Toxicokinetics of DL-glufosinate enantiomer in human BASTA poisoning.

We found that glufosinate (DL-GLUF) was distributed in the spinal fluid in glufosinate poisoning. A 50-year old Japanese man (weighing 67 kg) attempted to commit suicide by ingesting about 100 ml of BASTA (containing DL-GLUF 18.5 g; ratio of D-GLUF to L-GLUF: 1 : 1). He was transported to our hospital, where serious respiratory depression was seen 26 h after ingestion, and management with artificial ventilation was initiated. The D-GLUF concentration 1 h after ingestion was 191.1 microg/ml, almost the same as that of L-GLUF 193.5 microg/ml, but by 3 h after ingestion, these levels had sunk to 60.3 microg/ml and 52.3 microg/ml, respectively, with the concentration of L-GLUF lower than that of D-GLUF. Later, at 27 and 35 h after ingestion, the D-GLUF level was still higher than the L-GLUF level, and the total amounts of urinary excretion were 2835 mg for D-GLUF and 2298 mg for L-GLUF, each variable thus showing a difference between the enantiomers. Cerebrospinal fluid taken from the patient 27 h after poison ingestion revealed the presence of DL-GLUF on CG-MS analysis, and quantitative HPLC analysis of the enantiomers indicated that the D-GLUF concentration was 0.48 microg/ml, and the L-GLUF concentration 0.12 microg/ml. The levels in blood collected at the same time were: D-GLUF, 1.44 microg/ml, and L-GLUF, 0.35 microg/ml. Also, the cerebrospinal fluid contained about one-third of the blood levels of both DL-GLUF enantiomers. He was discharged without any sequelae after 11 d of hospitalization.