Corpus ID: 26355489

Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction.

  title={Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction.},
  author={Mitradev Boolell and Michael J. Allen and Stephen A. Ballard and Samuel Gepi-Attee and Gary J. Muirhead and Alasdair M. Naylor and I H Osterloh and Clive Gingell},
  journal={International journal of impotence research},
  volume={8 2},
Sildenafil (Viagra, UK-92,480) is a novel oral agent under development for the treatment of penile erectile dysfunction. Erection is dependent on nitric oxide and its second messenger, cyclic guanosine monophosphate (cGMP). However, the relative importance of phosphodiesterase (PDE) isozymes is not clear. We have identified both cGMP- and cyclic adenosine monophosphate-specific phosphodiesterases (PDEs) in human corpora cavernosa in vitro. The main PDE activity in this tissue was due to PDE5… Expand
The pharmacology of sildenafil, a novel and selective inhibitor of phosphodiesterase (PDE) type 5.
  • R. Wallis
  • Medicine, Chemistry
  • Nihon yakurigaku zasshi. Folia pharmacologica Japonica
  • 1999
These studies have shown that sildenafil is a potent and selective inhibitor of PDE5 and enhances the effect of nitric oxide on the corpus cavernosum and has been shown to be an effective oral treatment of erectile dysfunction. Expand
Effect of the selective phosphodiesterase type 5 inhibitor sildenafil on erectile dysfunction in the anesthetized dog.
By inhibiting cyclic guanosine monophosphate-specific phosphodiesterase type 5, sildenafil augments the neuronal mechanism responsible for penile erection and explains the significant improvements reported in the rigidity and duration of erections seen in patients with erectile dysfunction who have been treated with oral sildanafil. Expand
Effects of sildenafil on the relaxation of human corpus cavernosum tissue in vitro and on the activities of cyclic nucleotide phosphodiesterase isozymes.
The data support the proposal that enhancement of penile erection by sildenafil in patients with erectile dysfunction involves potentiation of the NO-stimulated cGMP signal mediating relaxation of cavernosal smooth muscle during sexual stimulation. Expand
Overall cardiovascular profile of sildenafil citrate.
Overall treatment with sildenafil for up to 1 year is well tolerated and is associated with a low incidence of adverse events that result in discontinuation of treatment in <3% of patients, which is generally consistent with the experience observed during clinical development. Expand
Phosphodiesterase type 5 inhibitor differentiation based on selectivity, pharmacokinetic, and efficacy profiles
Although the various PDE5 inhibitors differ with respect to selectivity and pharmacokinetic profiles, efficacy and safety of these agents are comparable in broad populations of men with erectile dysfunction, including those with diabetes or those taking multiple antihypertensive agents. Expand
PDE-5 Inhibition and Sexual Response: Pharmacological Mechanisms and Clinical Outcomes
Despite the overall effectiveness of PDE-5 inhibitors in the treatment of ED, significant psychological and interpersonal issues need to be addressed in their clinical use. Expand
Phosphodiesterase type 5 as a pharmacologic target in erectile dysfunction.
The scientific rationale of pharmacologically inhibiting phosphodiesterase type 5 (PDE5) in the treatment of erectile dysfunction (ED) is reviewed and selective inhibition of PDE5 is a rational therapeutic approach, as proved by the clinical success of sildenafil. Expand
Synergistic effects of BAY 60-4552 and vardenafil on relaxation of corpus cavernosum tissue of patients with erectile dysfunction and clinical phosphodiesterase type 5 inhibitor failure.
Despite downregulation of the NO/cGMP/PKG pathway, combining BAY 60-4552 with vardenafil significantly enhanced relaxation HCC strips of PDE5-i nonresponders. Expand
Safety and efficacy of sildenafil citrate in the treatment of male erectile dysfunction.
Sildenafil was associated with statistically significant improvement in erectile function compared with placebo and is contraindicated in men who are taking organic nitrates, because of the potential for a precipitous decrease in blood pressure. Expand
Pharmacological characterization of a novel phosphodiesterase type 5 (PDE5) inhibitor lodenafil carbonate on human and rabbit corpus cavernosum.
Lodenafil carbonate was more potent to inhibit the cGMP hydrolysis in PDE extracts compared with lodenfil and sildenafils, indicating that lodenafIL carbonate works as a prodrug. Expand