Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Toxicokinetics of DL-Glufosinate Enantiomer in Human BASTA® Poisoning
Yasushi HoriToshiharu TanakaManami FujisawaKenji Shimada
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2003 Volume 26 Issue 4 Pages 540-543

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Abstract

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 μg/ml, almost the same as that of L-GLUF 193.5 μg/ml, but by 3 h after ingestion, these levels had sunk to 60.3 μg/ml and 52.3 μg/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 μg/ml, and the L-GLUF concentration 0.12 μg/ml. The levels in blood collected at the same time were: D-GLUF, 1.44 μg/ml, and L-GLUF, 0.35 μg/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.

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© 2003 The Pharmaceutical Society of Japan
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