Pharmacokinetic evaluation of sildenafil as a pulmonary hypertension treatment

Expert Opin Drug Metab Toxicol. 2013 Sep;9(9):1193-205. doi: 10.1517/17425255.2013.804063. Epub 2013 Jun 12.

Abstract

Introduction: Sildenafil citrate is a potent, selective phosphodiesterase type 5 inhibitor approved for the treatment of pulmonary arterial hypertension (PAH) and plays an important role in the management of the disease.

Areas covered: In this review, we focus on the current available information on the pharmacokinetics, pharmacodynamics, clinical efficacy and safety of sildenafil citrate in PAH through a MEDLINE literature search. Comparison of sildenafil citrate with tadalafil, another phosphodiesterase type 5 inhibitor was also performed.

Expert opinion: In the last few years, considerable progress has been made in the understanding and treatment of PAH. Sildenafil citrate has multiple advantages and whether it is first-line treatment alone or in combination for the mild form of the disease, it is one of the treatments of choice. In terms of its future use, more studies are still needed to better evaluate the benefit/risk balance of sildenafil citrate in pediatric populations.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adult
  • Animals
  • Carbolines / therapeutic use
  • Child
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Humans
  • Hypertension, Pulmonary / drug therapy*
  • Hypertension, Pulmonary / physiopathology
  • Phosphodiesterase 5 Inhibitors / therapeutic use
  • Piperazines / pharmacokinetics*
  • Piperazines / therapeutic use*
  • Purines / pharmacokinetics
  • Purines / therapeutic use
  • Randomized Controlled Trials as Topic
  • Sildenafil Citrate
  • Sulfones / pharmacokinetics*
  • Sulfones / therapeutic use*
  • Tadalafil

Substances

  • Carbolines
  • Phosphodiesterase 5 Inhibitors
  • Piperazines
  • Purines
  • Sulfones
  • Tadalafil
  • Sildenafil Citrate