Kinetics and metabolism of pyrazolones (propyphenazone, aminopyrine and dipyrone)
| Autor: | Hans-Martin Kellner, Manfred Volz |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 1980 |
| Předmět: |
Metabolite
Microgram Dipyrone Administration Oral Urine Pharmacology chemistry.chemical_compound Oral administration medicine Animals Humans Pharmacology (medical) Aminopyrine Propyphenazone Biotransformation Demethylation Suppositories Anti-Inflammatory Agents Non-Steroidal Metabolism Articles Blood proteins Kinetics chemistry Pyrazoles Oxidation-Reduction Antipyrine medicine.drug |
| Popis: | 1 Propyphenazone 220 mg was administered orally to volunteers. Maximum plasma concentrations between 1.5 microgram/ml and 3.5 micrograms/ml were found 30 min later. After comparable doses plasma concentrations in dog and rabbit were lower. The distribution volumes were 2 l/kg. 2 The major metabolic route of propyphenazone is demethylation. The main urinary metabolite is the enolglucuronide of N-(2)-demethylpropyphenazone. 3 Aminopyrine is rapidly and almost completely absorbed after oral administration. Maximum plasma concentrations of 10 microgram/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 microgram/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. |
| Databáze: | OpenAIRE |
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