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

摘要: WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT Pulmonary arterial hypertension (PAH) is a rare syndrome of dyspnoea and fatigue due to an increase in pulmonary vascular resistance. Although the disease remains incurable, targeted therapies have been shown be beneficial patients. Oral sildenafil (20 mg three times daily) phosphodiesterase type 5 inhibitor with proven efficacy on exercise capacity, symptoms haemodynamics patients PAH. WHAT STUDY ADDS It advisable that chronic for PAH, including oral sildenafil, not interrupted. However, may able take their medication because intervening illness or requirement undergo general anaesthesia, preventing drug administration. This study demonstrates intravenous bolus 10 mg stable PAH safe, well tolerated maintains plasma levels preserve exposure. AIMS To assess pharmacokinetics pharmacodynamics stabilized 20 mg orally daily. METHODS Pharmacokinetic parameters were calculated using noncompartmental analysis. RESULTS After acute increase, concentrations within range reported previously tablet. At 0.5 h, mean ± SD changes from baseline −8.4 11.7 mmHg (systolic pressure), −2.6 7.3 mmHg (diastolic pressure) −3.5 10.4 beats min−1 (heart rate). There was no symptomatic hypotension. CONCLUSIONS further research warranted, appears provide similar exposure, tolerability safety