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药物洞察:用于治疗勃起功能障碍的口服5型磷酸二酯酶抑制剂

Drug Insight: oral phosphodiesterase type 5 inhibitors for erectile dysfunction.

作者信息

Briganti Alberto, Salonia Andrea, Gallina Andrea, Saccà Antonino, Montorsi Piero, Rigatti Patrizio, Montorsi Francesco

机构信息

Department of Urology at Università Vita Salute San Raffaele, Milan, Italy.

出版信息

Nat Clin Pract Urol. 2005 May;2(5):239-47. doi: 10.1038/ncpuro0186.

DOI:10.1038/ncpuro0186
PMID:16474835
Abstract

Erectile dysfunction (ED) is a common medical condition that affects the sexual life of millions of men. At present, first-line oral pharmacotherapy for most patients with ED is a phosphodiesterase type 5 (PDE-5) inhibitor, of which three are currently available worldwide. Sildenafil (Viagra, Pfizer) has a very satisfactory efficacy-safety profile in all patient categories. The first PDE-5 inhibitor to reach the market, it is now the most widely prescribed oral agent for ED. Tadalafil (Cialis, Lilly ICOS) and vardenafil (Levitra, Bayer/GlaxoSmithKline) were introduced to the European Union and the US in 2003 and 2004, respectively. These three PDE-5 inhibitors share many characteristics, but each has unique features. This review describes the chemical, pharmacologic and clinical features of sildenafil, vardenafil and tadalafil as oral first-line treatments for ED. First, we describe the physiology of penile erection and PDE-5 inhibitor pharmacology, including chemistry, PDE selectivity, pharmacokinetics, and possible drug interactions. We then summarize data on the efficacy and safety profiles of the three PDE-5 inhibitors for the treatment of ED in the general population, in patients with diabetes mellitus and in men that have undergone bilateral nerve-sparing retropubic radical prostatectomy.

摘要

勃起功能障碍(ED)是一种常见的医学病症,影响着数百万男性的性生活。目前,大多数ED患者的一线口服药物治疗是5型磷酸二酯酶(PDE-5)抑制剂,目前全球有三种此类药物可供使用。西地那非(万艾可,辉瑞公司)在所有患者类别中都具有非常令人满意的疗效-安全性。作为首个上市的PDE-5抑制剂,它现在是ED最广泛处方的口服药物。他达拉非(希爱力,礼来公司/卫材公司)和伐地那非(艾力达,拜耳公司/葛兰素史克公司)分别于2003年和2004年被引入欧盟和美国。这三种PDE-5抑制剂有许多共同特征,但每种都有独特之处。本综述描述了西地那非、伐地那非和他达拉非作为ED口服一线治疗药物的化学、药理学和临床特征。首先,我们描述阴茎勃起的生理学和PDE-5抑制剂药理学,包括化学、PDE选择性、药代动力学和可能的药物相互作用。然后,我们总结这三种PDE-5抑制剂在普通人群、糖尿病患者以及接受双侧保留神经的耻骨后根治性前列腺切除术的男性中治疗ED的疗效和安全性数据。

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J Sex Med. 2016 May;13(5):860-75. doi: 10.1016/j.jsxm.2016.02.171.
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World J Diabetes. 2013 Aug 15;4(4):124-9. doi: 10.4239/wjd.v4.i4.124.
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