Comparison of phosphodiesterase type 5 (PDE5) inhibitors
Comparison of phosphodiesterase type 5 (PDE5) inhibitors
复制标题
DOI：
10.1111/j.1742-1241.2006.01049.x
复制
发表时间：
2006-08-01
影响因子：
2.6
通讯作者：
Wright, P. J.
中科院分区：
文献类型：
--
作者：
Wright, P. J.
在目前可用于治疗勃起功能障碍的选择中，口服 5 型磷酸二酯酶 (PDE5) 抑制剂是推荐的一线治疗方法。本综述比较了目前获得许可的三种 PDE5 抑制剂：柠檬酸西地那非（西地那非）、盐酸伐地那非（伐地那非）和他达拉非。所有三种药物都具有相似的功效和毒性特征。西地那非和伐地那非具有相似的分子结构，但他达拉非在结构上不同，这反映在其药代动力学特征上。就起效而言，据报道，接受西地那非治疗的患者中有 35% 在 14 分钟内实现勃起并成功性交，接受伐地那非治疗的患者中有 21% 在 10 分钟内实现勃起，而接受他达拉非治疗的患者则有 16% 在 16 分钟内实现勃起。西地那非和伐地那非的半衰期均约为 4 小时，但他达拉非的半衰期为 17.5 小时。 PDE5 抑制剂之间的另一个区别是食物，尤其是脂肪食物，会影响西地那非和伐地那非的药代动力学特征，但不会影响他达拉非的药代动力学特征。 PDE5 抑制剂之间的这些药代动力学差异可能是患者偏好的基础，这是 ED 治疗的一个重要且新兴的方面。
Of the current options available to treat erectile dysfunction, oral phosphodiesterase type 5 (PDE5) inhibitors are the recommended first-line treatment. This review compares the three currently licensed PDE5 inhibitors: sildenafil citrate (sildenafil), vardenafil HCl (vardenafil) and tadalafil. All three drugs have similar efficacy and toxicity profiles. Sildenafil and vardenafil have similar molecular structures, but tadalafil is structurally different, which is reflected in its pharmacokinetic profile. With regard to the onset of action, achievement of an erection that leads to successful intercourse has been reported for 35% of patients treated with sildenafil within 14 min, 21% of patients treated with vardenafil within 10 min and 16% of patients treated with tadalafil within 16 min. Sildenafil and vardenafil both have half-lives of approximately 4 h but the half-life of tadalafil is 17.5 h. Another difference between the PDE5 inhibitors is that food, especially fatty food, affects the pharmacokinetic profiles of sildenafil and vardenafil, but not that of tadalafil. These pharmacokinetic differences among the PDE5 inhibitors may underlie patient preference, an important and emerging aspect of ED therapy.