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Tissue extraction of amiodarone and N‐desethylamiodarone in man after a single oral dose.
Author(s) -
Berdeaux A,
Roche A,
Labaille T,
Giroux B,
Edouard A,
Giudicelli JF
Publication year - 1984
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.1365-2125.1984.tb02539.x
Subject(s) - amiodarone , bioavailability , medicine , lumen (anatomy) , portal vein , vein , extraction ratio , anesthesia , extraction (chemistry) , pharmacology , chemistry , chromatography , atrial fibrillation
The hepatic extraction of amiodarone and N‐desethylamiodarone has been investigated in seven patients following catheterization of the portal and hepatic veins under general anaesthesia. Amiodarone (600 mg) was administered orally 4 h before regional blood sampling. Concentrations of amiodarone and N‐desethylamiodarone, determined by h.p.l.c., were about twice as high in the portal vein compared with those in the hepatic vein, the calculated hepatic extraction ratios of both compounds being 0.39 +/‐ 0.07 and 0.34 +/‐ 0.03, respectively. The presence of N‐desethylamiodarone in the portal vein in higher concentrations than in the hepatic vein strongly suggests that N‐ dealkylation of amiodarone occurs in the gut wall or lumen, a finding which might account for the low and highly variable intersubject amiodarone bioavailability.