Amann F W, Bolli P, Bühler F R
Int J Clin Pharmacol Ther Toxicol. 1984 Jan;22(1):13-5.
The new vasodilator Roche 12-4713, an oxodiazolo-pyrimidine with long-acting direct arteriolar dilating properties, was tested in 13 patients (ages 33-66 years, mean 53 +/- 7 SD) previously uncontrolled on a beta blocker-diuretic combination. The addition of Ro 12-4713 (30-180 mg per day) for 134 +/- 62 days resulted in a fall of blood pressure from 191 +/- 24/110 +/- 8 to 150 +/- 23/88 +/- 8 (p less than 0.001) without changes in heart rate (73 +/- 8 vs 74 +/- 11 bpm). Edema occurred in five patients, this was controlled in four by increasing the dose of the diuretic. Hypertrichosis appears to limit the drug's use in females. This new vasodilator proved highly effective in the treatment of severe hypertension. The long duration of action makes once a day administration possible.
新型血管扩张剂罗氏12 - 4713是一种具有长效直接小动脉扩张特性的氧二氮杂环嘧啶,对13名先前使用β受体阻滞剂 - 利尿剂联合治疗未能控制血压的患者(年龄33 - 66岁,平均53±7标准差)进行了测试。添加罗氏12 - 4713(每天30 - 180毫克),持续134±62天,血压从191±24/110±8降至150±23/88±8(p小于0.001),心率无变化(73±8对74±11次/分钟)。5名患者出现水肿,4名通过增加利尿剂剂量得到控制。多毛症似乎限制了该药物在女性中的使用。这种新型血管扩张剂在治疗重度高血压方面证明非常有效。其长效作用使得每日一次给药成为可能。