Cox D A, Leader J P, Milson J A, Singleton W
Br J Clin Pharmacol. 1986;21 Suppl 1(Suppl 1):83S-90S. doi: 10.1111/j.1365-2125.1986.tb02858.x.
Doxazosin is a long-acting selective alpha 1-adrenoceptor antagonist which has been shown to be effective and well tolerated in the treatment of hypertension given in once-daily doses as monotherapy for up to 1 year or as an adjunct to thiazide or beta-adrenoceptor blockers. Doxazosin has a pharmacokinetic profile in both young adult and elderly subjects which is compatible with once-daily administration. This has been confirmed by measurement of steady state pharmacokinetics in patients receiving long-term doxazosin therapy. In controlled double-blind studies involving approximately 550 patients on doxazosin 1-16 mg once daily, significant reductions in both standing and supine BP were maintained throughout the 24 h dosing interval. Effectiveness of doxazosin in terms of BP lowering and proportion of responders was similar to that achieved with hydrochlorothiazide 25-100 mg once daily, atenolol 50-100 mg once daily, nadolol 40-160 mg once daily, metoprolol 100-200 mg per day given twice daily, or prazosin 1-20 mg per day given twice daily. Doxazosin was as effective in elderly patients as in the younger age group and was as effective in blacks as in caucasians. Doxazosin was well tolerated. Side-effects were generally mild to moderate in severity. Overall incidence, including postural effects early in treatment, was similar to that seen with the comparative agents. In comparison with placebo, doxazosin favourably increased (P less than 0.05) the HDL/total cholesterol ratio.(ABSTRACT TRUNCATED AT 250 WORDS)
多沙唑嗪是一种长效选择性α1肾上腺素受体拮抗剂,已证明其作为单一疗法每日一次给药治疗高血压长达1年有效且耐受性良好,也可作为噻嗪类或β肾上腺素受体阻滞剂的辅助药物。多沙唑嗪在年轻成年人和老年受试者中的药代动力学特征均适合每日一次给药。接受长期多沙唑嗪治疗患者的稳态药代动力学测量已证实了这一点。在涉及约550例患者、每日一次服用1 - 16 mg多沙唑嗪的对照双盲研究中,在整个给药间隔24小时内,站立位和仰卧位血压均显著降低。多沙唑嗪在降低血压方面的有效性和反应者比例与每日一次服用25 - 100 mg氢氯噻嗪、每日一次服用50 - 100 mg阿替洛尔、每日一次服用40 - 160 mg纳多洛尔、每日两次服用100 - 200 mg美托洛尔或每日两次服用1 - 20 mg哌唑嗪相似。多沙唑嗪在老年患者中的疗效与年轻年龄组相似,在黑人中的疗效与白种人相似。多沙唑嗪耐受性良好。副作用一般为轻度至中度。总体发生率,包括治疗早期的体位性影响,与对照药物相似。与安慰剂相比,多沙唑嗪有利地提高了(P<0.05)高密度脂蛋白/总胆固醇比值。(摘要截短至250字)