Cilnidipine: a new generation Ca channel blocker with inhibitory action on sympathetic neurotransmitter release.
Cilnidipine is a unique Ca(2+) channel blocker with an inhibitory action on the sympathetic N-type Ca(2+) channels, which is used for patients with hypertension in Japan. Cilnidipine has been clarified to exert antisympathetic actions in various examinations from cell to human levels, in contrast to classical Ca(2+) channel blockers. Furthermore, renoprotective and neuroprotective effects as well as cardioprotective action of cilnidipine have been demonstrated in clinical practice or animal examinations. After the introduction of nifedipine as an antihypertensive drug, many Ca(2+) channel blockers with long-lasting action for blood pressure have been developed to minimize sympathetic reflex during antihypertensive therapy, which have been divided into three groups; namely, first, second, and third generation based on their pharmacokinetic profiles. Since cilnidipine directly inhibits the sympathetic neurotransmitter release by N-type Ca(2+) channel-blocking property, the drug can be expected as fourth generation, providing an effective strategy for the treatment of cardiovascular diseases.
Takahara
Akira
A
Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan. akirat@phar.toho-u.ac.jp
D000320:Adrenergic Fibers / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D000959:Antihypertensive Agents / Q000266:history / Q000627:therapeutic use*; D001794:Blood Pressure / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000009:adverse effects / Q000266:history / Q000627:therapeutic use*; D020864:Calcium Channels, N-Type / Q000187:drug effects* / Q000378:metabolism; D004095:Dihydropyridines / Q000009:adverse effects / Q000266:history / Q000627:therapeutic use*; D049673:History, 20th Century; D049674:History, 21st Century; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D009638:Norepinephrine / Q000378:metabolism*; D012018:Reflex / Q000187:drug effects; D016896:Treatment Outcome
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D004095:Dihydropyridines; C065927:cilnidipine; D009638:Norepinephrine