Pharmacodynamics, pharmacokinetics and clinical efficacy of phosphodiesterase-5 inhibitors

ABSTRACT

Introduction: Phosphodiesterase type 5 inhibitors (PDE5Is) are the first-line drugs in the management of erectile dysfunction (ED). However, over the past two decades tremendous efforts have been made to identify new clinical uses of PDE5Is beyond their roles in ED.

Areas covered: Basic science articles, clinical trials, reviews, and meta-analysis published between 1996 and 2015 were searched using MEDLINE (PubMed interface) to collect the most relevant and impactful studies from our perspectives as practicing urologists. This review mainly focuses on the level one evidence-based clinical efficacy and drug-related toxicity of oral PDE5Is. In addition, drug discovery, pharmacokinetics and pharmacodynamics, potential use in other diseases, and future directions are discussed.

Expert opinion: On-demand PED5Is for the treatment of ED has shifted toward chronic administration in a broad spectrum of conditions that are thought to be associated with endovascular health. Several studies have shown that PDE5Is may play a cardioprotective or neuroprotective role. Further studies are under way to verify beneficial effects of PDE5I in non-urological conditions.

KEYWORDS:

• Erectile dysfunction
• pharmacology
• phosphodiesterase 5 inhibitors

Article highlights

• A number of randomized controlled trials have demonstrated the efficacy of PDE5Is for the management of ED with various etiologies.

• Clinical pharmacologic properties, efficacy, and safety profiles of PDE5Is are described.

• The past and current uses of PDE5Is in the urologic fields are mentioned.

• The distinctive mechanism of PDE5Is involving NO/cGMP pathway has been widely investigated as a potential target for the management of both urologic and non-urologic conditions.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Additional information

Funding

This paper was not funded.