Lee Jeong Gu, Moon Du Geon, Kang Seok Ho, Cho Dae Yeon, Park Hong Seok, Bae Jae Hyun
Department of Urology, Korea University Medical Center, Seoul, Korea.
Urol Int. 2010;84(2):231-5. doi: 10.1159/000277604. Epub 2010 Mar 4.
To assess the relaxation effect of the phosphodiesterase-5 inhibitor udenafil on the bladder and prostatic urethra and its therapeutic potentials for benign prostatic hyperplasia (BPH)/lower urinary tract symptoms (LUTS).
For the in vitro study, muscle strips from urinary bladder and urethra were prepared from male New Zealand rabbits. The strips were mounted in organ baths and connected to force transducers. After stabilization, maximal tissue contractions were obtained by the addition of phenylepinephrine for urethra strips and carbachol for bladder strips. When the contraction was stabilized, a dose-response curve of udenafil was constructed. For the in vivo study using adult male Sprague-Dawley rats, changes of intravesical pressure and urethral perfusion pressure after intraarterial administration of udenafil were monitored.
Udenafil significantly relaxed the bladder and urethra strips in a dose-dependent manner. At 10(-3) M, udenafil induced a significant relaxation of the bladder strips by 37.3% and of the urethra strips by 44.0%. In the in vivo study, the intercontraction interval was significantly prolonged (p < 0.01) and the duration of urethral relaxation with high-frequency oscillations was significantly prolonged (p < 0.01) after udenafil.
Udenafil had relaxant effects on the bladder and prostatic urethral smooth muscle. Clinically, udenafil could be applied as an effective treatment for BPH/LUTS.
评估磷酸二酯酶-5抑制剂伐地那非对膀胱和前列腺尿道的舒张作用及其对良性前列腺增生(BPH)/下尿路症状(LUTS)的治疗潜力。
在体外研究中,从雄性新西兰兔获取膀胱和尿道的肌条。将肌条安装在器官浴槽中并连接到力传感器。稳定后,通过向尿道肌条添加去氧肾上腺素和向膀胱肌条添加卡巴胆碱来获得最大组织收缩。当收缩稳定后,构建伐地那非的剂量-反应曲线。在使用成年雄性Sprague-Dawley大鼠的体内研究中,监测动脉内给予伐地那非后膀胱内压和尿道灌注压的变化。
伐地那非以剂量依赖性方式显著舒张膀胱和尿道肌条。在10⁻³ M时,伐地那非使膀胱肌条舒张37.3%,尿道肌条舒张44.0%,差异有统计学意义。在体内研究中,给予伐地那非后,收缩间期显著延长(p < 0.01),高频振荡引起的尿道舒张持续时间显著延长(p < 0.01)。
伐地那非对膀胱和前列腺尿道平滑肌有舒张作用。临床上,伐地那非可作为治疗BPH/LUTS的有效药物。