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[泌尿外科中5型磷酸二酯酶(PDE5)抑制的基础]

[The basics of phosphodiesterase type 5 (PDE5) inhibition in urology].

作者信息

Becker A J, Uckert S, Stief C G

机构信息

Urologische Klinik & Poliklinik, Klinikum Grosshadern, Medizinische Fakultät, Ludwig-Maximilians-Universität (LMU) München, Marchioninistrasse 15, 81377 München.

出版信息

Urologe A. 2008 Dec;47(12):1582-7. doi: 10.1007/s00120-008-1797-z.

DOI:10.1007/s00120-008-1797-z
PMID:18854969
Abstract

Phosphodiesterase (PDE) isoenzymes hold a central role in controlling levels of the cyclic nucleotide monophosphates cyclic AMP and cyclic GMP, which are important second messengers in many transmitter pathways involved in regulating biological processes in urogenital tissues. The development of the PDE5 inhibitors Sildenafil (Viagra), Vardenafil (Levitra), and Tadalafil (Cialis), combining a high response rate and the advantage of on-demand intake, is the result of the scientific characterization of the physiology of penile erectile smooth muscle.The introduction of these compounds as safe and well-tolerated orally active drugs for the treatment of erectile dysfunction has not only become a worldwide clinical success, but it provided the basis for the development and introduction of several new therapeutic modalities into the management of male and female sexual dysfunction. It has also brought further attention to cyclic nucleotide phosphodiesterases as putative pharmacological targets in a variety of disorders, such as pulmonary arterial hypertension, Raynaud's disease, Peyronie's disease, the so-called benign prostatic syndrome, endothelial dysfunction, disturbances of male ejaculatory function (premature ejaculation), and female sexual dysfunction.Because the concept of taking a pill to cure an illness or relieve disease symptoms has become widely accepted by consumers, pharmacological research and development is focusing primarily on selective orally available drugs that influence peripheral intracellular or central regulatory mechanisms. This review briefly describes the current and evolving advances in the field of PDE5 pharmacotherapy in urology and other fields of medicine.

摘要

磷酸二酯酶(PDE)同工酶在控制环核苷酸单磷酸(环磷酸腺苷和环磷酸鸟苷)水平方面起着核心作用,环磷酸腺苷和环磷酸鸟苷是许多参与调节泌尿生殖组织生物过程的递质途径中的重要第二信使。PDE5抑制剂西地那非(伟哥)、伐地那非(艾力达)和他达拉非(希爱力)的研发,结合了高有效率和按需服用的优势,是阴茎勃起平滑肌生理学科学表征的成果。这些化合物作为治疗勃起功能障碍的安全且耐受性良好的口服活性药物被引入,不仅在全球范围内取得了临床成功,还为在男性和女性性功能障碍管理中开发和引入几种新的治疗方式奠定了基础。它还进一步引起了人们对环核苷酸磷酸二酯酶作为多种疾病(如肺动脉高压、雷诺病、佩罗尼氏病、所谓的良性前列腺综合征、内皮功能障碍、男性射精功能障碍(早泄)和女性性功能障碍)潜在药理学靶点的关注。由于服药治病或缓解疾病症状的观念已被消费者广泛接受,药理学研究和开发主要集中在影响外周细胞内或中枢调节机制的选择性口服可用药物上。本综述简要介绍了泌尿外科及其他医学领域中PDE5药物治疗领域的当前进展和不断发展的情况。

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本文引用的文献

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A randomised, placebo-controlled study to assess the efficacy of twice-daily vardenafil in the treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia.一项随机、安慰剂对照研究,旨在评估每日两次服用伐地那非治疗良性前列腺增生继发下尿路症状的疗效。
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Female sexual dysfunction: what's new?女性性功能障碍:有哪些新进展?
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Sildenafil citrate improves erectile function and urinary symptoms in men with erectile dysfunction and lower urinary tract symptoms associated with benign prostatic hyperplasia: a randomized, double-blind trial.枸橼酸西地那非可改善伴有良性前列腺增生相关勃起功能障碍和下尿路症状男性的勃起功能及尿路症状:一项随机双盲试验。
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Potential future options in the pharmacotherapy of female sexual dysfunction.女性性功能障碍药物治疗未来可能的选择。
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Potency and selectivity of vardenafil: a phosphodiesterase Type 5 inhibitor.伐地那非的效力和选择性:一种5型磷酸二酯酶抑制剂。
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Sildenafil: efficacy, safety, tolerability and mechanism of action in treating erectile dysfunction.西地那非:治疗勃起功能障碍的疗效、安全性、耐受性及作用机制
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Udenafil, a long-acting PDE5 inhibitor for erectile dysfunction.优地那非,一种用于治疗勃起功能障碍的长效磷酸二酯酶5抑制剂。
Curr Opin Investig Drugs. 2006 Jul;7(7):661-9.
10
Update on phosphodiesterase (PDE) isoenzymes as pharmacologic targets in urology: present and future.磷酸二酯酶(PDE)同工酶作为泌尿外科药理学靶点的最新进展:现状与未来
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