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. 1980;10(Suppl 2):299S–308S. doi: 10.1111/j.1365-2125.1980.tb01813.x

Kinetics and metabolism of pyrazolones (propyphenazone, aminopyrine and dipyrone)

Manfred Volz, Hans-Martin Kellner
PMCID: PMC1430198  PMID: 7002187

Abstract

1 Propyphenazone 220 mg was administered orally to volunteers. Maximum plasma concentrations between 1.5 μg/ml and 3.5 μg/ml were found 30 min later. After comparable doses plasma concentrations in dog and rabbit were lower. The distribution volumes were 2 1/kg.

2 The major metabolic route of propyphenazone is demethylation. The main urinary metabolite is the enolglucuronide of N-(2)-demethylprophyphenazone.

3 Aminopyrine is rapidly and almost completely absorbed after oral administration. Maximum plasma concentrations of 10 μg/ml are reached 1.5 h after a 500 mg dose. The biological half-life is 2-3 h, the relative distribution volume 60% on average, and binding to plasma proteins approximately 15%.

4 Unchanged aminopyrine is only excreted in small quantities. The major routes of metabolism are demethylation (4-methylaminoantipyrine and 4-aminoantipyrine) and acylation (4-acetyl and 4-formylaminoantipyrine). There are other biotransformation products.

5 After oral administration of [14C]-dipyrone 480 mg the maximum serum concentration of 13.4±0.8 μg/ml occurred at 1-1.5 hours.

6 Dipyrone was not detectable in serum or urine. Four of seven metabolites were identified, and were identical with the main metabolites of aminopyrine.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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