Martsevich S Iu, Metelitsa V I, Rumiantsev D O, Piotrovskiĭ V K, Slastnikova I D
Ter Arkh. 1989;61(8):24-7.
The possibility of the development of tolerance to anti-ischemic effects of nifedipine (NF) during chronic administration for 2 months was studied in 15 patients with stable angina pectoris of effort. The duration and degree of the anti-ischemic effect were assessed in terms of similar, individually adjusted exercises performed prior to and repeatedly after NF administration. After acute NF administration the anti-ischemic effect lasting at least 4 h (mean 5.4 +/- 0.4 h) was attained in all the patients. After 2 months of regular NF administration the duration of the NF anti-ischemic effect significantly decreased to 3.9 +/- 0.5 h. In 5 patients, the attenuation of NF efficacy turned out substantial. The study performed 8-10 days after NF withdrawal in those 5 patients revealed partial restoration of the effect. The development of tolerance to NF action was not associated with changes in NF and its metabolite plasma concentrations. NF binding to plasma proteins also remained constant during the study.
在15例稳定型劳力性心绞痛患者中,研究了硝苯地平(NF)连续给药2个月期间产生抗缺血作用耐受性的可能性。根据NF给药前和给药后反复进行的相似的、个体调整的运动,评估抗缺血作用的持续时间和程度。急性给予NF后,所有患者均获得了至少持续4小时(平均5.4±0.4小时)的抗缺血作用。规律给予NF 2个月后,NF抗缺血作用的持续时间显著缩短至3.9±0.5小时。在5例患者中,NF疗效的减弱十分明显。对这5例患者在停用NF 8 - 10天后进行的研究显示,其作用有部分恢复。对NF作用耐受性的产生与NF及其代谢产物的血浆浓度变化无关。在研究期间,NF与血浆蛋白的结合也保持不变。