title: Safety, tolerability and pharmacokinetics of an intravenous bolus of sildenafil in patients with pulmonary arterial hypertension.
abstract: OBJECTIVE
  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.
authors.affiliation: Pulmonary Hypertension and Heart Failure Clinic, Hôpital Erasme, Brussels, Belgium. jvachier@ulb.ac.be
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Vachiery
authors.forename: Sandrine
authors.initials: S
authors.lastname: Huez
authors.forename: Hunter
authors.initials: H
authors.lastname: Gillies
authors.forename: Gary
authors.initials: G
authors.lastname: Layton
authors.forename: Naoto
authors.initials: N
authors.lastname: Hayashi
authors.forename: Xiang
authors.initials: X
authors.lastname: Gao
authors.forename: Robert
authors.initials: R
authors.lastname: Naeije
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000368:Aged; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood; D004334:Drug Administration Schedule; D005260:Female; D006801:Humans; D006976:Hypertension, Pulmonary / Q000097:blood / Q000188:drug therapy*; D007262:Infusions, Intravenous; D008297:Male; D008875:Middle Aged; D058986:Phosphodiesterase 5 Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood; D010879:Piperazines / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood; D011687:Purines / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood; D000068677:Sildenafil Citrate; D013450:Sulfones / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood; D014665:Vasodilator Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood; D055815:Young Adult
chemical_list: D000959:Antihypertensive Agents; D058986:Phosphodiesterase 5 Inhibitors; D010879:Piperazines; D011687:Purines; D013450:Sulfones; D014665:Vasodilator Agents; D000068677:Sildenafil Citrate