伐地那非的安全性和耐受性

本文回顾了伐地那非治疗勃起功能障碍(erectile dysfunction,ED)的安全性和耐受性,包括其总体安全性、心血管安全性和视觉安全性。临床试验和实际应用的实践经验证明,最常见的不良事件为头痛、颜面潮红和鼻充血,并且多为轻、中度和一过性。无论在一般ED人群中还是在难治性ED人群中,无论是短期还是长期应用,伐地那非均有良好的安全性和耐受性。     

伐地那非治疗难治性勃起功能障碍的最新进展

5型磷酸二酯酶(phosphodiesterase 5,PDE5)在阴茎勃起功能中所起的作用越来越引起人们的关注。环磷酸鸟苷(cGMP)信号通路介导的一氧化氮平滑肌舒张效应是正常勃起功能的必要条件,这个信号通路的下调能引起勃起功能障碍(erectile dysfunction,ED)的许多病理状态,并导致一些慢性疾病的发生。本文回顾了伐地那非治疗ED患者的有效性和安全性。结果表明,伐地那非对于合并异常脂蛋白血症和高血压、糖尿病、抑郁症、前列腺切除术后、外伤性脊髓损伤、西地那非治疗无效、肾移植术后、慢性前列腺炎和早泄的ED患者安全有效,为这些难治性ED患者提供了一种合理的治疗选择。另外,伐地那非还能延长ED患者的勃起时间。     

伐地那非治疗糖尿病患者的勃起功能障碍

勃起功能障碍 (erectiledysfunction ,ED)在糖尿病患者中发生率要高于非糖尿病人群 ,而且更难治疗。伐地那非是一种高选择性的新型磷酸二酯酶 5抑制剂 ,是广泛ED人群的一线治疗药物。最近发表的大型临床试验表明 ,无论糖尿病合并ED的患者基线时的病情严重程度如何 ,也无论他们的血糖控制情况如何 ,伐地那非都能有效地改善其勃起功能 ,而且使用安全 ,耐受性良好     

伐地那非治疗糖尿病患者的勃起功能障碍

勃起功能障碍(erectile dysfunction，ED)在糖尿病患者中发生率要高于非糖尿病人群，而且更难治疗。伐地那非是一种高选择性的新型磷酸二酯酶5抑制剂，是广泛ED人群的一线治疗药物。最近发表的大型临床试验表明，无论糖尿病合并ED的患者基线时的病情严重程度如何，也无论他们的血糖控制情况如何，伐地那非都能有效地改善其勃起功能，而且使用安全，耐受性良好。     

伐地那非对肾阳虚、肾阴虚及肝气郁结型勃起功能障碍的疗效分析

目的:观察伐地那非对肾阳虚、肾阴虚及肝气郁结型勃起功能障碍(ED)的临床疗效。方法:将124例ED患者按中医辨证分为肾阳虚型ED(44例)、肾阴虚型ED(41例)、肝气郁结型ED(39例),所有患者每天服用伐地那非5 mg,总疗程为8周。结果:伐地那非能显著提高各型ED患者的勃起功能问卷-5(IIEF-5)和勃起质量表(EQS)评分,且各组间比较差别有统计学意义(P<0.01);伐地那非显著提高肾阳虚和肾阴虚型ED患者性交成功百分率(P<0.01),肝气郁结型ED在治疗后性交成功百分率也有明显提高(P<0.05);伐地那非还能显著提高各型ED患者阴茎勃起硬度,3组治疗后总体有效率分别为81.82%、73.17%、43.59%。结论:伐地那非对肾阳虚和肾阴虚型ED患者疗效优于肝气郁结型ED患者。     

难治性勃起功能障碍的研究进展

勃起功能障碍(ED)是一种常见病、多发病。目前主要是首选PDE5抑制剂(PDE5I)治疗,总有效率可达80%,部分患者尤其是伴有糖尿病﹑心血管疾病及前列腺癌根治术后者,单独应用PDE5I效果不佳,称为难治性ED。除了NO-cGMP通路外,勃起与ED的发生过程还涉及多条信号通路(RhoA/Rho激酶、H2S、CO等),复杂的信号网络构成了难治性ED发生的基础,以PDE5I为主的交替治疗、联合治疗等可提高对难治性ED治疗成功率。本文就对PDE5I治疗无效的难治性ED的研究进展作一综述。     

磷酸二酯酶5抑制剂治疗勃起功能障碍的疗效和安全性比较

磷酸二酯酶 5 (PDE 5 )抑制剂西地那非的问世使男性勃起功能障碍 (ED)的治疗手段发生了根本性的改变。1998年以来有 10 0多个国家的 2 0 0 0多万患者使用了西地那非 ,患者的死亡率与总体人群的死亡率差异无显著性。西地那非治疗ED平均有效率达 80 %以上 ,成为治疗ED的首选手段。随着新的PDE 5抑制剂伐地那非和泰地那非在国外先后进入临床使用 ,药物治疗ED有了更多的选择。本文通过比较 3种PDE 5抑制剂的药效学、药动学及不良反应以评价其疗效和安全性。     

关于CONFIRMED研究中伐地那非与西地那非临床疗效的比较

CONFIRMED研究是完全遵循良好试验设计规范进行设计的一项研究。该研究是一项非劣性设计,主要目的是比较伐地那非与西地那非在治疗男性勃起功能障碍(ED)方面患者选择的倾向性,结果表明,总体倾向性伐地那非优于西地那非,尤其在总体满意度、性交满意度及伴侣关系满意度等方面显著优于西地那非。通过比较伐地那非与西地那非的结构,伐地那非的结构更具优势,其5型磷酸二酯酶(PDE5)选择性远远高于西地那非,这是伐地那非临床疗效优于西地那非的分子学基础。本研究提供了伐地那非优于西地那非的临床证据,进一步证实了伐地那非是对ED患者进行治疗的一线药物。     

口服伐地那非治疗勃起功能障碍疗效和安全性的临床研究

目的 :评价伐地那非对男性勃起功能障碍 (ED)患者的疗效和安全性。　方法 :应用随机、双盲、安慰剂平行对照、剂量固定 (5、1 0和 2 0mg)方法 ,对 88例ED患者进行 1 2周的临床研究。　结果 :5、1 0和 2 0mg伐地那非使ED患者达到和维持勃起的临床主要和次要指标均明显高于安慰剂 (P <0 .0 1 ) ;伐地那非各剂量组不良事件发生率高于安慰剂组 ,均为轻至中度 ,呈一过性。　结论 :伐地那非是治疗各种病因导致ED的安全、有效的药物。     

伐地那非治疗高血压患者勃起功能障碍的有效性和安全性

勃起功能障碍(erectile dysfunction,ED)在高血压患者中的发病率明显高于非高血压人群,由于担心联合用药会出现严重不良反应,医生往往不愿为该类患者处方治疗ED的药物。伐地那非是一种新型高选择性磷酸二酯酶5型抑制剂,它对心血管系统的安全性已被多项临床试验所证实。最近进行的一项大型临床研究表明,对于同时服用多种降压药的高血压合并ED患者,伐地那非能够显著改善患者的勃起功能,并且使用安全,尤其对于血压或心率等项指标均未见临床意义的改变。     

Effects of sildenafil and vardenafil treatments on sleep quality and depression in hemodialysis patients with erectile dysfunction

ED is prevalent in hemodialysis (HD) patients, and closely related to poor sleep and depression. Efficacy of treating ED either with sildenafil or vardenafil has been shown to be beneficial in ameliorating concomitant depression in non-HD patients. It is yet to be shown whether treatment of ED with a PDE-5 inhibitor would improve poor sleep in HD patients. We aimed to compare the effects of sildenafil and vardenafil on sleep quality and depression in HD patients with ED. A total of 32 maintenance HD patients with ED randomized into two groups to receive either sildenafil or vardenafil for 4 weeks. After a 2-week washout and a crossover, each group received the other drug for another 4-week period. Sleep quality and depression were evaluated via post-sleep inventory (PSI) and Beck's depression inventory (BDI), respectively, at baseline and at the end of the treatment. Sildenafil and vardenafil both improved PSI and BDI scores significantly compared with pretreatment values. However, there was no difference between sildenafil and vardenafil with respect to these parameters. PDE-5 inhibitors, sildenafil and vardenafil, caused a significant improvement in sleep quality and depression in this cohort of HD patients with ED.     

Safety and efficacy of vardenafil in patients with erectile dysfunction: Result of a bridging study in Japan

AIM: Vardenafil is a selective and highly potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED), with improved selectivity for PDE5 and demonstrated efficacy for improving sexual function in men with ED. The current study investigated the safety and efficacy of this new PDE5 inhibitor in Japanese men with ED. METHODS: This was a prospective, double blind, randomized clinical trial designed to evaluate the efficacy and safety of vardenafil. Following a 4-week treatment-free observation period, 283 eligible patients were randomized to 12 weeks treatment with vardenafil 5 mg, 10 mg, 20 mg, or placebo. Primary efficacy responses were assessed using the scores of Q3 and Q4 of the international index of erectile function (IIEF). RESULTS: All three vardenafil doses showed significantly better improvement than the placebo group in Q3 and Q4 scores of the IIEF questionnaire, either at 12 weeks or at the 'last observation carried forward' (LOCF, P < 0.0001). Q3 scores were improved to 4.06 with vardenafil 5 mg, 4.53 with vardenafil 10 mg, and 4.64 with vardenafil 20 mg, versus 3.17 with placebo. Comparable scores for Q4 were 3.47, 4.15 and 4.31 versus 2.31 for placebo. Up to 86% of patients achieved improved erections as assessed by the global assessment question (GAQ). Reported adverse event rates were 35.3%, 45.3% and 54.5% with vardenafil 5 mg, 10 mg and 20 mg, respectively, versus 21.1% in the placebo group. No serious adverse drug reactions were reported. The most common treatment-emergent adverse events were transient headache, flushing and rhinitis, which were mostly mild. CONCLUSION: Vardenafil is an effective and well-tolerated treatment for ED and provides improvement in key indices of erectile function among Japanese men with ED. The results of our trial show that up to nearly 90% of patients achieve improved erections with the administration of vardenafil.     

舍曲林和伐地那非治疗合并勃起功能障碍的早泄患者的临床观察

目的:评价舍曲林和伐地那非治疗合并勃起功能障碍(ED)的早泄患者的临床疗效和安全性。方法:60例诊断为合并ED的早泄患者随机分为舍曲林组和伐地那非组,每组30例。舍曲林组每天服用舍曲林50 mg,疗程2个月。伐地那非组每次性生活前服用伐地那非10~20 mg,疗程2个月。以治疗前后IIEF-5评分的改变来评价ED治疗效果,以治疗前后阴道内射精潜伏期(IELT)的变化来评价早泄治疗效果。结果:伐地那非组勃起功能改善24例,有效率为80%;而舍曲林组仅8例勃起功能改善,有效率为27%,两者差异有显著性(P<0.05)。伐地那非组早泄改善20例,有效率为67%;而舍曲林组早泄改善12例,有效率为40%,两者差异有显著性(P<0.05)。两组患者中,勃起功能改善者的早泄治疗的有效率均显著高于勃起功能无改善者。两组的不良反应均为轻度,无停药者。结论:对合并ED的早泄患者,改善患者的勃起功能是关键。     

Efficacy and tolerability of vardenafil in Asian men with erectile dysfunction

Aim： To evaluate the efficacy and tolerability of vardenafil, a phosphodiesterase type-5 （PDE-5） inhibitor, in men of Asian ethnicity with erectile dysfunction （ED）. Methods： In this prospective, double-blind, multinational study, Asian men were randomized to receive vardenafil （10 mg） or placebo （4：1 ratio） for 12 weeks. The primary efficacy variables were the International Index of Erectile Function erectile function domain （IIEF-EF）, and Sexual Encounter Profile （SEP） questions related to penetration and intercourse completion. Significant mean improvements were required in all three measures to show positive benefits of vardenafil treatment. Secondary efficacy variables included the Global Assessment Question （GAQ） on erection improvement. Results： Least-squares mean baseline IIEF-EF domain scores （vardenafil 14.6, placebo 13.4） were consistent with moderate ED. After 12 weeks, vardenafil treatment was associated with significant increases from the baseline in IIEF-EF domain scores compared with the placebo （22.4 vs. 14.3; P 〈 0.001）. Vardenafil was associated with significant improvements from baseline in least squares （LS） mean success rates for SEP-2 （vardenafil 82.2 vs. placebo 43.6; P 〈 0.001） and SEP-3 （vardenafil 66.1 vs. placebo 24.0; P 〈 0.001）. Positive GAQ responses were reported by 81.8% of vardenafil recipients vs. 24.3% of placebo recipients. Adverse events were reported by 25.4% of the vardenafil group, the majority mild and transient. Conclusion： Vardenafil （10 mg） is a highly effective and well-tolerated treatment for moderate ED in Asian men. These results add to the increasing amount of data demonstrating the safety and efficacy of vardenafil for the treatment of ED in a range of patient populations.     

同期内使用3种PDE5抑制剂治疗ED的经验

目的:观察与比较同期内使用3种PDE5抑制剂治疗ED患者的疗效,满意情况和不良反应。分析影响患者疗效、接受度、倾向性的因素。方法:11个月在门诊应用3种PDE5抑制剂治疗ED患者331例。使用西地那非134例,他达拉非88例,及伐地那非109例。医师详细指导药物的应用,注意事项,观察的内容等,并互留电话,列表登记、随访。结果:复诊或电话随访时间,结果为:①获得良好的疗效及满意率为西地那非72例(79.12%),他达拉非52例(78.78%),伐地那非63例(81.81%)。②PDE5抑制剂单纯或交叉应用的资料分析显示:青年患者或新婚者,偏好伐地那非;③中青年患者倾向于他达拉非;中老年及较长期应用PDE5抑制剂的患者多选用西地那非。3种PDE5抑制剂用于早泄均有一定疗效。④对不能继续用此类药治疗ED的原因进行了分析,分别为:价高,不治本,效果差,耽心不良反应。结论:①同期3种PDE5抑制剂治疗ED的疗效基本相近。亦各有一些优势和特点。②3种PDE5抑制剂的安全性均好,一般、轻度不良反应相近,中度、特殊的不良反应少,严重不良反应均无发生。③PDE5抑制剂的疗效观察,目前众多的问卷、量表实际均仍以主观的感受为主。对同一个人以相同形式、相同问题、繁简一致阐述,获得的有关疗效满意情况、感受等简易回答是有可比性、可信度和实用性的。     

长期口服小剂量伐地那非治疗按需服药无效ED的疗效观察

目的:评估持续口服小剂量伐地那非治疗按需服药无效的勃起功能障碍(ED)患者的疗效及停药后效果维持状况.方法:将按需服药无效的39例ED患者改用长期口服小剂量伐地那非治疗3个月,在治疗前后及停药后3个月分别记录患者国际勃起功能指数-5(International index of erectile function-5,IIEF-5)评分及患者性生活日记中插入和保持勃起的成功率,并且记录治疗前后夫妻性满意度.结果:本组患者治疗后主要疗效指标均高于治疗前,且治疗前后指标差异有统计学意义(P<0.01);停药后3个月,主要指标仍高于基线水平,且差异有统计学意义(P<0.05).结论:每天口服小剂量伐地那非对约半数(48.6%)按需服药无效的ED患者,可改善勃起功能,且安全、有效.     

Comparable efficacy of once-daily versus on-demand vardenafil in men with mild-to-moderate erectile dysfunction: findings of the RESTORE study

BACKGROUND: Phosphodiesterase (type) 5 (PDE5) inhibitors are currently administered on demand for treatment of erectile dysfunction (ED). Once-daily dosing has been suggested to benefit patients. OBJECTIVE: To determine whether daily vardenafil use provides added clinical benefits to patients compared with on-demand dosing. DESIGN, SETTING, AND PARTICIPANTS: In this placebo-controlled, double-blind, multicentre parallel-group study, men with mild-to-moderate ED were randomised to 24 wk of treatment, followed by a 4-wk washout. INTERVENTION: Patients were randomised to receive once-daily vardenafil 10mg plus on-demand placebo for 12 or 24 wk, or once-daily placebo plus on-demand vardenafil 10mg for 24 wk. MEASUREMENTS: Primary efficacy variable was the between-group difference in change in International Index of Erectile Function-Erectile Function domain (IIEF-EF) score from baseline to end of washout. Secondary variables included change from baseline in proportion of positive respondents to Sexual Encounter Profile questions and in satisfaction with treatment as assessed with the Treatment Satisfaction Scale (TSS). RESULTS AND LIMITATIONS: LS mean changes from baseline in IIEF-EF scores were 2.02, 2.29, and 2.63 for vardenafil 12 wk once daily, 24 wk once daily, and 24 wk on demand, respectively. After washout, the trend was towards improved IIEF-EF scores in the on-demand group (20.58 [+/-0.96]) versus both once-daily groups (12 wk, 19.88 [+/-0.93]; 24 wk, 20.11 [+/-0.94]). Furthermore, there were no significant between-group differences in the percentage of patients with "normal" erectile function. TSS analyses demonstrated no significant differences between treatment groups. This study recruited patients with mild-to-moderate ED; therefore, the results may not be the same as in patients with severe ED. CONCLUSIONS: Once-daily vardenafil did not produce greater sustained effects on EF than on-demand vardenafil in men with mild-to-moderate ED, suggesting that daily dosing of PDE5 inhibitors does not produce sustained clinical benefits beyond cessation of treatment above those observed with on-demand administration.     

Phosphodiesterase type 5 inhibitors for the treatment of erectile dysfunction in patients with diabetes mellitus

Sildenafil, a phosphodiesterase 5 (PDE5) inhibitor, has become a first-line therapy for diabetic patients with erectile dysfunction (ED). The efficacy in this subgroup, based on the Global Efficacy Question, is 56% vs 84% in a selected group of non-diabetic men with ED. Two novel PDE5 inhibitors, tadalafil (Lilly ICOS) and vardenafil (Bayer), have recently completed efficacy and safety clinical trials in 'general' and diabetic study populations and are now candidates for US FDA approval. A summary analysis of the phase three clinical trials of sildenafil, tadalafil and vardenafil in both study populations is presented to provide a foundation on which the evaluation of the role of the individual PDE5 inhibitors for the treatment of patients with ED and DM can be built.