Bianchetti M G, Weidmann P, Boehringer K, Link L, Schiffl H, Beretta-Piccoli C, Colombo J P
Eur J Clin Pharmacol. 1982;23(6):483-9. doi: 10.1007/BF00637493.
The efficacy and side effects of the new vasodilator carprazidil and the established vasodilator minoxidil were compared in 18 hypertensive patients inadequately controlled by 2 to 4 conventional drugs; the latter included diuretics, beta-blockers and/or sympatholytics and, in half the cases, vasodilators, such as hydralazine, diazoxide or the postsynaptic alpha-blocker prazosin. The vasodilators were withdrawn and, using a crossover design all patients received carprazidil (mean final dose 88 mg) and minoxidil (20 mg) for an average period of 5 to 6 months. The effects of the 2 agents appeared to be qualitatively and quantitatively similar. Both tended to cause sodium retention and an increase in heart rate, which required an increased dose of diuretic in one third of the cases or of a beta-blocker in a quarter. With this approach mean body weight and blood volume were not altered in the established phase of carprazidil or minoxidil treatment; heart rate and plasma norepinephrine tended to be only minimally increased, plasma renin was slightly increased, and plasma aldosterone and epinephrine were largely unchanged. Supine and upright blood pressure were reduced from initial values of 189/113 and 167/ 113 mm Hg, to 149/95 and 138/95 mm Hg (-18 and - 17%), respectively, during carprazidil, and to 154/95 and 141/96 mm Hg (-17 and - 15%) during minoxidil therapy. Hypertrichosis occurred with both agents in almost all patients, and limits their more prolonged use in females. No adverse side effects on haematological parameters, liver or renal function were observed, nor was antinuclear antibody detected. It is concluded that carprazidil and minoxidil are equivalent vasodilator agents in the treatment of severe hypertension, particularly in males.
在18例使用2至4种传统药物治疗效果不佳的高血压患者中,比较了新型血管扩张剂卡普地尔与已有的血管扩张剂米诺地尔的疗效和副作用;这些传统药物包括利尿剂、β受体阻滞剂和/或交感神经阻滞剂,半数患者还使用了血管扩张剂,如肼屈嗪、二氮嗪或突触后α受体阻滞剂哌唑嗪。停用血管扩张剂后,采用交叉设计,所有患者均接受卡普地尔(平均最终剂量88毫克)和米诺地尔(20毫克)治疗,平均疗程为5至6个月。两种药物的效果在质和量上似乎相似。两者均倾向于引起钠潴留和心率增加,三分之一的病例需要增加利尿剂剂量,四分之一的病例需要增加β受体阻滞剂剂量。采用这种方法,在卡普地尔或米诺地尔治疗的稳定期,平均体重和血容量未发生改变;心率和血浆去甲肾上腺素仅略有升高,血浆肾素略有升高,血浆醛固酮和肾上腺素基本未变。卡普地尔治疗期间,仰卧位和直立位血压分别从初始值189/113和167/113毫米汞柱降至149/95和138/95毫米汞柱(-18%和-17%),米诺地尔治疗期间分别降至154/95和141/96毫米汞柱(-17%和-15%)。几乎所有患者使用这两种药物均出现多毛症,限制了其在女性患者中的长期使用。未观察到对血液学参数、肝肾功能的不良副作用,也未检测到抗核抗体。结论是,卡普地尔和米诺地尔在治疗重度高血压方面是等效的血管扩张剂,尤其在男性患者中。