Beschreibung:
<jats:sec><jats:label /><jats:p> <jats:bold>What is already known about this subject</jats:bold> </jats:p><jats:p>• Furosemide is an effective diuretic, but its absorption may be too slow to allow oral treatment in certain patients.</jats:p><jats:p> <jats:bold>What this study adds</jats:bold> </jats:p><jats:p>• In healthy volunteers, sublingual administration is associated with a higher <jats:italic>C</jats:italic><jats:sub>max</jats:sub>, a higher bioavailability and a more accentuated initial natriuretic response than oral furosemide. Sublingual administration may offer advantages over oral administration of furosemide in certain clinical situations.</jats:p></jats:sec><jats:sec><jats:title>Background</jats:title><jats:p>In patients with decompensated heart failure, absorption of orally administered furosemide may be delayed, possibly leading to impaired pharmacodynamic effects. Sublingual administration may represent an alternative in such situations.</jats:p></jats:sec><jats:sec><jats:title>Methods</jats:title><jats:p>In a crossover study including 11 healthy men, 20 mg furosemide was administered intravenously, orally and sublingually on three different days. Pharmacokinetics and pharmacodynamics were assessed from repeated blood and urine samples.</jats:p></jats:sec><jats:sec><jats:title>Results</jats:title><jats:p>Compared with oral administration, sublingual administration was associated with 43% higher <jats:italic>C</jats:italic><jats:sub>max</jats:sub>[difference 215 ng ml<jats:sup>−1</jats:sup>, 95% confidence interval (CI) 37, 392], a higher urinary recovery (8.9 <jats:italic>vs.</jats:italic> 7.3 mg, difference 1.6 mg, 95% CI 0.3, 2.9), an 28% higher AUC (difference 328 ng h<jats:sup>−1</jats:sup> ml<jats:sup>−1</jats:sup>, 95% CI 24, 632) and a higher bioavailability of furosemide (59 <jats:italic>vs.</jats:italic> 47%, difference 12.0%, 95% CI −1.2, 25.2). Sodium excretion was higher after sublingual compared with oral administration (peak excretion rate 1.8 <jats:italic>vs.</jats:italic> 1.4 mmol min<jats:sup>−1</jats:sup>, <jats:italic>P</jats:italic> < 0.05), whereas urine volume did not differ significantly between the two application modes. In comparison, intravenous administration showed the expected more rapid and intense response.</jats:p></jats:sec><jats:sec><jats:title>Conclusion</jats:title><jats:p>Sublingually administered furosemide tablets differ in certain kinetic and dynamic properties from identical tablets given orally. Sublingual administration of furosemide may offer therapeutic advantages in certain groups of patients.</jats:p></jats:sec>