The aim of this review study is to elucidate the effects that phosphodiesterase 5 （PDE5） inhibitors exert on spermatozoa motility, capacitation process and on their ability to fertilize the oocyte. Second messenger ...The aim of this review study is to elucidate the effects that phosphodiesterase 5 （PDE5） inhibitors exert on spermatozoa motility, capacitation process and on their ability to fertilize the oocyte. Second messenger systems such as the cAMP/adenylate cyclase （AC） system and the cGMP/guanylate cyclase （GC） system appear to regulate sperm functions. Increased levels of intracytosolic cAMP result in an enhancement of sperm motility and viability. The stimulation of GC by low doses of nitric oxide （NO） leads to an improvement or maintenance of sperm motility, whereas higher concentrations have an adverse effect on sperm parameters. Several in vivo and in vitro studies have been carried out in order to examine whether PDE5 inhibitors affect positively or negatively sperm parameters and sperm fertilizing capacity. The results of these studies are controversial. Some of these studies demonstrate no significant effects of PDE5 inhibitors on the motility, viability, and morphology of spermatozoa collected from men that have been treated with PDE5 inhibitors. On the other hand, several studies demonstrate a positive effect of PDE5 inhibitors on sperm motility both in vivo and in vitro. In vitro studies of sildenafil citrate demonstrate a stimulatory effect on sperm motility with an increase in intracellular cAMP suggesting an inhibitory action of sildenafil citrate on a PDE isoform other than the PDE5. On the other hand, tadalafil＇s actions appear to be associated with the inhibitory effect of this compound on PDE11. In vivo studies in men treated with vardenafil in a daily basis demonstrated a significantly larger total number of spermatozoa per ejaculate, quantitative sperm motility, and qualitative sperm motility; it has been suggested that vardenafil administration enhances the secretory function of the prostate and subsequently increases the qualitative and quantitative motility of spermatozoa. The effect that PDE5 inhibitors exert on sperm parameters may lead to the improvement of the outcome of assi展开更多
目的:评估他达拉非半量(10 mg)隔日口服治疗勃起功能障碍(ED)的疗效。方法:选择158例符合美国国立卫生研究院诊断标准的ED患者,随机分为他达拉非(希爱力)组和复方玄驹胶囊组两组,分别接受3个月的治疗,治疗后各组又随访3个月以上。采用...目的:评估他达拉非半量(10 mg)隔日口服治疗勃起功能障碍(ED)的疗效。方法:选择158例符合美国国立卫生研究院诊断标准的ED患者,随机分为他达拉非(希爱力)组和复方玄驹胶囊组两组,分别接受3个月的治疗,治疗后各组又随访3个月以上。采用勃起功能障碍症状评分(international index of erectilefunction-5,IIEF-5)评估治疗前后及继续随访3个月后各组的疗效,同时比较患者性生活日记中插入成功率和性交中保持勃起至完成性交的成功率。采用焦虑自评量表评价焦虑状态。结果:治疗前两组IIEF-5评分分别为(9.96±4.21)、(9.69±4.35)分,差异无统计学意义(P>0.05)。治疗3个月后IIEF-5评分分别为(20.38±4.18)、(16.08±3.26)分,随访至6个月时IIEF-5评分分别为(18.16±2.31)、(11.98±3.97)分,差异均有统计学意义(P<0.01),而且两组间在治疗后和6个月随访时的评分差异也具有统计学意义(P<0.05)。药物治疗后,患者性生活日记中插入成功率和保持勃起的成功率明显提高,希爱力组高于复方玄驹胶囊组。焦虑评分值两组治疗后明显低于治疗前(P<0.05)。结论:他达拉非隔日半量口服可有效治疗ED,且疗效优于传统中药,可作为临床上的一线治疗方法。展开更多
The International Consultation on Urological Disease have recently published comprehensive conclusions, based on evidence reviewed by eight committees, on aspects of male lower urinary tract symptoms(LUTS). In this re...The International Consultation on Urological Disease have recently published comprehensive conclusions, based on evidence reviewed by eight committees, on aspects of male lower urinary tract symptoms(LUTS). In this review, we summarise the conclusions from fourof the committees, namely, the evidence regarding the epidemiology of male LUTS, patient assessment, nocturia and medical management. It is indisputable that with an expanding and ageing global population the prevalence of male LUTS is likely to increase. Therefore symptom prevention and preservation of quality of life(Qo L) feature highly in the guidelines. There are now a number of different medical options, proven to lead to significant improvements in symptom scores, flow rate and Qo L available to men with LUTS. Metaanalyses have shown the benefits for alpha blockers, antimuscarinics, 5-α reductase and phosphodiesterase-5 inhibitors. High level evidence also exists for combinations of all of the above with alpha blockers and so men with concomitant storage symptoms, prostate volume > 30 mL, PSA > 1.4 or erectile dysfunction may be considered for combination treatment of an alpha blocker with an antimuscarinic, 5-α reductase inhibitor or phosphodiesterase-5 inhibitor respectively. In an era of personalised medicine, appropriate patient selection is likely to provide the key to the most effective clinical management strategy.展开更多
The study was to compare treatment preference, efficacy, and tolerability of sildenafil citrate （sildenafil） and tadalafil for treating erectile dysfunction （ED） in Chinese men na＇ive to phosphodiesterase 5 （PDE...The study was to compare treatment preference, efficacy, and tolerability of sildenafil citrate （sildenafil） and tadalafil for treating erectile dysfunction （ED） in Chinese men na＇ive to phosphodiesterase 5 （PDE5） inhibitor therapies. This multicenter, randomized, open-label, crossover study evaluated whether Chinese men with ED preferred 20-mg tadalafil or 100-mg sildenafil. After a 4 weeks baseline assessment, 383 eligible patients were randomized to sequential 20-mg tadalafil per 100-mg sildenafil or vice versa for 8 weeks respectively and then chose which treatment they preferred to take during the 8 weeks extension. Primary efficacy was measured by Question 1 of the PDE5 Inhibitor Treatment Preference Questionnaire （PITPQ）. Secondary efficacy was analyzed by PITPQ Question 2, the International Index of Erectile Function （IIEF） erectile function （EF） domain, sexual encounter profile （SEP） Questions 2 and 3, and the Drug Attributes Questionnaire. Three hundred and fifty men （91%） completed the randomized treatment phase. Two hundred and forty-two per 350 （69.1%） patients preferred 20-mg tadalafil, and 108/350 （30.9%） preferred lO0-mg sildenafil （P 〈 0.001） as their treatment in the 8 weeks extension. Ninety-two per 242 （38%） patients strongly preferred tadalafil and 37/108 （34.3%） strongly the preferred sildenafil. The SEP2 （penetration）, SEP3 （successful intercourse）, and IIEF-EF domain scores were improved in both tadalafil and sildenafil treatment groups. For patients who preferred tadalafil, getting an erection long after taking the medication was the most reported reason for tadalafil preference. The only treatment-emergent adverse event reported by 〉 2% of men was headache. After tadalafil and sildenafil treatments, more Chinese men with ED na＇ive to PDE5 inhibitor preferred tadalafil. Both sildenafil and tadalafil treatments were effective and safe.展开更多
The introduction of oral phosphodiesterase-5 inhibitors （PDE51s） in the late 1990s and early 2000s revolutionized the field of sexual medicine and PDE51s are currently first-line monotherapy for erectile dysfunction...The introduction of oral phosphodiesterase-5 inhibitors （PDE51s） in the late 1990s and early 2000s revolutionized the field of sexual medicine and PDE51s are currently first-line monotherapy for erectile dysfunction （ED）. However, a significant proportion of patients with complex ED will be therapeutic non-responders to PDE51 monotherapy. Combination therapy has recently been adopted for more refractory cases of ED, but a critical evaluation of current combination therapies is lacking. A thorough PubMed and Cochrane Library search was conducted focusing on the effectiveness of combination therapies for ED in therapeutic non-responders to PDE51 therapy. Journal articles spanning the time period between January 1990 and December 2010 were reviewed. Criteria included all pertinent review articles, randomized controlled trials, cohort studies and retrospective analyses. References from retrieved articles were also manually scanned for additional relevant publications. Published combination therapies include PDE51 plus vacuum erectile device （VED）, intraurethral medication, intracavernosal injection （ICI）, androgen supplement, a-blocker or miscellaneous combinations. Based on this review, some of these combination treatments appeared to be quite effective in preliminary testing. Caution must be advised, however, as the majority of combination therapy articles in the last decade have numerous limitations including study biases and small subject size. Regardless of limitations, present combination therapy research provides a solid foundation for future studies in complex ED management.展开更多
The aim of this systematic review is to determine the comparative effectiveness and safety of phosphodiesterase 5 inhibitors （PDE5-1s） and （x-blockers used alone or combined for the treatment of lower urinary tract...The aim of this systematic review is to determine the comparative effectiveness and safety of phosphodiesterase 5 inhibitors （PDE5-1s） and （x-blockers used alone or combined for the treatment of lower urinary tract symptoms （LUTS） due to benign prostatic hyperplasia （BPH）. An electronic search of PubMed, Cochrane Library and Embase up to January 2014 was performed to identify randomized controlled trials comparing the efficacy and safety of PDE5-Is and （x-blockers for treatment of lower urinary tract symptoms due to benign prostatic hyperplasia, which assessed IPSS score, maximum flow rate, postvoided residual urine, quality of life and Erectile Function （IIEF） score as outcomes. Data were analyzed by fixed or random effect models using Cochrane Collaboration review manager software. A total of 12 studies were included, Our novel data demonstrated that there was a trend that （x-blockers were more efficacious than PDE5-Is on decreasing IPSS score and increasing maximum flow rate. （x-blockers were significantly more effective than PDE5-Is on reduction of postvoided residual urine with a mean difference of 3.67 （95% CI 1.56 to 5.77, P = 0.0006） and PDE5-Is showed greater effect than （x-blockers on increasing IIEF score with a mean difference of 9.82 （95% CI 3.80 to 15.85, P = 0.001）. In conclusion, our novel data demonstrated that PDE5-Is plus ABs ranked the highest on the improvement of LUTS/BPH. PDE5-Is monotherapy was also effective in this kind of disorder except less reduction of PVR than ABs, In addition, both combined- or mono-therapy were safe.展开更多
Introduction: Headaches are a common symptom affecting individuals worldwide, including in the tropical zone, and have been extensively studied in Togo. Phosphodiesterase-5 inhibitors, commonly prescribed for erectile...Introduction: Headaches are a common symptom affecting individuals worldwide, including in the tropical zone, and have been extensively studied in Togo. Phosphodiesterase-5 inhibitors, commonly prescribed for erectile dysfunction, are known to induce headaches, yet there is a lack of research on this topic in sub-Saharan Africa and Togo. Methods: A cross-sectional study conducted from February 1st to June 30th, 2023, including adult patients seeking erectile dysfunction treatment and prescribed PDE-5 inhibitors. Results: A total of 28 patients were included in the study, with an average age of 34.46 ± 7.5 years. The age group of 30 - 39 years was the most represented (53.57%). Among the participants, 67.86% had a history of chronic headaches. During the intake of PDE-5 inhibitors, 71.43% reported the onset of headaches. Among the 19 patients with chronic headaches, 68.42% developed headaches following PDE-5 inhibitor use (RR = 0.88, 95% CI: 0.55 - 1.40, p = 0.484). The characteristics of the induced headaches were similar to the patients’ pre-existing headaches in 78.95% of cases. Additional symptoms included nasal congestion (36.84%) and an urge to have a bowel movement (26.32%). Sildenafil (75.00%) and Tadalafil (25.00%) were the primarily prescribed PDE-5 inhibitors. The incidence of headaches did not significantly differ between the two groups (RR = 1.33, 95% CI: 0.67 - 2.64, p = 0.306). Treatment for the induced headaches involved self-medication with paracetamol (65.00%) and nonsteroidal anti-inflammatory drugs (NSAIDs) (35.00%). Conclusion: Headaches induced by PDE-5 inhibitors are a well-established reality, emphasizing the need for caution and warning in patients with pre-existing headache conditions, while individualized approaches are necessary to address the potential interplay between migraine medications and erectile dysfunction treatments.展开更多
文摘The aim of this review study is to elucidate the effects that phosphodiesterase 5 （PDE5） inhibitors exert on spermatozoa motility, capacitation process and on their ability to fertilize the oocyte. Second messenger systems such as the cAMP/adenylate cyclase （AC） system and the cGMP/guanylate cyclase （GC） system appear to regulate sperm functions. Increased levels of intracytosolic cAMP result in an enhancement of sperm motility and viability. The stimulation of GC by low doses of nitric oxide （NO） leads to an improvement or maintenance of sperm motility, whereas higher concentrations have an adverse effect on sperm parameters. Several in vivo and in vitro studies have been carried out in order to examine whether PDE5 inhibitors affect positively or negatively sperm parameters and sperm fertilizing capacity. The results of these studies are controversial. Some of these studies demonstrate no significant effects of PDE5 inhibitors on the motility, viability, and morphology of spermatozoa collected from men that have been treated with PDE5 inhibitors. On the other hand, several studies demonstrate a positive effect of PDE5 inhibitors on sperm motility both in vivo and in vitro. In vitro studies of sildenafil citrate demonstrate a stimulatory effect on sperm motility with an increase in intracellular cAMP suggesting an inhibitory action of sildenafil citrate on a PDE isoform other than the PDE5. On the other hand, tadalafil＇s actions appear to be associated with the inhibitory effect of this compound on PDE11. In vivo studies in men treated with vardenafil in a daily basis demonstrated a significantly larger total number of spermatozoa per ejaculate, quantitative sperm motility, and qualitative sperm motility; it has been suggested that vardenafil administration enhances the secretory function of the prostate and subsequently increases the qualitative and quantitative motility of spermatozoa. The effect that PDE5 inhibitors exert on sperm parameters may lead to the improvement of the outcome of assi
文摘目的:评估他达拉非半量(10 mg)隔日口服治疗勃起功能障碍(ED)的疗效。方法:选择158例符合美国国立卫生研究院诊断标准的ED患者,随机分为他达拉非(希爱力)组和复方玄驹胶囊组两组,分别接受3个月的治疗,治疗后各组又随访3个月以上。采用勃起功能障碍症状评分(international index of erectilefunction-5,IIEF-5)评估治疗前后及继续随访3个月后各组的疗效,同时比较患者性生活日记中插入成功率和性交中保持勃起至完成性交的成功率。采用焦虑自评量表评价焦虑状态。结果:治疗前两组IIEF-5评分分别为(9.96±4.21)、(9.69±4.35)分,差异无统计学意义(P>0.05)。治疗3个月后IIEF-5评分分别为(20.38±4.18)、(16.08±3.26)分,随访至6个月时IIEF-5评分分别为(18.16±2.31)、(11.98±3.97)分,差异均有统计学意义(P<0.01),而且两组间在治疗后和6个月随访时的评分差异也具有统计学意义(P<0.05)。药物治疗后,患者性生活日记中插入成功率和保持勃起的成功率明显提高,希爱力组高于复方玄驹胶囊组。焦虑评分值两组治疗后明显低于治疗前(P<0.05)。结论:他达拉非隔日半量口服可有效治疗ED,且疗效优于传统中药,可作为临床上的一线治疗方法。
文摘The International Consultation on Urological Disease have recently published comprehensive conclusions, based on evidence reviewed by eight committees, on aspects of male lower urinary tract symptoms(LUTS). In this review, we summarise the conclusions from fourof the committees, namely, the evidence regarding the epidemiology of male LUTS, patient assessment, nocturia and medical management. It is indisputable that with an expanding and ageing global population the prevalence of male LUTS is likely to increase. Therefore symptom prevention and preservation of quality of life(Qo L) feature highly in the guidelines. There are now a number of different medical options, proven to lead to significant improvements in symptom scores, flow rate and Qo L available to men with LUTS. Metaanalyses have shown the benefits for alpha blockers, antimuscarinics, 5-α reductase and phosphodiesterase-5 inhibitors. High level evidence also exists for combinations of all of the above with alpha blockers and so men with concomitant storage symptoms, prostate volume > 30 mL, PSA > 1.4 or erectile dysfunction may be considered for combination treatment of an alpha blocker with an antimuscarinic, 5-α reductase inhibitor or phosphodiesterase-5 inhibitor respectively. In an era of personalised medicine, appropriate patient selection is likely to provide the key to the most effective clinical management strategy.
文摘The study was to compare treatment preference, efficacy, and tolerability of sildenafil citrate （sildenafil） and tadalafil for treating erectile dysfunction （ED） in Chinese men na＇ive to phosphodiesterase 5 （PDE5） inhibitor therapies. This multicenter, randomized, open-label, crossover study evaluated whether Chinese men with ED preferred 20-mg tadalafil or 100-mg sildenafil. After a 4 weeks baseline assessment, 383 eligible patients were randomized to sequential 20-mg tadalafil per 100-mg sildenafil or vice versa for 8 weeks respectively and then chose which treatment they preferred to take during the 8 weeks extension. Primary efficacy was measured by Question 1 of the PDE5 Inhibitor Treatment Preference Questionnaire （PITPQ）. Secondary efficacy was analyzed by PITPQ Question 2, the International Index of Erectile Function （IIEF） erectile function （EF） domain, sexual encounter profile （SEP） Questions 2 and 3, and the Drug Attributes Questionnaire. Three hundred and fifty men （91%） completed the randomized treatment phase. Two hundred and forty-two per 350 （69.1%） patients preferred 20-mg tadalafil, and 108/350 （30.9%） preferred lO0-mg sildenafil （P 〈 0.001） as their treatment in the 8 weeks extension. Ninety-two per 242 （38%） patients strongly preferred tadalafil and 37/108 （34.3%） strongly the preferred sildenafil. The SEP2 （penetration）, SEP3 （successful intercourse）, and IIEF-EF domain scores were improved in both tadalafil and sildenafil treatment groups. For patients who preferred tadalafil, getting an erection long after taking the medication was the most reported reason for tadalafil preference. The only treatment-emergent adverse event reported by 〉 2% of men was headache. After tadalafil and sildenafil treatments, more Chinese men with ED na＇ive to PDE5 inhibitor preferred tadalafil. Both sildenafil and tadalafil treatments were effective and safe.
文摘The introduction of oral phosphodiesterase-5 inhibitors （PDE51s） in the late 1990s and early 2000s revolutionized the field of sexual medicine and PDE51s are currently first-line monotherapy for erectile dysfunction （ED）. However, a significant proportion of patients with complex ED will be therapeutic non-responders to PDE51 monotherapy. Combination therapy has recently been adopted for more refractory cases of ED, but a critical evaluation of current combination therapies is lacking. A thorough PubMed and Cochrane Library search was conducted focusing on the effectiveness of combination therapies for ED in therapeutic non-responders to PDE51 therapy. Journal articles spanning the time period between January 1990 and December 2010 were reviewed. Criteria included all pertinent review articles, randomized controlled trials, cohort studies and retrospective analyses. References from retrieved articles were also manually scanned for additional relevant publications. Published combination therapies include PDE51 plus vacuum erectile device （VED）, intraurethral medication, intracavernosal injection （ICI）, androgen supplement, a-blocker or miscellaneous combinations. Based on this review, some of these combination treatments appeared to be quite effective in preliminary testing. Caution must be advised, however, as the majority of combination therapy articles in the last decade have numerous limitations including study biases and small subject size. Regardless of limitations, present combination therapy research provides a solid foundation for future studies in complex ED management.
基金supported by the National Natural Science Foundation of China(No.82100064)National Key R&D Program of China(No.2018YFA0800600)+2 种基金Key Research and Development Program of Guangdong Province for“Innovative Drug Creation”(No.2019B020201015)Guangdong Innovative Research Team Program(No.2016ZT06Y432)the Natural Science Foundation of Guangdong Province,China(No.2020A1515011302)。
文摘The aim of this systematic review is to determine the comparative effectiveness and safety of phosphodiesterase 5 inhibitors （PDE5-1s） and （x-blockers used alone or combined for the treatment of lower urinary tract symptoms （LUTS） due to benign prostatic hyperplasia （BPH）. An electronic search of PubMed, Cochrane Library and Embase up to January 2014 was performed to identify randomized controlled trials comparing the efficacy and safety of PDE5-Is and （x-blockers for treatment of lower urinary tract symptoms due to benign prostatic hyperplasia, which assessed IPSS score, maximum flow rate, postvoided residual urine, quality of life and Erectile Function （IIEF） score as outcomes. Data were analyzed by fixed or random effect models using Cochrane Collaboration review manager software. A total of 12 studies were included, Our novel data demonstrated that there was a trend that （x-blockers were more efficacious than PDE5-Is on decreasing IPSS score and increasing maximum flow rate. （x-blockers were significantly more effective than PDE5-Is on reduction of postvoided residual urine with a mean difference of 3.67 （95% CI 1.56 to 5.77, P = 0.0006） and PDE5-Is showed greater effect than （x-blockers on increasing IIEF score with a mean difference of 9.82 （95% CI 3.80 to 15.85, P = 0.001）. In conclusion, our novel data demonstrated that PDE5-Is plus ABs ranked the highest on the improvement of LUTS/BPH. PDE5-Is monotherapy was also effective in this kind of disorder except less reduction of PVR than ABs, In addition, both combined- or mono-therapy were safe.
文摘Introduction: Headaches are a common symptom affecting individuals worldwide, including in the tropical zone, and have been extensively studied in Togo. Phosphodiesterase-5 inhibitors, commonly prescribed for erectile dysfunction, are known to induce headaches, yet there is a lack of research on this topic in sub-Saharan Africa and Togo. Methods: A cross-sectional study conducted from February 1st to June 30th, 2023, including adult patients seeking erectile dysfunction treatment and prescribed PDE-5 inhibitors. Results: A total of 28 patients were included in the study, with an average age of 34.46 ± 7.5 years. The age group of 30 - 39 years was the most represented (53.57%). Among the participants, 67.86% had a history of chronic headaches. During the intake of PDE-5 inhibitors, 71.43% reported the onset of headaches. Among the 19 patients with chronic headaches, 68.42% developed headaches following PDE-5 inhibitor use (RR = 0.88, 95% CI: 0.55 - 1.40, p = 0.484). The characteristics of the induced headaches were similar to the patients’ pre-existing headaches in 78.95% of cases. Additional symptoms included nasal congestion (36.84%) and an urge to have a bowel movement (26.32%). Sildenafil (75.00%) and Tadalafil (25.00%) were the primarily prescribed PDE-5 inhibitors. The incidence of headaches did not significantly differ between the two groups (RR = 1.33, 95% CI: 0.67 - 2.64, p = 0.306). Treatment for the induced headaches involved self-medication with paracetamol (65.00%) and nonsteroidal anti-inflammatory drugs (NSAIDs) (35.00%). Conclusion: Headaches induced by PDE-5 inhibitors are a well-established reality, emphasizing the need for caution and warning in patients with pre-existing headache conditions, while individualized approaches are necessary to address the potential interplay between migraine medications and erectile dysfunction treatments.
