PDE-5 Inhibition and Sexual Response: Pharmacological Mechanisms and Clinical Outcomes

Raymond C. Rosen*, Kevin E McKenna

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

65 Scopus citations

Abstract

Phosphodiesterase type-5 (PDE-5) inhibitors are a new class of vasoactive drugs that have been developed for treatment of erectile dysfunction (ED). The mechanism of action involves active inhibition of the PDE-5 enzyme and resulting increase in cyclic guanosine monophosphate (cGMP) and smooth muscle relaxation in the penis. Sildenafil citrate (Viagra) is a potent and selective PDE-5 inhibitor, which is the first drug in this class to be approved for treatment of ED. More than 10 million men worldwide have been treated with this drug. Sildenafil has been shown to be generally effective in the treatment of ED, although the degree of efficacy varies according to the etiology and severity of the disorder. The drug is well tolerated, with relatively few contraindications (e.g., nitrates) and safety risks. The cardiovascular effects of sildenafil, in particular, have been extensively investigated. The results of recent studies suggest that sildenafil may have an additional role in the treatment of other male and female sexual disorders, such as premature ejaculation and female sexual arousal disorder, although results to date are inconclusive. Two additional agents in this class (tadalafil [Cialis], vardenafil [Levitra]) have been developed recently and are under regulatory review. Tadalafil is a long-acting PDE-5 inhibitor, which is effective for up to 36 hr in the majority of men. Vardenafil has a similar duration of action to sildenafil, but is more potent and selective biochemically. Both drugs appear to be generally safe and well tolerated, with a similar side-effect profile to sildenafil. There are no controlled comparison studies to date. 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. The potential impact on societal attitudes toward sexuality and sexual dysfunction also warrants consideration.

Original languageEnglish (US)
Pages (from-to)36-88
Number of pages53
JournalAnnual Review of Sex Research
Volume8
StatePublished - Dec 1 2002

Keywords

  • Erectile dysfunction
  • Erection
  • Female sexual dysfunction
  • Penis
  • Phosphodiesterase type-5 inhibitor
  • Sildenafil
  • Tadalafil
  • Vardenafil

ASJC Scopus subject areas

  • Sociology and Political Science
  • Psychology(all)

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