Comparison of 5-fluorouracil anabolite levels after intravenous bolus and continuous infusion.

The levels of 5-fluorouracil (5FU) and its anabolites in the serum, bile, pancreatic juice, liver, pancreas, and skeletal muscle of dogs were compared after single bolus administration and after continuous infusion. Six dogs had a bolus of 5FU (15 mg/kg) and were studied for 120 min. Five dogs had a continuous infusion of 5FU (30 mg/kg) and were studied for 24 h. After the bolus infusion, serum 5FU levels were initially high and then declined, whereas anabolite levels gradually increased over 45 min. Within 2 h, anabolite levels exceeded 5FU levels in tissues but were undetectable in bile and pancreatic juice. During the continuous infusion, anabolite levels in serum increased more rapidly than 5FU levels and remained significantly higher for 24 h. Anabolite levels also exceeded 5FU levels in bile, pancreatic juice, pancreas, and muscle but not in the liver. Continuous infusion of 5FU produced higher levels of the anabolites than did bolus infusion and maintained constant levels throughout the infusion period.