Akashi A, Chiba T, Suzuki I, Hashimoto H
Arch Int Pharmacodyn Ther. 1978 Sep;235(1):134-46.
Antihypertensive and pharmacological properties of budralazine were examined in comparison with other antihypertensive drugs. Budralazine was orally effective against various types of hypertension in rats and it, like reserpine but unlike hydralazine, produced a much greater pressure reduction in hypertensive than in normotensive rats. The drug was similar to reserpine and alpha-methyldopa but not to hydralazine in showing a gradually progressive action. At equihypotensive oral doses, budralazine was less potent than hydralazine in producing tachycardia in unrestrained SHR. After long-term therapy, it effectively prevented the development of hypertension in SHR to almost the same extent as did hydralazine. Budralazine failed to produce diuresis in SHR at antihypertensive doses but antagonized isolated rabbit aortic contractions induced by vasoconstrictors and decreased femoral arterial resistance in dogs. Thus, the antihypertensive budralazine is characterized by the ability to produce vasodilator, non-diuretic and weak cardiac stimulant effects.
将布屈嗪的抗高血压和药理特性与其他抗高血压药物进行了比较研究。布屈嗪对大鼠的各种类型高血压口服有效,并且与利血平一样,但与肼屈嗪不同的是,它在高血压大鼠中产生的降压作用比在正常血压大鼠中更大。该药物与利血平和α-甲基多巴类似,但与肼屈嗪不同,呈现出逐渐进展的作用。在等降压口服剂量下,布屈嗪在未束缚的自发性高血压大鼠(SHR)中引起心动过速的效力低于肼屈嗪。长期治疗后,它能有效预防SHR高血压的发展,其程度与肼屈嗪几乎相同。布屈嗪在抗高血压剂量下未能在SHR中产生利尿作用,但能拮抗血管收缩剂诱导的离体兔主动脉收缩,并降低犬股动脉阻力。因此,具有抗高血压作用的布屈嗪的特点是具有产生血管舒张、无利尿作用和微弱心脏刺激作用的能力。