Lehmann H U, Witt E, Hochrein H
Med Klin. 1977 Jul 15;72(28-29):1203-8.
Compound BQ 22-708 is a pyridopyridazine with marked antihypertensive effects on experimentally induced hypertension. At this study hemodynamic reactions were controlled in 5 patients with resistent hypertension, two of them with the complication of hypertensive, two of them with the complication of hypertensive crisis, after oral administration of a mean dose of 11 mg BQ 22-708 (range 5 to 15 mg). Mean arterial pressure was reduced by 40 mm Hg. The onset of drug activity occurred 10 to 20 minutes after application. Maximum was reached after 90 to 180 minutes, whereas the antihypertensive effect lasted for about 5 to 6 hours. Peripheral resistance was reduced by about 50%. Heart rate and cardiac output increased. In patients with normal cardiac function stroke volume remained constant, whereas in patients with heart insufficiency an increase occurred. BQ 22-708 led to a slight reduction in pulmonary artery pressure and pulmonary capillary wedge pressure. Right atrial mean pressure remained unchanged. Additional treatment with a beta-adrenergic-blocking-agent or a drug with Ca-antagonistic-activities is indicated for inhibition of BQ-related increase of heart-rate.
化合物BQ 22 - 708是一种吡啶并哒嗪,对实验性诱导的高血压具有显著的降压作用。在本研究中,对5例顽固性高血压患者进行了血流动力学反应监测,其中2例伴有高血压并发症,2例伴有高血压危象并发症,口服平均剂量为11 mg的BQ 22 - 708(范围为5至15 mg)后进行观察。平均动脉压降低了40 mmHg。用药后10至20分钟出现药物活性起效。90至180分钟后达到最大效果,而降压作用持续约5至6小时。外周阻力降低了约50%。心率和心输出量增加。在心脏功能正常的患者中,每搏输出量保持不变,而在心力衰竭患者中则增加。BQ 22 - 708导致肺动脉压和肺毛细血管楔压略有降低。右心房平均压保持不变。为抑制与BQ相关的心率增加,建议加用β - 肾上腺素能阻滞剂或具有钙拮抗活性的药物进行治疗。