Nitrofurantoin is a urinary tract antibacterial agent whose clinical effectiveness depends on the high urinary drug levels encountered during therapeutic drug dosage. Under these conditions, only low blood drug concentrations are usually found. On the basis of urinary nitrofurantoin excretion determined after oral and intravenous drug administration, orally administered nitrofurantoin in a suitable dosage form is well absorbed. In vitro testing does not accurately reflect nitrofurantoin bioavailability, which is affected by formulation differences, drug particle size, and dosage form. Nitrofurantoin is readily absorbed and quickly distributed into most body fluids. It is rapidly excreted in large amounts in bile and urine. With the exception of the active drug secretion in the kidney tubule and biliary drug transport, nitrofurantoin transfer across body membranes occurs by diffusion. Nitrofurantoin has a short elimination half-life in whole blood or plasma. In conjunction with its rapid excretion by the primary routes, there is little evidence for any prolonged binding of nitrofurantoin to either plasma proteins or tissues. The first-order kinetics involved in nitrofurantoin absorption and elimination is most appropriately described by a one-compartment open model. Biliary and urinary excretion of unchanged nitrofurantoin and enzymatic degradation are the primary means of elimination.