Fach W A, Becker H J
Z Kardiol. 1984 Oct;73(10):613-22.
The dose-effect relation and duration of action of 2 mg, 4 mg and 6 mg molsidomine on ischemic ST-segment depression in the exercise-ECG were determined in a randomized and double-blind acute study of 12 patients with confirmed coronary artery disease. With 2 mg molsidomine a significant reduction in the amount of ischemic ST-depression from 18.0 mm to 8.1 mm, 45% of the baseline-figure, resulted. With 6 mg molsidomine a diminuation of the ST-segment depression from 16.2 mm to 6 mm, approximately 40%, was noted. The significant antianginal effect of 2 mg molsidomine lasted at least 3 hours. After 5 hours an effect was seen only in some patients. 4 mg and 6 mg molsidomine still showed a significant reduction of ST-segment depression after 5 hours. A sufficient antianginal efect over 24 hours is only achieved with a 2-mg dose administered 5-6 times or with a 4-6 mg dose applied 4-5 times daily. The most marked fall in blood pressure was noticed after 6 mg molsidomine. On average, the systolic blood pressure fell 41 mm Hg (22%). Orthostatic reactions were not seen. The maximal dose-dependent plasma levels were 15.8 ng/ml, 30.1 ng/ml and 50.0 ng/ml. A definite, reliable clinical effect was seen in some cases from plasma levels above 2 ng/ml.
在一项针对12例确诊冠心病患者的随机双盲急性研究中,测定了2毫克、4毫克和6毫克吗多明对运动心电图中缺血性ST段压低的剂量效应关系及作用持续时间。给予2毫克吗多明后,缺血性ST段压低量从18.0毫米显著降至8.1毫米,为基线值的45%。给予6毫克吗多明后,ST段压低从16.2毫米降至6毫米,约为40%。2毫克吗多明的显著抗心绞痛作用至少持续3小时。5小时后仅在部分患者中观察到作用。4毫克和6毫克吗多明在5小时后仍显示ST段压低显著降低。每日给予2毫克剂量5 - 6次或4 - 6毫克剂量4 - 5次才能在24小时内实现足够的抗心绞痛效果。给予6毫克吗多明后观察到最明显的血压下降。平均收缩压下降41毫米汞柱(22%)。未观察到体位性反应。最大剂量依赖性血浆水平分别为15.8纳克/毫升、30.1纳克/毫升和50.0纳克/毫升。血浆水平高于2纳克/毫升时,在某些病例中可观察到明确、可靠的临床效果。