Plosker G L, Brogden R N
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1996 Nov;9(5):379-95. doi: 10.2165/00002512-199609050-00008.
Serenoa repens (Permixon) has been available for several years for the treatment of men with benign prostatic hyperplasia (BPH). The drug is the n-hexane lipidosterolic extract of the dwarf American palm (also known as Serenoa repens) and is a complex mixture of various compounds. A number of pharmacodynamic effects have been demonstrated with the lipidosterolic extract of Serenoa repens (LSESR), suggesting multiple mechanisms of action including in vitro inhibition of both type 1 and type 2 isoenzymes of 5 alpha-reductase and interference with binding of dihydrotestosterone to cytosolic androgen receptors in prostate cells. In controlled clinical trials in men with BPH, oral administration of Serenoa repens 160 mg twice daily for 1 to 3 months was generally superior to placebo in improving subjective symptoms, such as dysuria, as well as objective parameters. The frequency of nocturia was reduced by 33 to 74%, while urinary frequency during the day decreased by 11 to 43% and peak urinary flow rate increased by 26 to 50% with Serenoa repens. Corresponding values for placebo were 13 to 39%, 1 to 29% and 2 to 35%. The only large comparative trial conducted to date, in which > 1000 men with moderate BPH were randomised to receive Serenoa repens 160 mg twice daily or finasteride 5 mg once daily for 6 months, demonstrated similar efficacy between the two drugs. No statistically significant difference was demonstrated between treatment groups for improvement in patient self-rated quality-of-life scores and the primary end-point of objective symptom score; International Prostate Symptom Score improved by 37% with Serenoa repens compared with 39% with finasteride. In much smaller comparative trials, few significant differences were demonstrated between Serenoa repens and alpha 1-receptor antagonists, and larger randomised trials of adequate duration are required to better compare the clinical efficacy of these drugs. The most frequently reported adverse events in clinical trials with Serenoa repens have been minor gastrointestinal problems (e.g. nausea and abdominal pain). In conclusion, Serenoa repens is well tolerated and has greater efficacy than placebo and similar efficacy to finasteride in improving symptoms in men with BPH. Although there is a need for further comparative studies, particularly with alpha 2-receptor antagonists, available data indicate that Serenoa repens is a useful alternative to alpha 1-receptor antagonists and finasteride in the treatment of men with BPH.
锯叶棕果实提取物（保前列）已上市数年，用于治疗良性前列腺增生（BPH）男性患者。该药物是矮生美洲棕榈（也称为锯叶棕）的正己烷脂甾醇提取物，是多种化合物的复杂混合物。锯叶棕果实提取物（LSESR）已证实具有多种药效学作用，提示其作用机制多样，包括在体外抑制5α-还原酶1型和2型同工酶，以及干扰二氢睾酮与前列腺细胞胞质雄激素受体的结合。在BPH男性患者的对照临床试验中，口服锯叶棕果实提取物160mg，每日两次，持续1至3个月，在改善主观症状（如排尿困难）以及客观参数方面通常优于安慰剂。服用锯叶棕果实提取物后，夜尿频率降低了33%至74%，白天尿频减少了11%至43%，尿流率峰值增加了26%至50%。安慰剂组的相应数值分别为13%至39%、1%至29%和2%至35%。迄今为止进行的唯一一项大型对照试验，将1000多名中度BPH男性随机分为两组，分别接受锯叶棕果实提取物160mg每日两次或非那雄胺5mg每日一次，治疗6个月，结果显示两种药物疗效相似。治疗组在改善患者自评生活质量评分和客观症状评分的主要终点方面，未显示出统计学上的显著差异；锯叶棕果实提取物组国际前列腺症状评分改善了37%，非那雄胺组为39%。在规模小得多的对照试验中，锯叶棕果实提取物与α1受体拮抗剂之间未显示出显著差异，需要进行更大规模、足够疗程的随机试验，以更好地比较这些药物的临床疗效。锯叶棕果实提取物临床试验中最常报告的不良事件为轻微胃肠道问题（如恶心和腹痛）。总之，锯叶棕果实提取物耐受性良好，在改善BPH男性患者症状方面，其疗效优于安慰剂，与非那雄胺相似。尽管需要进一步的对照研究，特别是与α2受体拮抗剂的对照研究，但现有数据表明，在治疗BPH男性患者方面，锯叶棕果实提取物是α1受体拮抗剂和非那雄胺的有用替代药物。
