Buoninconti R, Motolese M
Int J Clin Pharmacol Ther Toxicol. 1985 Nov;23(11):613-6.
The antihypertensive activity of a new arterial dilator, cadralazine, was evaluated in 40 patients with mild-to-moderate arterial hypertension. Cadralazine was given once daily over 6 weeks, and blood pressure and heart rate were recorded 24-26 hours after dosing. Cadralazine dose was 10 mg daily initially, and 15 or 20 mg daily from the 3rd or 5th trial week according to a target diastolic pressure reduction to 95 mmHg or below. Slow-release metoprolol 200 mg once daily was added when heart rate increase exceeded 25% of the pretreatment value. Blood pressure showed a significant and progressive reduction throughout the study period, both in the patients receiving cadralazine as monotherapy (19 patients) and in those who added metoprolol (21 patients). The target diastolic pressure reduction was reached in 2 patients with the 10-mg dose, in 19 of the remaining 38 patients with the 15-mg dose, and in 13 of the other 19 patients with the 20-mg dose. Considering only those patients who did not add metoprolol, the target was reached in the 2 patients with the 10-mg dose, in 10 of the 19 patients with the 15-mg dose and in 7 of the 19 patients with the 20-mg dose. None of the laboratory tests showed clinically relevant changes. Neither LE cells nor antinuclear antibodies were found. In conclusion, cadralazine is a promising long-acting antihypertensive vasodilator. A clinically satisfactory antihypertensive effect is achieved mostly by a 15-mg or a 20-mg dose given once daily.(ABSTRACT TRUNCATED AT 250 WORDS)
一种新型动脉扩张剂卡屈嗪的降压活性在40例轻至中度动脉高血压患者中进行了评估。卡屈嗪每日给药一次,持续6周,给药后24 - 26小时记录血压和心率。卡屈嗪初始剂量为每日10 mg,从第3或第5个试验周起,根据目标舒张压降至95 mmHg或更低,剂量调整为每日15或20 mg。当心率增加超过治疗前值的25%时,加用每日一次200 mg的缓释美托洛尔。在整个研究期间,无论是接受卡屈嗪单药治疗的患者(19例)还是加用美托洛尔的患者(21例),血压均呈现显著且逐步下降。10 mg剂量组有2例患者达到目标舒张压降低值,其余38例接受15 mg剂量的患者中有19例达到目标值,另外19例接受20 mg剂量的患者中有13例达到目标值。仅考虑未加用美托洛尔的患者,10 mg剂量组的2例患者、19例接受15 mg剂量的患者中的10例以及19例接受20 mg剂量的患者中的7例达到了目标值。所有实验室检查均未显示出临床相关变化。未发现狼疮细胞和抗核抗体。总之,卡屈嗪是一种有前景的长效降压血管扩张剂。每日一次给予15 mg或20 mg剂量大多能取得临床上令人满意的降压效果。(摘要截短至250字)