Lund-Johansen Per, Kirby Roger S
Dept. of Heart Diseases, Institute of Medicine, Haukeland Sykehus, Norway.
Blood Press Suppl. 2003 May;1:5-13. doi: 10.1080/08038020310000078.
Doxazosin is an effective treatment for patients with hypertension, benign prostatic hyperplasia (BPH) and the two comorbidly. In its standard formulation, doxazosin requires a multistep titration regimen to minimize a possible first-dose effect. A new extended-release gastrointestinal therapeutic system (GITS) formulation of doxazosin was developed to improve the pharmacokinetic profile of the parent compound and to reduce or eliminate the need for dose titration and the potential risk of overdosing. This review presents an analysis of the effect of doxazosin GITS monotherapy on blood pressure (BP) and tolerability, as evaluated in four clinical trials, two conducted in patients with stage 1 to stage 2 hypertension and two in patients with BPH with different levels of BP. Doxazosin GITS was as effective as doxazosin standard and more effective than placebo was in reducing and controlling BP in patients with hypertension. Among normotensive patients with BPH, no clinically significant effect on BP was observed and no episodes of syncope were recorded. Doxazosin GITS was generally better tolerated than doxazosin standard, based on the proportion of patients with adverse events and those withdrawing due to adverse events. Moreover, the GITS formulation eliminated the need for titration in most patients. Doxazosin GITS is an effective and well-tolerated treatment in patients with hypertension and/or BPH and without heart failure or clinical coronary heart disease and has advantages over doxazosin standard in terms of a simpler dosing regimen and improved tolerability.
多沙唑嗪是治疗高血压、良性前列腺增生（BPH）以及这两种疾病合并存在患者的有效药物。在其标准制剂中，多沙唑嗪需要多步滴定方案以将可能的首剂效应降至最低。一种新的多沙唑嗪缓释胃肠道治疗系统（GITS）制剂被开发出来，以改善母体化合物的药代动力学特征，并减少或消除剂量滴定的需求以及过量用药的潜在风险。本综述分析了四项临床试验中评估的多沙唑嗪GITS单药治疗对血压（BP）和耐受性的影响，其中两项试验针对1至2期高血压患者，另外两项针对不同血压水平的BPH患者。在高血压患者中，多沙唑嗪GITS在降低和控制血压方面与多沙唑嗪标准制剂效果相当，且比安慰剂更有效。在血压正常的BPH患者中，未观察到对血压有临床显著影响，也未记录到晕厥发作。基于发生不良事件的患者比例以及因不良事件退出治疗的患者比例，多沙唑嗪GITS的耐受性总体上优于多沙唑嗪标准制剂。此外，GITS制剂使大多数患者无需进行滴定。多沙唑嗪GITS是治疗高血压和/或BPH且无心力衰竭或临床冠心病患者的一种有效且耐受性良好的药物，在给药方案更简单和耐受性改善方面优于多沙唑嗪标准制剂。
