Pharmacological profiles and clinical effects of azelnidipine, a long-acting calcium channel blocker.
Azelnidipine (Calblock) is a newly developed dihydropyridine-type calcium antagonist for the treatment of hypertension. In hypertensive animals, a single oral administration of azelnidipine caused a slowly developed and long-lasting hypotensive effect with a little reflex tachycardia. The extent of tachycardia was less with azelnidipine than with other agents of the same class. Long-term administrations of azelnidipine produced a stable antihypertensive effect with a slight decrease in heart rate. The hypotensive effect was preceded by an increase in plasma drug concentration and it persisted even after plasma drug concentration declined to very low levels. In the isolated arteries, the calcium blocking action developed gradually after treatment with azelnidipine and survived for a long period of time after the drug was removed from the bathing solution. These data suggest that the high affinity to vascular tissue contributes to the long-lasting hypotensive effects of this agent. The results from clinical studies in hypertensive patients indicated that once daily administration of azelnidipine achieved stable, 24-h control of blood pressure with no change or a slight decrease in heart rate. Clinical studies also showed a low incidence of adverse events such as headache, facial flush, dizziness, and palpitations. These characteristics make azelnidipine a new generation calcium antagonist that can be used for the treatment of hypertension.
Sada
Toshio
T
Pharmacology and Molecular Biology Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Saito
Hironobu
H
D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D001383:Azetidinecarboxylic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000627:therapeutic use*; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use*; D004095:Dihydropyridines / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use*; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D001383:Azetidinecarboxylic Acid; C061679:azelnidipine