Toxicity and biotransformation of acetaminophen in rat hepatocytes (I). Uptake and release.

Uptake and conjugation of acetaminophen were studied in isolated rat hepatocytes. Acetaminophen was taken up by the cells and the conjugates formed in the cells were rapidly released from the cells at a constant rate. The kinetic analysis demonstrated that uptake was due to a saturable process as well as a simple diffusion. Decrease in uptake of acetaminophen by metabolic inhibitors suggested that uptake of acetaminophen by hepatocytes might be, at least in part, due to an energy dependent process.