Kurosawa S, Kurosawa N, Owada E, Matsuhashi N, Ito K
J Int Med Res. 1987 May-Jun;15(3):121-7. doi: 10.1177/030006058701500301.
The haemodynamic effects and pharmacokinetics of nifedipine suppositories, used mainly for hypertensive emergencies, were studied in 10 severely hypertensive patients. Following rectal administration, significant hypotensive effects occurred after 0.5 h and lasted until 7 h after administration. The mean (+/- SE) maximum decreases in systolic and diastolic blood pressures 1.5 h after administration were: systolic, 61.8 +/- 7.9 mmHg (P less than 0.001); and diastolic, 30.8 +/- 4.0 mmHg (P less than 0.001). No serious side-effects were reported and heart rate did not change significantly. Mean nifedipine concentration in the blood peaked at 52.4 ng/ml, 1 h after administration and, after 7 h, was still 14.3 ng/ml which is higher than the minimum plasma concentration required for hypotensive effects to occur. There was a close correlation between nifedipine concentration in the blood and hypotensive effects. These results indicate that rectal administration of nifedipine should be regarded as a useful alternative treatment in hypertensive emergencies.
在10例重度高血压患者中研究了主要用于高血压急症的硝苯地平栓剂的血流动力学效应和药代动力学。直肠给药后，0.5小时后出现显著的降压作用，持续至给药后7小时。给药后1.5小时收缩压和舒张压的平均（±标准误）最大降幅分别为：收缩压，61.8±7.9 mmHg（P<0.001）；舒张压，30.8±4.0 mmHg（P<0.001）。未报告严重副作用，心率无明显变化。给药后1小时血中硝苯地平平均浓度达峰值52.4 ng/ml，7小时后仍为14.3 ng/ml，高于产生降压作用所需的最低血浆浓度。血中硝苯地平浓度与降压作用之间存在密切相关性。这些结果表明，直肠给药硝苯地平应被视为高血压急症的一种有用的替代治疗方法。
