伐地那非的药效学和药代动力学

Pharmacodynamics and Pharmacokinetics of Vardenafil in Patients with Erectile Dysfunction

伐地那非是一种强效、高选择性的 5型磷酸二酯酶 (PDE5 )抑制剂 ,对PDE5的抑制作用约为西地那非的 10倍。该药能显著增强阴茎勃起功能 ;而且起效迅速 ,患者口服后最早 10min即可充分勃起完成性交 ,是迄今为止起效最快的PDE5抑制剂。伐地那非口服绝对生物利用度为 15 % ,可被迅速吸收 ,血浆清除半衰期约为 4～ 5h。药效学、药代动力学、安全性及耐受性研究表明 ,伐地那非是一个治疗ED的安全、有效的口服药物。

Vardenafil is a potent and highly selective phosphodiesterase type 5 (PDE5) inhibitor with a potency about 10-fold higher than sildenafil. Vardenafil can significantly improve erectile function and works rapidly. Vardenafil is a PDE5 inhibitor with the fastest onset of action among its kind so far found and works as early as 10 minutes after oral administration, providing patients with penile erection sufficient to complete an intercourse. The absolute oral bioavailability is about 15%. Vardenafil is rapidly absorbed with a median t max of 0.7 h and a terminal half-life(t 1/2) of more than 4 h. The observed pharmacodynamic properties, pharmacokinetic characteristics and good safety and tolerability profile showed that vardenafil treatment provides an effective and generally well tolerated treatment for ED.