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Sublingual administration of furosemide: new application of an old drug
Author(s) -
Haegeli Laurent,
BrunnerLa Rocca Hans Peter,
Wenk Markus,
Pfisterer Matthias,
Drewe Jürgen,
Krähenbühl Stephan
Publication year - 2007
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2007.03035.x
Subject(s) - furosemide , medicine , sublingual administration , bioavailability , pharmacokinetics , pharmacodynamics , crossover study , oral administration , pharmacology , urine , route of administration , diuretic , anesthesia , placebo , alternative medicine , pathology
What is already known about this subject • Furosemide is an effective diuretic, but its absorption may be too slow to allow oral treatment in certain patients. What this study adds • In healthy volunteers, sublingual administration is associated with a higher C max , 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. Background 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. Methods 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. Results Compared with oral administration, sublingual administration was associated with 43% higher C max [difference 215 ng ml −1 , 95% confidence interval (CI) 37, 392], a higher urinary recovery (8.9 vs. 7.3 mg, difference 1.6 mg, 95% CI 0.3, 2.9), an 28% higher AUC (difference 328 ng h −1 ml −1 , 95% CI 24, 632) and a higher bioavailability of furosemide (59 vs. 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 vs. 1.4 mmol min −1 , P < 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. Conclusion 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.