Effects of Benidipine in a Rat Model of Experimental Angina

Abstract

To compare the antianginal eŠects of 1,4-dihydropyridine-type calcium-channel blockers, we evaluated the eŠects of benidipine, amlodipine, nifedipine, and efonidipine on vasopressin-induced myocardial ischemia in rats, an experimental model of angina. Intravenous administration of benidipine (3 mg/kg), amlodipine (1000 mg/kg), and nifedipine (100 mg/kg) suppressed the vasopressin-induced S-wave depression, an index of myocardial ischemia. Efonidipine (100 mg/kg, i.v.) tended to inhibit the S-wave depression. At the antianginal dose of each drug, amlodipine, nifedipine, and efonidipine decreased blood pressure signiˆcantly, whereas benidipine had little eŠect on blood pressure at a dose of 3 mg/kg. These results indicate that benidipine, unlike the other 1,4-dihydropyridine-type calcium-channel blockers examined in this study, inhibits vasopressin-induced coronary vasospasm with fewer undesirable eŠects such as hypotension in rats, suggesting that benidipine may be useful in the treatment of angina pectoris.

Effects of treatment with once-daily nifedipine CR and twice-daily benidipine on prevention of symptomatic attacks in patients with coronary spastic angina pectoris—Adalat Trial vs Coniel in Tokyo against Coronary Spastic Angina (ATTACK CSA)

“…Nifedipine CR was effective in maintaining higher effective blood concentrations for more than 12 h when the administration timing was changed to after the evening meal. However, benidipine, a dihydropyridine Ca channel blocker, the same as nifedipine, has been reported to have coronary dilatation action and sustained action better than those of nifedipine in pharmacological research using various ischemic heart disease models [34,35]. The approved dosage and administration of benidipine for angina pectoris is 4 mg twice a day [22].…”

Nanostructured Lipid Carriers to Enhance the Bioavailability and Solubility of Ranolazine: Statistical Optimization and Pharmacological Evaluations

“…Following vasopressin administration, the ECG alterations (ST segment elevation) were taken into consideration as a metric to show the presence of myocardial ischemia, which may be caused by coronary vasoconstriction [ 55 ]. ST segment elevation was defined as the difference in ST segment amplitude following and immediately before vasopressin delivery [ 56 ]. Four groups of six male Sprague-Dawley rats, each weighing 250–300 g, were used.…”

The possible antianginal effect of allopurinol in vasopressin-induced ischemic model in rats

“…cannula, vasopressin (VP) was intravenously injected at a dosage of 2 IU/kg through the same cannula. The ST-segment depression ⩾ 1 μv was considered as an index of myocardial angina (Ikeda et al, 2006), as shown in which recorded by the Powerlab system (Model Figure). The recorded signals should be free of electrical interference and noise.…”