Lehmann G, Reiniger G, Beyerle A, Zeitler H, Rudolph W
Department of Cardiology, German Heart Centre, Munich.
Eur J Clin Pharmacol. 1995;48(2):109-14. doi: 10.1007/BF00192734.
We investigated the extent and duration of the haemodynamic effects of two regimens of molsidomine, i.e. two tablets of a standard regimen consisting of 4 mg given 6 h apart and one tablet of 16 mg in sustained-release form once daily in 13 patients with chronic congestive heart failure using a placebo-controlled, randomized, double-blind and crossover protocol over a period of 12 h. Both regimens significantly affected systolic, mean and diastolic pulmonary arterial pressure (reductions of up to 15%), right atrial pressure (reductions of up to 35%) and total pulmonary resistance (reductions of up to 18%). The lower dose achieved its maximum action after about 1 h and remained effective for 2 h, whereas the higher dose in sustained-release form showed maximal efficacy at 2 h and remained active even at 12 h. In contrast, only minor changes in arterial blood pressure, systemic vascular resistance and cardiac output were observed on both regimens, almost exclusively at 2 h. Heart rate was not affected by either of the regimens tested. Neither regimen led to any untoward adverse effects. Thus, molsidomine is a potent vasodilating agent which, apart from its effects on preload, also acts on pulmonary arterial and right atrial pressures, leaving systemic circulation largely unaffected on the regimens tested. Administered on its own, it is therefore suitable for treatment of congestive heart failure.
我们采用安慰剂对照、随机、双盲和交叉试验方案,对13例慢性充血性心力衰竭患者使用两种莫西赛明给药方案(即标准方案两片,每6小时服用4毫克;以及缓释片每日一次,每次一片16毫克),观察12小时内血液动力学效应的程度和持续时间。两种方案均显著影响收缩期、平均和舒张期肺动脉压(最多降低15%)、右心房压(最多降低35%)和总肺阻力(最多降低18%)。较低剂量在约1小时后达到最大作用,持续有效2小时,而较高剂量的缓释片在2小时时显示最大疗效,甚至在12小时时仍有活性。相比之下,两种方案仅在2小时时几乎仅观察到动脉血压、全身血管阻力和心输出量有轻微变化。两种测试方案均未影响心率。两种方案均未导致任何不良副作用。因此,莫西赛明是一种强效血管扩张剂,除了对前负荷有影响外,还作用于肺动脉压和右心房压,在所测试的方案中对体循环影响不大。因此,单独使用它适合治疗充血性心力衰竭。