Briganti Alberto, Salonia Andrea, Gallina Andrea, Suardi Nazareno, Rigatti Patrizio, Montorsi Francesco
Cattedra di Urologia, University Vita e Salute-San Raffaele, Milan, Italy.
Expert Opin Emerg Drugs. 2004 May;9(1):179-89. doi: 10.1517/eoed.9.1.179.32954.
Erectile dysfunction (ED) is a common medical condition that affects the sexual life of millions of men worldwide. Many drugs are now available for the treatment of ED, with oral pharmacotherapy representing the first-line option for most patients. Sildenafil citrate, an inhibitor of the enzyme phosphodiesterase type 5 (PDE5), is the most widely prescribed oral agent and has a very satisfactory efficacy-safety profile in all patient categories. Tadalafil (Cialis; Eli Lilly & Co., ICOS) and vardenafil (Levitra; Bayer Pharmaceuticals, GlaxoSmithKline) are new PDE5 inhibitors that have recently been approved worldwide. Both have been associated with significant positive efficacy-safety profiles. Apomorphine sublingual is a dopamine D1 and D2 receptor agonist, which has been approved for marketing in Europe. It is best selected for treating patients with mild-to-moderate ED, but it is seldom used in clinical practice due to its limited efficacy and side effects, particularly nausea. Patients who do not respond to oral pharmacotherapy or who are unable to use it are appropriate candidates for intracavernosal and intraurethral therapy. The efficacy of second-line treatment is high, but the attrition rate remains significant. For the purpose of this review, clinical and pharmacological analysis focuses on the recent advances in the field of oral therapy, including PDE5 inhibitors and sublingual apomorphine.
勃起功能障碍(ED)是一种常见的医学病症,影响着全球数百万男性的性生活。目前有许多药物可用于治疗ED,口服药物治疗是大多数患者的一线选择。枸橼酸西地那非是一种5型磷酸二酯酶(PDE5)抑制剂,是处方最广泛的口服药物,在所有患者类别中都具有非常令人满意的疗效-安全性。他达拉非(希爱力;礼来公司,ICOS)和伐地那非(艾力达;拜耳制药公司,葛兰素史克)是最近在全球范围内获批的新型PDE5抑制剂。两者都具有显著的积极疗效-安全性。阿扑吗啡舌下片是一种多巴胺D1和D2受体激动剂,已在欧洲获批上市。它最适合用于治疗轻度至中度ED患者,但由于其疗效有限且有副作用,尤其是恶心,在临床实践中很少使用。对口服药物治疗无反应或无法使用口服药物的患者适合进行海绵体内和尿道内治疗。二线治疗的疗效很高,但脱落率仍然很高。出于本综述的目的,临床和药理学分析聚焦于口服治疗领域的最新进展,包括PDE5抑制剂和舌下阿扑吗啡。