Godin M, Fillastre J P, Bret M
Nouv Presse Med. 1978 Dec;7(45):4139-41.
Prazosine, a derivative of quinazoline, acts by relaxing the smooth vascular muscles and blocking postsynaptic alpha-adrenoreceptors. A special protocol was used to treat arterial hypertension in 21 subjects. A small dose (0.5 mg) was given the first day to avoid orthostatic hypotension, then 0.5 mg x 3 on days 2, 3 and 4, followed by 1 mg x 3 on subsequent days. Dosage can be progressively increased up to 30 mg/day. During the first 36 days of treatment, prazosine was given alone. A significant drop in systolic and diastolic arterial pressure was observed in the reclining subject. The effect on orthostatic pressures were nevertheless significantly lower than before initiating treatment. Prazosine induces only a slight increase plasma renin activity. In 9 patients the use of prazosine alone at 3 to 6 mg per day produced not only a drop in arterial pressure but its normalization. In 5 other patients, the administration of prazosine associated with a beta-blocker, acebutolol, induced normalization of arterial pressure. The association of prazosine with a thiazide diuretic was not considered successful. In 5 patients, treatment was interrupted with the appearance of coronary insufficiency, orthostatic hypotension and frequent headaches. Minor side-effects observed in 8 others patients did not require interruption of treatment. Based on the above results, it can be stated that prazosine is an efficient new peripheral vasodilator with good patient tolerance for the treatment of arterial hypertension.
哌唑嗪是一种喹唑啉衍生物,其作用机制是舒张血管平滑肌并阻断突触后α-肾上腺素能受体。采用一种特殊方案对21名受试者进行动脉高血压治疗。第一天给予小剂量(0.5毫克)以避免体位性低血压,然后在第2、3和4天给予0.5毫克×3次,随后几天给予1毫克×3次。剂量可逐渐增加至30毫克/天。在治疗的前36天,单独使用哌唑嗪。在卧位受试者中观察到收缩压和舒张压显著下降。然而,对体位性血压的影响明显低于开始治疗前。哌唑嗪仅使血浆肾素活性略有增加。在9名患者中,每天单独使用3至6毫克哌唑嗪不仅使动脉压下降,而且使其恢复正常。在另外5名患者中,哌唑嗪与β受体阻滞剂醋丁洛尔联合使用使动脉压恢复正常。哌唑嗪与噻嗪类利尿剂联合使用未被认为成功。在5名患者中,由于出现冠状动脉供血不足、体位性低血压和频繁头痛而中断治疗。在另外8名患者中观察到的轻微副作用不需要中断治疗。基于上述结果,可以说哌唑嗪是一种有效的新型外周血管扩张剂,对动脉高血压治疗具有良好的患者耐受性。