医薬品の生体内変化に関する研究(第71報) : アミノピリンの代謝について

概要

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In connection with the previous work that antipyrine is oxidized not only to 4-hydroxyantipyrine, but also to 3-hydroxymethyl-2-methyl-1-phenyl-3-pyrazolin-5-one, which was oxidized in part to 2-methyl-5-oxo-1-phenyl-3-pyrazolin-3-carboxylic acid, ^<1)> metabolism of aminopyrine was investigated to see whether the methyl group at 3-position of pyrazolinone ring also undergoes oxidation. The major pathway of this drug was reconfirmed to be dealkylation in rabbits and rats, 4-aminoantipyrine and 4-acetamidoantipyrine being excreted as the major metabolites. In addition, it was also found that a part of ingested aminopyrine was excreted as 4-dimethylamino-3-hydroxymethyl-2-methyl-1-phenyl-3-pyrazolin-5-one in the urine. In rats, this hydroxymethyl metabolite was found to be partially oxidized to 4-dimethylamino-2-methyl-5-oxo-1-phenyl-3-pyrazolin-3-carboxylic acid. The possible relationship between this oxidation pathway of the methyl group at 3-position of pyrazolinone and allergic reaction of aminopyrine was discussed.
社団法人日本薬学会の論文
1970-11-25