Wilde M I, Fitton A, McTavish D
Adis International Limited, Auckland, New Zealand.
Drugs. 1993 Mar;45(3):410-29. doi: 10.2165/00003495-199345030-00008.
Alfuzosin, a new quinazoline derivative, acts as a selective and competitive antagonist of alpha 1-adrenoceptor-mediated contraction of prostatic, prostatic capsule, bladder base and proximal urethral smooth muscle, thereby reducing the tone of these structures. Consequently, urethral pressure and resistance, bladder outlet resistance, bladder instability and symptoms associated with benign prostatic hyperplasia are reduced. A limited range of clinical studies have shown oral alfuzosin to be more effective than placebo (in studies of < or = 6 months duration), to have sustained effects on long term administration (< or = 30 months), and to be comparable with the alpha 1-adrenoceptor antagonist prazosin, in the symptomatic treatment of benign prostatic hyperplasia. This is reflected in increases in urinary flow rate and decreases in symptom score and residual urinary volume. The most marked improvements occur in patients with severe pretreatment urinary flow abnormalities. Furthermore, preliminary results suggest a beneficial effect of alfuzosin on quality of life in patients with benign prostatic hyperplasia. The overall incidence of adverse effects appears similar to that with placebo, and the incidence of vasodilatory-related adverse effects appears lower than that with prazosin. The relative selectivity of alfuzosin for alpha 1-adrenoceptors in the genitourinary tract compared with receptors in the vasculature is a potential advantage over other alpha-adrenoceptor antagonists, including prazosin, as the symptoms of benign prostatic hyperplasia may be reduced by alfuzosin at doses that have minimal vasodilatory effects, thereby minimising postural hypotension and syncope. However, vasodilatory-related adverse effects are the most common adverse effects that occur with alfuzosin, and dose and first-dose hypotensive relationships, especially in the elderly, cannot be excluded at this stage in the clinical use of alfuzosin. The full potential of alfuzosin in the symptomatic treatment of benign prostatic hyperplasia will be clarified by further long term comparative studies (with large patient numbers) against placebo and other alpha 1-adrenoceptor antagonists. Nevertheless, oral alfuzosin 7.5 to 10 mg/day in divided doses appears to be a promising first-line agent for symptomatic treatment of noncomplicated mild to moderate benign prostatic hyperplasia in patients with a high dynamic component to their obstruction. In addition, alfuzosin offers an alternative to prostatectomy (the current 'gold standard') in patients who require surgery but are unfit for this treatment, and in patients requiring symptomatic relief while awaiting surgery.
阿夫唑嗪是一种新型喹唑啉衍生物，可作为α1肾上腺素能受体介导的前列腺、前列腺包膜、膀胱底部和近端尿道平滑肌收缩的选择性竞争性拮抗剂，从而降低这些结构的张力。因此，尿道压力和阻力、膀胱出口阻力、膀胱不稳定性以及与良性前列腺增生相关的症状都会减轻。有限的临床研究表明，口服阿夫唑嗪比安慰剂更有效（在持续时间≤6个月的研究中），长期给药（≤30个月）有持续效果，并且在良性前列腺增生的症状治疗中与α1肾上腺素能受体拮抗剂哌唑嗪相当。这表现为尿流率增加、症状评分降低和残余尿量减少。最显著的改善出现在治疗前尿流异常严重的患者中。此外，初步结果表明阿夫唑嗪对良性前列腺增生患者的生活质量有有益影响。不良反应的总体发生率似乎与安慰剂相似，与血管舒张相关的不良反应发生率似乎低于哌唑嗪。与血管系统中的受体相比，阿夫唑嗪对泌尿生殖道中α1肾上腺素能受体的相对选择性是其相对于其他α肾上腺素能受体拮抗剂（包括哌唑嗪）的潜在优势，因为阿夫唑嗪可以在具有最小血管舒张作用的剂量下减轻良性前列腺增生的症状，从而将体位性低血压和晕厥降至最低。然而，与血管舒张相关的不良反应是阿夫唑嗪最常见的不良反应，在阿夫唑嗪的临床使用现阶段，不能排除剂量和首剂低血压关系，尤其是在老年人中。通过进一步针对安慰剂和其他α1肾上腺素能受体拮抗剂的长期比较研究（纳入大量患者），将阐明阿夫唑嗪在良性前列腺增生症状治疗中的全部潜力。尽管如此，对于梗阻动态成分高的非复杂性轻度至中度良性前列腺增生患者，每日口服7.5至10毫克阿夫唑嗪，分剂量服用似乎是一种有前景的一线症状治疗药物。此外，对于需要手术但不适合这种治疗的患者，以及在等待手术期间需要症状缓解的患者，阿夫唑嗪为前列腺切除术（当前的“金标准”）提供了一种替代方案。
