Babamoto K S, Hirokawa W T
Department of Pharmaceutical Services, UCLA Medical Center 90024.
Clin Pharm. 1992 May;11(5):415-27.
The physicochemical properties, pharmacology, pharmacokinetics, cardiovascular and metabolic effects, adverse effects, dosage, and administration of doxazosin are described, and comparative clinical studies of doxazosin therapy in patients with mild to moderate hypertension are reviewed. Doxazosin mesylate, an alpha 1-adrenoceptor antagonist, is rapidly absorbed after oral administration and undergoes extensive hepatic metabolism. The drug decreases blood pressure by reducing peripheral resistance. Maximum hypotensive effects occur four to eight hours after the dose. Doxazosin favorably affects serum lipids by increasing concentrations of high-density lipoprotein (HDL) cholesterol, increasing the HDL:total cholesterol ratio, and decreasing concentrations of low-density lipoprotein cholesterol, total cholesterol, and triglycerides. In comparative clinical trials, doxazosin lowered standing and supine systolic and diastolic blood pressures as effectively as other alpha-adrenoceptor antagonists, beta-adrenoceptor antagonists, diuretics, angiotensin-converting-enzyme inhibitors, and calcium-channel-blocking agents. The most frequently reported adverse effects are dizziness, headache, nausea, lethargy, and fatigue. Doxazosin may be used either alone or in combination with a beta-adrenoceptor inhibitor or a diuretic. Orthostatic hypotension after the first dose occurs infrequently and may be minimized by initiating therapy at a dosage of 1 mg/day. The dosage may be increased at two-week intervals as needed, and blood pressure should be closely monitored. Doxazosin has blood-pressure-lowering effects comparable to those of other alpha 1-adrenoceptor inhibitors and to those of antihypertensives in other drug classes.
本文描述了多沙唑嗪的理化性质、药理学、药代动力学、心血管及代谢作用、不良反应、剂量及用法，并综述了多沙唑嗪治疗轻至中度高血压患者的比较临床研究。甲磺酸多沙唑嗪是一种α1肾上腺素受体拮抗剂，口服后吸收迅速，并经历广泛的肝脏代谢。该药物通过降低外周阻力来降低血压。给药后4至8小时出现最大降压效果。多沙唑嗪通过增加高密度脂蛋白（HDL）胆固醇浓度、提高HDL与总胆固醇的比值以及降低低密度脂蛋白胆固醇、总胆固醇和甘油三酯的浓度，对血脂产生有益影响。在比较临床试验中，多沙唑嗪降低站立位和仰卧位收缩压及舒张压的效果与其他α肾上腺素受体拮抗剂、β肾上腺素受体拮抗剂、利尿剂、血管紧张素转换酶抑制剂和钙通道阻滞剂一样有效。最常报告的不良反应是头晕、头痛、恶心、嗜睡和疲劳。多沙唑嗪可单独使用，或与β肾上腺素受体抑制剂或利尿剂联合使用。首剂后发生体位性低血压的情况很少见，通过以1毫克/天的剂量开始治疗可将其降至最低。可根据需要每两周增加一次剂量，并应密切监测血压。多沙唑嗪的降压作用与其他α1肾上腺素受体抑制剂及其他药物类别的抗高血压药物相当。
