Zamboulis C, Reid J L
Clin Pharmacol Ther. 1980 Dec;28(6):715-21. doi: 10.1038/clpt.1980.226.
The effects of oral guanfacine were examined in six patients with essential hypertension. Guanfacine caused a substantial fall in both lying and standing systolic and diastolic blood pressure. The fall in pressure was evident by 6 hr, maximal by 10 to 12 hr, and lasted as long as 36 hr. In four patients satisfactory blood pressure control throughout the day was achieved during inpatient administration with single daily doses of 2 to 4 mg in the evening. The other two patients required twice-daily dosing for optimal control of blood pressure. There was no evidence of tolerance to the hypotensive effect. Sedation and xerostomia were apparent after the first dose but did not limit dose titration. Guanfacine lowered lying and standing plasma norepinephrine; this continued on long-term dosing. Urinary catecholamines were reduced from 59.21 +/- 17.24 (mean +/- SEM) to 28.91 +/- 4.20 micrograms/24 hr after 7 days of treatment. The hemodynamic effects, side effects, and biochemical evidence of reduced sympathetic activity after guanfacine resembled the centrally acting antihypertensive clonidine, although guanfacine appeared to have a longer duration of action.
对6例原发性高血压患者进行了口服胍法辛的疗效研究。胍法辛使卧位和立位收缩压及舒张压均显著下降。血压下降在6小时时明显，10至12小时时达到最大，持续长达36小时。4例患者在住院期间每晚单次服用2至4毫克，全天血压控制良好。另外2例患者需要每日两次给药以实现血压的最佳控制。没有证据表明对降压作用产生耐受性。首次给药后出现镇静和口干，但不影响剂量滴定。胍法辛降低了卧位和立位血浆去甲肾上腺素水平；长期给药时这种作用持续存在。治疗7天后，尿儿茶酚胺从59.21±17.24（平均值±标准误）降至28.91±4.20微克/24小时。胍法辛治疗后降低交感神经活性的血流动力学效应、副作用和生化证据与中枢性抗高血压药可乐定相似，尽管胍法辛的作用持续时间似乎更长。
