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[新型血管扩张剂莫西赛利治疗心绞痛的测力计研究:与β受体阻滞剂联合应用的价值]

[Ergometric study of a new vasodilator agent in angina: molsidomine. Value of combination with beta-blockaders].

作者信息

Witchitz S, Kolsky H, Moisson P, Valette H

出版信息

Arch Mal Coeur Vaiss. 1981 Apr;74(4):463-71.

PMID:6112971
Abstract

Molsidomine, a new venous vasodilator, was studied in 40 cases of stable angina by ergometric stress testing. 1. In 10 patients, one hour after 2 mg molsidomine sublingually, the work inducing a 1 mm ST depression (WST 1) increased by 94% (p less than 0,05), the total work by 52% (p less than 0,005) and the maximum ST depression (ST max) fell by 45% (p less than 0,01). Resting heart rate was unchanged. There was a mild fall in systemic blood pressure. 2. Molsidomine had a significant synergic effect in 3 groups of 10 patients on betablocker therapy but with ischaemic changes on exercise: a) Molsidomine 1 mg sublingually increased WST 1 by 36% (p less than 0,05); at a 2 mg dosage, by 55% (p less than 0,001). ST max decreased from 2,4 +/- 0,4 mm to 1,3 +/- 0,3 (p less than 0,005) and 1,2 +/- 0,33 (p less than 0,001) respectively. The maximal effect was obtained with 1 mg in 5 out of 10 patients. b) One and three hours after 2 mg Molsidomine sublingually or orally: WST 1 increased from 97% to 110% (p less than 0,005): ST max decreased in similar proportions (p less than 0,005). c) 2 mg Molsidomine and 230 mg isosorbide dinitrate orally were compared after two hours: WST 1 increased by 130% after Molsidomine (p less than 0,005) and by 112% after isosorbide (p less than 0,005). ST max decreased in similar proportions (p less than 0,005). The blood pressure fell less with molsidomine. Molsidomine appeared to be better tolerated than isosorbide. (5 cases of mild headache in 40 patients compared to 4 cases out of 10 patients). The results of a preliminary clinical trial are reported. The association of molsidomine (2 mg per os three times daily) reduced the number of anginal attacks by over 50% in 16 out of 17 patients inadequately controlled by betablockade alone. 3 patients complained of headache at the onset of therapy. The efficacity was comparable and the tolerance better than in 28 patients with isosorbide dinitrate and betablockade, and in 10 patients with nifedipine and betablockade. In conclusion, molsidomine is a venous vasodilator with useful pharmacokinetic properties. It seems to be effective and well tolerated in the treatment of angina whether used alone or in association with betablockers.

摘要

莫生多明是一种新型静脉血管扩张剂,我们通过运动负荷试验对40例稳定型心绞痛患者进行了研究。1. 10例患者舌下含服2毫克莫生多明1小时后,诱发1毫米ST段压低的作功量(WST 1)增加了94%(p<0.05),总作功量增加了52%(p<0.005),最大ST段压低(ST max)下降了45%(p<0.01)。静息心率未变。体循环血压略有下降。2. 在3组接受β受体阻滞剂治疗但运动时有缺血改变的10例患者中,莫生多明有显著的协同作用:a)舌下含服1毫克莫生多明使WST 1增加了36%(p<0.05);剂量为2毫克时,增加了55%(p<0.001)。ST max分别从2.4±0.4毫米降至1.3±0.3(p<0.005)和1.2±0.33(p<0.001)。10例患者中有5例服用1毫克时效果最佳。b)舌下或口服2毫克莫生多明后1小时和3小时:WST 1从97%增加到110%(p<0.005);ST max下降幅度相似(p<0.005)。c)两小时后比较口服2毫克莫生多明和230毫克硝酸异山梨酯:莫生多明后WST 1增加了130%(p<0.005),硝酸异山梨酯后增加了112%(p<0.005)。ST max下降幅度相似(p<0.005)。莫生多明引起的血压下降较小。莫生多明似乎比硝酸异山梨酯耐受性更好。(40例患者中有5例出现轻度头痛,而10例患者中有4例)。报告了一项初步临床试验的结果。莫生多明(每日口服3次,每次2毫克)与β受体阻滞剂联合应用,使17例仅用β受体阻滞剂控制不佳的患者中有16例心绞痛发作次数减少了50%以上。3例患者在治疗开始时抱怨头痛。其疗效相当,耐受性优于28例接受硝酸异山梨酯和β受体阻滞剂治疗的患者以及10例接受硝苯地平和β受体阻滞剂治疗的患者。总之,莫生多明是一种具有有益药代动力学特性的静脉血管扩张剂。无论是单独使用还是与β受体阻滞剂联合使用,它在治疗心绞痛方面似乎都是有效且耐受性良好的。

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