Literature DB >> 21219411

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

Jean-Luc Vachiery1, Sandrine Huez, Hunter Gillies, Gary Layton, Naoto Hayashi, Xiang Gao, Robert Naeije.   

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.
© 2011 The Authors. British Journal of Clinical Pharmacology © 2011 The British Pharmacological Society.

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Year:  2011        PMID: 21219411      PMCID: PMC3040551          DOI: 10.1111/j.1365-2125.2010.03831.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


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