockers have been divided into three groups; namely, 1st, 2nd, and 3rd generation. Since cilnidipine directly inhibits the sympathetic neurotransmitter release by N-type Ca2+ channel-blocking property, the drug can be expected as 4th generation, providing an effective strategy for the treatment of cardiovascular diseases (Takahara, 2009).