Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress

2008 ◽  
Vol 17 (6) ◽  
pp. 855-864 ◽  
Author(s):  
Serap Gur ◽  
Suresh C Sikka ◽  
Wayne JG Hellstrom
Keyword(s):  
Oxidative Stress ◽  
Erectile Dysfunction ◽  
Pde5 Inhibitors ◽  
Phosphodiesterase 5

scholarly journals Phenanthrenes from Eulophia macrobulbon as Novel Phosphodiesterase-5 Inhibitors

2017 ◽  
Vol 12 (1) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Prapapan Temkitthawon ◽  
Kanokwan Changwichit ◽  
Nantaka Khorana ◽  
Jarupa Viyoch ◽  
Khanit Suwanborirux ◽  
...  
Keyword(s):  
Pulmonary Hypertension ◽  
Erectile Dysfunction ◽  
Chemical Constituents ◽  
Pde5 Inhibitor ◽  
Pde5 Inhibitors ◽  
New Class ◽  
Phosphodiesterase 5 Inhibitors ◽  
Phosphodiesterase 5

Phosphodiesterase 5 (PDE5) inhibitors can be used for the treatment of erectile dysfunction and pulmonary hypertension. In order to search for new leads of PDE5 inhibitors, we investigated the chemical constituents of the tubers of Eulophia macrobulbon (E.C. Parish & Rchb. f) Hook. f A new phenanthrene, 9,10-dihydro-4-(4′-hydroxybenzyl)-2,5-dimethoxyphenanthrene-1,7-diol (1) and three known phenanthrenes i.e., 1-(4′-hydroxybenzyl)-4,8-dimethoxyphenanthrene-2,7-diol (2), (9,10-dihydro-2,5-dimethoxyphenanthrene-1,7-diol (3) and 1,5,7-trimethoxyphenanthrene-2,6-diol) (4) were isolated. Among these, 2 was the most potent PDE5 inhibitor (IC50 =1.67±0.54 μM) evaluated by the [3H]cGMP radioassay method, whereas 1 showed mild activity (IC50 = 62.3±3.3 μM). Their inhibitory selectivities against PDE5 over PDE6 were also studied. This study suggests phenanthrenes as a new class of PDE5 inhibitors.

Phosphodiesterase 5 Inhibitors for Erectile Dysfunction

2005 ◽  
Vol 39 (7-8) ◽  
pp. 1286-1295 ◽  
Author(s):  
Stephen M Setter ◽  
Jason L Iltz ◽  
Jack E Fincham ◽  
R Keith Campbell ◽  
Danial E Baker
Keyword(s):  
Clinical Trial ◽  
Erectile Dysfunction ◽  
Data Extraction ◽  
Pde5 Inhibitor ◽  
Clinical Trial Data ◽  
Research Review ◽  
Pde5 Inhibitors ◽  
Search Terms ◽  
Review Articles ◽  
Phosphodiesterase 5

OBJECTIVE To review the pharmacologic and clinical trial data of the Food and Drug Administration–approved phosphodiesterase 5 (PDE5) inhibitors for the treatment of erectile dysfunction (ED). DATA SOURCES Primary research and review articles were identified through a search of ScienceDirect, PubMed/MEDLINE, and International Pharmaceutical Abstracts (1990–August 2004). The following search terms were used in the Medicine Dentistry and Pharmacology, Toxicology, and Pharmaceutical Sciences subcategories: phosphodiesterase 5 inhibitor, PDE5 inhibitor, erectile dysfunction, sildenafil, vardenafil, tadalafil, prostatectomy, and diabetes. Web of Science (1990–August 2004) was used to search for additional abstracts using the same search terms as above. The package inserts for sildenafil, vardenafil, and tadalafil were also consulted. STUDY SELECTION AND DATA EXTRACTION All identified research, review articles, and abstracts were assessed for relevance, and all relevant information was included. Priority was given to the primary medical literature and clinical trial reports. DATA SYNTHESIS ED is a common disorder in males with increased prevalence associated with age and presence of cardiovascular disease, prostatectomy, or diabetes mellitus. Sildenafil, vardenafil, and tadalafil are selective PDE5 inhibitors currently available for treatment of ED. Their pharmacology and pharmacokinetics vary slightly, but with potentially important clinical differences in duration of activity; all have similar clinical efficacy and adverse effect profiles in patients with ED of various causes. CONCLUSIONS Sildenafil, vardenafil, and tadalafil are safe and effective PDE5 inhibitors for the treatment of ED.

Cutaneous Reaction to Drugs Used for Erectile Dysfunction: Case Report and Review of the Literature

2006 ◽  
Vol 10 (3) ◽  
pp. 128-130 ◽  
Author(s):  
Renee A. Beach ◽  
Frank Murphy ◽  
Ronald B. Vender
Keyword(s):  
Erectile Dysfunction ◽  
Drug Eruption ◽  
Pde5 Inhibitor ◽  
Sexual Performance ◽  
Pde5 Inhibitors ◽  
Fixed Drug Eruption ◽  
The Past ◽  
Fixed Drug ◽  
Performance Satisfaction ◽  
Phosphodiesterase 5

Background: In the past 9 years, drugs for erectile dysfunction (ED) have been increasingly prescribed for men with erectile difficulty. These drugs, phosphodiesterase 5 (PDE5) inhibitors, help men with ED obtain and sustain an erection, improving both sexual function and sexual performance satisfaction. However, these drugs contain side effects. Objectives: A 56-year-old man developed an erythematous, circle-shaped lesion on his penis. The lesion was recurrent, with evidence of desquamation. The aim was to determine the source of the recurrent lesion based on its morphology and the patient's verbal history. Results: A clinical diagnosis of fixed drug eruption owing to use of the PDE5 inhibitor tadalafil (Cialis) was made. He was not rechallenged with the drug. However, he experienced a subsequent recurrence of the eruption on inadvertent rechallenge. Conclusions: We believe this case to be the first report of this type of reaction owing to tadalafil. Therefore, fixed drug eruption is a newly observable side effect of this drug.

scholarly journals Classical activation of macrophages and vardenafil

2017 ◽  
Vol 131 (11) ◽  
pp. 1141-1145 ◽  
Author(s):  
Richmond Muimo
Keyword(s):  
Cystic Fibrosis ◽  
Erectile Dysfunction ◽  
Pulmonary Arterial Hypertension ◽  
Arterial Hypertension ◽  
Lung Inflammation ◽  
Therapeutic Strategy ◽  
Pde5 Inhibitors ◽  
Transport Defect ◽  
Pulmonary Arterial ◽  
Phosphodiesterase 5

Inhibitors of phosphodiesterase 5 (PDE5) – sildenafil citrate (Viagra; Pfizer) and vardenafil hydrochloride (Levitra; Bayer/GlaxoSmithKline) – approved for the treatment of erectile dysfunction and pulmonary arterial hypertension also rescue the loss of cystic fibrosis (CF) chloride channel function and the mislocalization of F508del-CFTR in affected tissues in CF. Can PDE5 inhibitors provide a therapeutic strategy which combines ability to correct the basic ion transport defect and to control de-regulated lung inflammation in CF?

scholarly journals Evaluation of prescribing pattern of phosphodiesterase-5 inhibitors and assessing effectiveness of sildenafil and tadalafil in patients with erectile dysfunction

2022 ◽  
Vol 8 (4) ◽  
pp. 280-283
Author(s):  
Yatish Byndoor ◽  
Tamilisetti Vidya Sagar ◽  
Sanjay Kumar
Keyword(s):  
Erectile Dysfunction ◽  
Health Care Providers ◽  
Erectile Function ◽  
Phosphodiesterase Inhibitors ◽  
Care Providers ◽  
Pde5 Inhibitors ◽  
Prescribing Pattern ◽  
Therapy Option ◽  
Generic Products ◽  
Phosphodiesterase 5

Several factors may affect identification and treatment of erectile dysfunction by health care providers, this study evaluates prescribing pattern of PDE-5 inhibitors and assess effectiveness of Sildenafil and Tadalafil in patients with erectile dysfunction.This is a descriptive and observational study, observed participants without providing any interventions, after fulfilling inclusion and exclusion criteria, patients were enrolled into study and informed written consent was obtained from all patients, data was obtained from medical records, analysed descriptively. International Index of Erectile Function (IIEF) Questionnaire is used in assessment of erectile dysfunction and treatment outcomes.In our study, 80% of patients were prescribed with phosphodiesterase inhibitors and 20% received nutritional supplements. 80 percent of drugs were prescribed under generic name, subjects treated with Sildenafil/Tadalafil were found to be associated with higher mean scores for questions of International Index of Erectile Function (IIEF). Tadalafil scored high in terms of sexual desire domain.PDE5 inhibitors represent major first-line oral therapy option for men with erectile dysfunction, shift of market from brand to generic products allows more freedom of choice, although multiple reports suggest general equivalency of four major PDE5 inhibitors, tadalafil suggested to be preferable.

The Effect of PDE5 Inhibitors on the Male Reproductive Tract

2020 ◽  
Vol 26 ◽  
Author(s):  
Nikolaos Sofikitis ◽  
Aris Kaltsas ◽  
Fotios Dimitriadis ◽  
Jens Rassweiler ◽  
Nikolaos Grivas ◽  
...  
Keyword(s):  
Male Infertility ◽  
Reproductive Tract ◽  
Tunica Albuginea ◽  
Scientific Data ◽  
Secretory Function ◽  
Pde5 Inhibitors ◽  
Male Reproductive Tract ◽  
Review Study ◽  
Phosphodiesterase 5

The therapeutic range of cyclic nucleotide phosphodiesterase 5 inhibitors (PDE5) inhibitors is getting wider in the last years. This review study focuses on the potential employment of PDE5 inhibitors as an adjunct tool for the therapeutic management of male infertility. The literature tends to suggest a beneficial effect of PDE5 inhibitors on Leydig and Sertoli cells secretory function. It also appears that PDE5 inhibitors play a role in the regulation of the contractility of the testicular tunica albuginea and the epididymis. Moreover scientific data suggest that PDE5 inhibitors enhance the prostatic secretory function leading to an improvement in sperm motility. Other studies additionally demonstrate a role of PDE5 inhibitors in the regulation of sperm capacitation process. Placebo-controlled, randomized, blind studies are necessary to unambiguously incorporate PDE5 inhibitors as an adjunct tool for the pharmaceutical treatment of semen disorders and male infertility.

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