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J Vet Pharmacol Ther. 2018 Apr;41(2):334-339. doi: 10.1111/jvp.12471. Epub 2017 Nov 21.

Pharmacokinetic profiles of the two major active metabolites of metamizole (dipyrone) in cats following three different routes of administration.

Author information

1
Department of Pharmacology, University of Life Sciences, Lublin, Poland.
2
College of Veterinary Medicine, Chungnam National University, Daejeon, South Korea.
3
Faculty of Veterinary Medicine, Royal University of Agriculture, Phnom Penh, Cambodia.
4
Department of Veterinary Science, University of Queensland, Gatton, Brisbane, QLD, Australia.
5
Department of Pharmacology, Faculty of Veterinary Medicine, Kasetsart University, Bangkok, Thailand.
6
Department of Veterinary Sciences, University of Pisa, Pisa, Italy.

Abstract

This study was performed to determine pharmacokinetic profiles of the two active metabolites of the analgesic drug metamizole (dipyrone, MET), 4-methylaminoantipyrine (MAA), and 4-aminoantipyrine (AA), after intravenous (i.v., intramuscular (i.m.), and oral (p.o.) administration in cats. Six healthy mixed-breed cats were administered MET (25 mg/kg) by i.v., i.m., or p.o. routes in a crossover design. Adverse clinical signs, namely salivation and vomiting, were detected in all groups (i.v. 67%, i.m. 34%, and p.o. 15%). The mean maximal plasma concentration of MAA for i.v., i.m., and p.o. administrations was 148.63 ± 106.64, 18.74 ± 4.97, and 20.59 ± 15.29 μg/ml, respectively, with about 7 hr of half-life in all routes. Among the administration routes, the area under the plasma concentration curve (AUC) value was the lowest after i.m. administration and the AUCEV/i.v . ratio was higher in p.o. than the i.m. administration without statistical significance. The plasma concentration of AA was detectable up to 24 hr, and the mean plasma concentrations were smaller than MAA. The present results suggest that MET is converted into the active metabolites in cats as in humans. Further pharmacodynamics and safety studies should be performed before any clinical use.

KEYWORDS:

cat; dipyrone; metabolite; metamizole; painkiller; pharmacokinetics

PMID:
29164623
DOI:
10.1111/jvp.12471
[Indexed for MEDLINE]

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