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新型钙拮抗剂西尼地平反复口服给药对二肾一夹肾性高血压犬的降压作用

[Antihypertensive effects of repeated oral administration of cilnidipine, a novel calcium antagonist, in 2K1C renal hypertensive dogs].

作者信息

Takahara A, Uchida H, Konda T, Dohmoto H, Yoshimoto R, Komori M, Morioka T, Ono I, Takata Y, Kato H

机构信息

Life Science Laboratories, Central Research Laboratories, Ajinomoto Co., Inc., Yokohama, Japan.

出版信息

Nihon Yakurigaku Zasshi. 1995 Oct;106(4):279-87. doi: 10.1254/fpj.106.279.

DOI:10.1254/fpj.106.279
PMID:8537075
Abstract

Antihypertensive effects of repeated oral administration of cilnidipine in 2K1C renal hypertensive dogs were compared with those of nicardipine. On the first day, oral administration of cilnidipine (3 mg/kg) or nicardipine (3 mg/kg) markedly lowered both systolic and diastolic blood pressure 1 hr after administration. The hypotensive effects of cilnidipine were longer compared with those of nicardipine. Both drugs elevated the heart rate and plasma renin activity. On the 8th and 15th days, similar responses were obtained by repeated administrations of cilnidipine and nicardipine. After withdrawal of these drugs, no rebound phenomena in blood pressure were observed. The changes in mean blood pressure were correlated with plasma cilnidipine or nicardipine concentrations that were obtained at each time of blood pressure measurement (r = -0.598; P < 0.001 and r = -0.594; P < 0.001, respectively). These results suggest that stable and long-acting antihypertensive effects of cilnidipine for 15 consecutive days in renal hypertensive dogs are related to the change in plasma drug concentrations.

摘要

将西尼地平反复口服给药对2K1C肾性高血压犬的降压作用与尼卡地平进行比较。第一天,口服西尼地平(3mg/kg)或尼卡地平(3mg/kg)后1小时,收缩压和舒张压均显著降低。与尼卡地平相比,西尼地平的降压作用持续时间更长。两种药物均使心率和血浆肾素活性升高。在第8天和第15天,反复给予西尼地平和尼卡地平得到了相似的反应。停用这些药物后,未观察到血压反跳现象。平均血压的变化与每次测量血压时获得的血浆西尼地平或尼卡地平浓度相关(r分别为-0.598;P<0.001和r=-0.594;P<0.001)。这些结果表明,西尼地平在肾性高血压犬中连续15天具有稳定且长效的降压作用与血浆药物浓度的变化有关。

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