title: [Cardiovascular repercussion of lodenafil carbonate, a new PDE5 inhibitor, with and without alcohol consumption].
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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Unidade de Farmacocinética Biocrom, São Paulo, SP, Brasil.
authors.forename: Adauto Carvalho
authors.initials: AC
authors.lastname: Silva
authors.forename: Odaly
authors.initials: O
authors.lastname: Toffoletto
authors.forename: Luiz Antonio Galvão
authors.initials: LA
authors.lastname: Lucio
authors.forename: Paula Ferreira Dos
authors.initials: PF
authors.lastname: Santos
authors.forename: Jorge Barros
authors.initials: JB
authors.lastname: Afiune
authors.forename: João
authors.initials: J
authors.lastname: Massud Filho
authors.forename: Sergio
authors.initials: S
authors.lastname: Tufik
mesh_terms: D000293:Adolescent; D000328:Adult; D000428:Alcohol Drinking / Q000378:metabolism / Q000503:physiopathology; D000704:Analysis of Variance; D001682:Biological Availability; D001794:Blood Pressure / Q000187:drug effects; D002254:Carbonates / Q000493:pharmacokinetics / Q000494:pharmacology*; D002319:Cardiovascular System / Q000187:drug effects*; D006329:Heart Conduction System / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D008875:Middle Aged; D010726:Phosphodiesterase Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D010879:Piperazines / Q000493:pharmacokinetics / Q000494:pharmacology*; D011743:Pyrimidines / Q000493:pharmacokinetics / Q000494:pharmacology*; D055815:Young Adult
chemical_list: D002254:Carbonates; D010726:Phosphodiesterase Inhibitors; D010879:Piperazines; D011743:Pyrimidines; C532120:lodenafil carbonate