KONZENTRATIONEN VON AMIODARON UND FLECAINID IM PLASMA UND IM SPEICHEL. HINWEISE FUR EINEN AKTIVEN TRANSPORT VON FLECAINID

Translated title of the contribution: Drug concentrations of amiodarone and flecainide in plasma and in the saliva

J. Nitsch, U. Kohler, L. Neyses, B. Luderitz

    Research output: Contribution to journalArticlepeer-review

    Abstract

    Only the free protein-unbound drug concentration in plasma is pharmacologically active. The concentration of some drugs in saliva is equal to the free drug level. We compared concentrations (in plasma before, 30 and 60 min after the morning dose, in saliva before, 30, 60, 90 and 120 min after the morning dose) of amiodarone (n=8, 2x200 mg orally per day) and flecainide (n=16, 2x100 mg) administered as chronic antiarrhythmic treatment. Drug levels were measured by 'high performance liquid chromatography'. Results: Just prior to the first morning dose, amiodarone concentrations in plasma were 1.0-2.9 (2.0 ± 0.6) μg/ml, in saliva 0.02-0.25 μg/ml; flecainide in plasma 80-560 (316 ± 163) ng/ml, in saliva 630-3700 (1749 ± 963) ng/ml. After the morning dose we found maximal flecainide plasma levels of 462 ± 203 and saliva levels of 3218 ± 2857 ng/ml. The highest flecainide concentrations in the saliva (13,400 and 11,300 ng/ml) were found in two patients 30 and 60 min after the morning dose. Flecainide, but not amiodarone, is excreted actively in the saliva, probably indicating an enteroenteric circulation. This should be considered to reduce life-threatening flecainide intoxications by gastric and intestinal lavage and suction. The concentration of flecainide in the saliva does not represent the non-protein-bound free drug level in the plasma.
    Translated title of the contributionDrug concentrations of amiodarone and flecainide in plasma and in the saliva
    Original languageGerman
    Pages (from-to)99-102
    Number of pages3
    JournalZeitschrift fur Kardiologie
    Volume77
    Issue number2
    Publication statusPublished - 1988

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