Weber M A, Brewer D D, Drayer J I, Aronow W S, Lipson J L, Ricci B A
Clin Pharmacol Ther. 1982 May;31(5):572-8. doi: 10.1038/clpt.1982.80.
Trimazosin was given for periods of at least 6 mo to 25 patients with mild to moderate essential hypertension. In doses of 300 to 900 mg dialy trimazosin alone led to blood pressure control (supine diastolic blood pressure less than 90 mm Hg with a fall of at least 10 mm Hg) in 16 patients (64%). Despite the decrements in blood pressure there were no changes in body weight or creatinine clearance. There was also no changes in plasma renin activity or urinary aldosterone excretion rate. Although patients with high control renin values appeared to have greater blood pressure decreases than those with low renin values, responsiveness to treatment was not associated with consistent effects of trimazosin on the renin-angiotensin system. Trimazosin induced a small decrease in plasma total cholesterol concentration. In seven patients whose blood pressures were not controlled by trimazosin alone, the addition of polythiazide led to decreased blood pressure and in five control of pressure was achieved. Thus, trimazosin is an effective antihypertensive when given by itself or in combination with a diuretic. Its mechanism of action has not been established, but its ability to induce vasodilation without concomitant sodium retention or stimulation of the renin axis may be an important factor in its effectiveness.
将曲马唑嗪给予25例轻度至中度原发性高血压患者，用药时间至少6个月。每日剂量为300至900毫克的曲马唑嗪单药治疗使16例患者（64%）血压得到控制（仰卧位舒张压低于90毫米汞柱，且至少下降10毫米汞柱）。尽管血压有所下降，但体重和肌酐清除率并无变化。血浆肾素活性和尿醛固酮排泄率也没有改变。虽然肾素值高的患者似乎比肾素值低的患者血压下降幅度更大，但治疗反应性与曲马唑嗪对肾素 - 血管紧张素系统的持续作用无关。曲马唑嗪使血浆总胆固醇浓度略有下降。在7例单用曲马唑嗪血压未得到控制的患者中，加用多噻嗪后血压下降，5例患者血压得到控制。因此，曲马唑嗪单用或与利尿剂联合使用时是一种有效的抗高血压药物。其作用机制尚未明确，但它能够在不伴有钠潴留或刺激肾素轴的情况下诱导血管舒张，这可能是其有效性的一个重要因素。
