Safety, tolerability and pharmacokinetics of an intravenous bolus of sildenafil in patients with pulmonary arterial hypertension

Br J Clin Pharmacol. 2011 Feb;71(2):289-92. doi: 10.1111/j.1365-2125.2010.03831.x.

Abstract

Aims: To assess pharmacokinetics and pharmacodynamics of a 10 mg intravenous sildenafil bolus in pulmonary arterial hypertension (PAH) patients stabilized on 20 mg sildenafil orally three times daily.

Methods: Pharmacokinetic parameters were calculated using noncompartmental analysis.

Results: After an acute increase, plasma concentrations stabilized within the range reported previously for a 20 mg oral tablet. At 0.5 h, mean ± SD changes from baseline were -8.4 ± 11.7 mmHg (systolic pressure), -2.6 ± 7.3 mmHg (diastolic pressure) and -3.5 ± 10.4 beats min(-1) (heart rate). There was no symptomatic hypotension.

Conclusions: Although further research is warranted, a 10 mg sildenafil intravenous bolus appears to provide similar exposure, tolerability and safety to the 20 mg tablet.

Trial registration: ClinicalTrials.gov NCT00800592.

Publication types

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

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adult
  • Aged
  • Antihypertensive Agents / administration & dosage*
  • Antihypertensive Agents / adverse effects
  • Antihypertensive Agents / blood
  • Drug Administration Schedule
  • Female
  • Humans
  • Hypertension, Pulmonary / blood
  • Hypertension, Pulmonary / drug therapy*
  • Infusions, Intravenous
  • Male
  • Middle Aged
  • Phosphodiesterase 5 Inhibitors / administration & dosage
  • Phosphodiesterase 5 Inhibitors / adverse effects
  • Phosphodiesterase 5 Inhibitors / blood
  • Piperazines / administration & dosage*
  • Piperazines / adverse effects
  • Piperazines / blood
  • Purines / administration & dosage
  • Purines / adverse effects
  • Purines / blood
  • Sildenafil Citrate
  • Sulfones / administration & dosage*
  • Sulfones / adverse effects
  • Sulfones / blood
  • Vasodilator Agents / administration & dosage*
  • Vasodilator Agents / adverse effects
  • Vasodilator Agents / blood
  • Young Adult

Substances

  • Antihypertensive Agents
  • Phosphodiesterase 5 Inhibitors
  • Piperazines
  • Purines
  • Sulfones
  • Vasodilator Agents
  • Sildenafil Citrate

Associated data

  • ClinicalTrials.gov/NCT00800592