Cardiovascular repercussion of lodenafil carbonate, a new PDE5 inhibitor, with and without alcohol consumption

Arq Bras Cardiol. 2010 Feb;94(2):150-6, 160-7, 152-8.
[Article in English, Portuguese, Spanish]

Abstract

Background: Millions of men around the world suffer from erectile dysfunction, for which phosphodiesterase 5 inhibitors (PDE-5 inhibitors) are currently the first treatment option. Sexual activity and alcohol consumption are closely related, and the simultaneous use of alcohol and PDE-5 inhibitors can happen. Lodenafil carbonate is a new PDE-5 inhibitor, developed by a Brazilian pharmaceutical company.

Objective: This work aimed at evaluating the cardiovascular safety of lodenafil carbonate, with and without simultaneous alcohol consumption.

Methods: Fifteen male volunteers received 160 mg lodenafil carbonate (LC), in three different moments. Participants were assigned to three groups, treated with LC in fasting condition, with alcohol or receiving only placebo. The volunteers were continuously monitored during 24 hours for physical impairment, blood pressure, heart rate, QT interval and lodenafil's pharmacokinetic parameters.

Results: Lodenafil carbonate alone or with alcohol did not induce clinically relevant modifications in arterial blood pressure or heart rate. A statistically significant decrease in blood pressure was seen four hours after LC and alcohol intake, and an increase in heart rate six hours after intake of lodenafil carbonate alone. The QTc interval was not significantly modified. Lodenafil carbonate bioavailability was increased in 74% when drug intake was associated with alcohol.

Conclusion: These results show that the use of lodenafil carbonate did not have clinically relevant effects on blood pressure or heart rate, and was not associated with QT interval prolongation. The association of lodenafil carbonate and alcohol affected its pharmacokinetic properties, increasing the bioavailability of the drug.

Publication types

  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Alcohol Drinking* / metabolism
  • Alcohol Drinking* / physiopathology
  • Analysis of Variance
  • Biological Availability
  • Blood Pressure / drug effects
  • Carbonates / pharmacokinetics
  • Carbonates / pharmacology*
  • Cardiovascular System / drug effects*
  • Heart Conduction System / drug effects
  • Heart Rate / drug effects
  • Humans
  • Male
  • Middle Aged
  • Phosphodiesterase Inhibitors / pharmacokinetics
  • Phosphodiesterase Inhibitors / pharmacology*
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology*
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology*
  • Young Adult

Substances

  • Carbonates
  • Phosphodiesterase Inhibitors
  • Piperazines
  • Pyrimidines
  • lodenafil carbonate