Schultz H S, Chretien S D, Brewer D D, Eltorai M I, Weber M A
J Clin Pharmacol. 1981 Feb-Mar;21(2):65-71. doi: 10.1002/j.1552-4604.1981.tb01751.x.
Lofexidine, a new centrally acting antihypertensive agent, was compared in a double-blind study with clonidine in the treatment of mild (standing diastolic blood pressure 95-104 mm Hg) or moderate (105-129 mm Hg) essential hypertension. In dialy dosages of 0.2 or 0.4 mg, monotherapy with lofexidine produced significant decreases in blood pressure and heart rate that were not different from those with clonidine. Blood pressure and heart rate were not different from those with clonidine. Blood pressure control (supine and standing diastolic pressure less than 90 mm Hg) occurred in seven of eight mild hypertensives treated with lofexidine and in seven of ten treated with clonidine. In moderate hypertension, three of 11 and seven of ten, ten of the 14 responders to clonidine required dosages of 0.4 mg daily or less. The maximum dosage tested was 1.6 mg daily. Concomitant hydrochlorothiazide therapy was given to eight of the lofexidine responders and 12 of the clonidine responders. For both drugs, drowsiness and dry mouth were the chief complaints. Neither agent changed standard clinical biochemistries except for decreased potassium and increased bicarbonate concentrations due to concurrent diuretic therapy. Lofexidine to have clinical characteristics similar to those of clonidine. Each of these agents is best used in lower doses, which are frequently effective and less likely to produce symptomatic complaints.
洛非西定是一种新型的中枢性抗高血压药物,在一项双盲研究中,将其与可乐定用于治疗轻度(站立位舒张压95 - 104 mmHg)或中度(105 - 129 mmHg)原发性高血压进行比较。以每日0.2或0.4 mg的剂量,洛非西定单药治疗可使血压和心率显著降低,与可乐定治疗的效果无差异。血压和心率与可乐定治疗的情况无差异。在接受洛非西定治疗的8例轻度高血压患者中,有7例血压得到控制(仰卧位和站立位舒张压低于90 mmHg),接受可乐定治疗的10例患者中有7例血压得到控制。在中度高血压患者中,11例接受洛非西定治疗的患者中有3例、10例接受可乐定治疗的患者中有7例,14例对可乐定有反应的患者中有10例每日所需剂量为0.4 mg或更低。测试的最大剂量为每日1.6 mg。8例对洛非西定有反应的患者和12例对可乐定有反应的患者同时接受了氢氯噻嗪治疗。两种药物的主要不良反应均为嗜睡和口干。除因同时使用利尿剂导致血钾降低和碳酸氢盐浓度升高外,两种药物均未改变标准临床生化指标。洛非西定具有与可乐定相似的临床特征。这两种药物均以较低剂量使用效果最佳,这些低剂量通常有效且较少引起症状性不良反应。