Bei 9 Patientinnen mit Mamma-Karzinom und Pleurakarzinosen, die im Rahmen des CMF-Schema 600 mg/m2 5-Fluorouracil i.v. erhielten, wurde die Pharmakokinetik von 5-Fluorouracil und seine Permeation in maligne Ergüsse untersucht. Trotz der kurzen Plasmahalbwertzeit von 5-Fluorouracil (16,8 min) konnten in den Ergüssen deutliche Wirkspiegel mit Gipfelkonzentrationen bis 115 nmol/ml nach 30 Minuten beobachtet werden. Infolge der raschen Elimination von 5-Fluorouracil im Plasma und der vergleichsweise langsamen Rückdiffusion aus dem Pleuraraum (t1/2 55 min) persistierten die Spiegel in den Ergüssen wesentlich länger als im Blut. Die Fläche unter der Pleuraspiegelkurve (AUC) erreichte 50% (27–85%) der entsprechenden Plasmawerte (AUC 10,9 ± 2,3 μmol × min × ml-1). Unter systemischer Therapie eines Mamma-Karzinoms mit malignen Pleuraergüssen sind daher aus pharmakokinetischer Sicht keine zusätzlichen lokalen 5-Fluorouracil-Instillationen erforderlich.

Keywords:
Pharmakokinetik von 5-Fluorouracil, Wirkspiegel in malignen Ergüssen, Mamma-Karzinom
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© 1984 S. Karger AG, Basel
1984
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