Substituted Pyrazolopyridopyridazines as Orally Bioavailable Potent and Selective PDE5 Inhibitors:  Potential Agents for Treatment of Erectile Dysfunction

2003 ◽  
Vol 46 (4) ◽  
pp. 457-460 ◽  
Author(s):  
Guixue Yu ◽  
Helen Mason ◽  
Ximao Wu ◽  
Jian Wang ◽  
Saeho Chong ◽  
...  

2010 ◽  
Vol 7 (11) ◽  
pp. 603-609 ◽  
Author(s):  
Victor Palit ◽  
Ian Eardley


2004 ◽  
Vol 14 (6) ◽  
pp. 1577-1580 ◽  
Author(s):  
Yingzhi Bi ◽  
Patrick Stoy ◽  
Leonard Adam ◽  
Bin He ◽  
John Krupinski ◽  
...  




Medicine ◽  
2018 ◽  
Vol 97 (40) ◽  
pp. e12559 ◽  
Author(s):  
Xiao Li ◽  
Qi Zhao ◽  
Jingshang Wang ◽  
Jisheng Wang ◽  
Hengheng Dai ◽  
...  


2017 ◽  
Vol 96 (7) ◽  
pp. E34-E39 ◽  
Author(s):  
Sertan Öntepeli ◽  
Nuray Bayar Muluk ◽  
Devrim Tuğlu ◽  
Timuçin Şipal

We conducted a prospective study of transient evoked otoacoustic emissions (TEOAEs) and distortion-product otoacoustic emissions (DPOAEs) in men who were taking an oral phosphodiesterase type 5 (PDE5) inhibitor for erectile dysfunction. Our study group was made up of 30 men (60 ears), aged 34 to 60 years (mean: 50.9). They were randomly divided into three groups; 10 men were given sildenafil (Viagra) at 50 mg twice a week, 10 were given tadalafil (Cialis) at 20 mg twice a week, and 10 were given vardenafil (Levitra) at 20 mg twice a week. All patients took their drug for 3 weeks, for a total of 6 tablets for each patient. Audiometric tests and TEOAE and DPOAE measurements were performed before and after treatment. Post-treatment audiometry demonstrated improvement in hearing in all three groups. However, post-treatment TEOAE amplitudes and DPOAE amplitudes differed among the three groups; they were significantly higher in the sildenafil group at 1.0 kHz and the same in the tadalafil group; in the vardenafil group, the DPOAE amplitude was significantly lower at 3.0 kHz while there was no change in the TEOAE amplitude. We speculate that the possible mechanism for these findings is that PDE5 inhibitors block degradation of cyclic guanosine monophosphate (cGMP) and induce dilation of the cochlear microcirculation, resulting in an increase in cochlear blood flow. We also believe that the decrease in DPOAE amplitudes at 3.0 kHz seen in the vardenafil group may be related to an accumulation of nitric oxide/cGMP complex, which is toxic to the cochlea; however, since there was no change in TEOAE amplitude in the vardenafil group, this influence may be minimal. Further studies are needed to obtain a more comprehensive assessment of the effects of PDE5 inhibitors on hearing with the use of higher doses and longer durations of therapy.







2016 ◽  
Vol 88 (2) ◽  
pp. 128 ◽  
Author(s):  
Vincenzo Mirone ◽  
Ferdinando Fusco ◽  
Fabio Parazzini ◽  
Alessandro Zucchi

Introduction: PDE5 inhibitors are the firstline treatment for erectile dysfunction. Although all these drugs share the same mechanism of action, each agent could have different characteristics in terms of selectivity, pharmacokinetics and tolerability profile. Materials and Methods: This manuscript illustrates a project, undertaken by the Italian Society of Urology in order to obtain a “snapshot” of the experience of Italian urologists with the use of PDE5 inhibitors in the clinical practice. This project included a survey, targeting a sample of 136 Italian urologists experienced in the treatment of ED, and the organization of a conference of experts who, based on the findings of the survey, the scientific literature and the clinical experience, would define some recommendations for the use of PDE5 inhibitors in clinical practice with a particular focus on Avanafil, the most recent drug in this class. Results: The following recommendations on the use of Avanafil were issued: 1) In patients who are candidates for the use of Avanafil, it is advisable to use the 200-mg dose from the first administration; 2) When used at the highest dose (200 mg), Avanafil shows a favourable tolerability profile with an efficacy similar to that of other agents; 3) The patient should be instructed to take Avanafil on an empty stomach, i.e., 30-45 minutes before or 2 hours after a meal; 4) The efficacy window of Avanafil is between 30 minutes and 6 hours after dosing, which qualifies this molecule as a new drug with an intermediate duration of action; 5) Avanafil at a dose of 50-100 mg/day may be a therapeutic option in chronic rehabilitation. Conclusions: Among PDE5 inhibitors, Avanafil is a new agent with an intermediate duration of action, characterized by high efficacy and good tolerability even at the highest dose (200 mg).



2010 ◽  
Vol 11 (7) ◽  
pp. 1109-1122 ◽  
Author(s):  
Philip Dorsey ◽  
Christopher Keel ◽  
Meghan Klavens ◽  
Wayne JG Hellstrom


Sign in / Sign up

Export Citation Format

Share Document