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特拉唑嗪。对其药效学和药代动力学特性以及在良性前列腺增生症中的治疗潜力的综述。

Terazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in benign prostatic hyperplasia.

作者信息

Wilde M I, Fitton A, Sorkin E M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs Aging. 1993 May-Jun;3(3):258-77. doi: 10.2165/00002512-199303030-00007.

DOI:10.2165/00002512-199303030-00007
PMID:7686794
Abstract

Terazosin selectively antagonises alpha 1-adrenoceptor-mediated contraction of the prostate, prostatic capsule, proximal urethra and bladder base, and consequently reduces urethral pressure, bladder outlet resistance and urinary symptoms associated with symptomatic benign prostatic hyperplasia. The efficacy of terazosin is reflected in increases in peak urinary flow rate, and reductions in obstructive and irritative symptom scores compared with placebo, and reductions in residual urinary volume from baseline. Clinical improvements begin to occur within 2 weeks and have been sustained for up to 2 years. The most marked treatment effects tend to occur in patients with more severe pretreatment urinary flow abnormalities. The relatively long duration of action of terazosin, allowing once-daily administration, offers a potential clinical advantage over other alpha 1-adrenoceptor antagonists although formal compliance studies have not been reported. Terazosin is generally well tolerated, but caution is recommended at treatment initiation and when dosage adjustments are made due to an increased risk of postural hypotension and related adverse effects at these times; such a risk has also been observed with several other alpha 1-adrenoceptor antagonists. Although publication of clinical trial results with terazosin is still evolving, this drug shows promise in the treatment of patients with mild to moderate symptomatic benign prostatic hyperplasia for whom surgery is not absolutely indicated. Terazosin also shows promise as a nonsurgical treatment alternative in patients with severe symptoms who are unfit for surgery and also in those who are on long waiting lists for surgery.

摘要

特拉唑嗪可选择性拮抗α1 -肾上腺素能受体介导的前列腺、前列腺包膜、尿道近端和膀胱底部的收缩,从而降低尿道压力、膀胱出口阻力以及与有症状的良性前列腺增生相关的泌尿系统症状。与安慰剂相比,特拉唑嗪的疗效体现在最大尿流率增加、梗阻性和刺激性症状评分降低以及残余尿量较基线减少。临床改善在2周内开始出现,并可持续长达2年。最显著的治疗效果往往出现在治疗前尿流异常较严重的患者中。尽管尚未有正式的依从性研究报告,但特拉唑嗪相对较长的作用持续时间允许每日一次给药,这相较于其他α1 -肾上腺素能受体拮抗剂具有潜在的临床优势。特拉唑嗪一般耐受性良好,但在治疗开始时以及因体位性低血压风险增加和此时相关不良反应而进行剂量调整时,建议谨慎用药;其他几种α1 -肾上腺素能受体拮抗剂也观察到了这种风险。尽管关于特拉唑嗪的临床试验结果仍在不断公布,但这种药物在治疗轻度至中度有症状的良性前列腺增生患者(对于这些患者并非绝对需要手术)方面显示出前景。特拉唑嗪在治疗不适于手术的严重症状患者以及那些等待手术时间较长的患者中,作为一种非手术治疗选择也显示出前景。

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