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Pharmacokinetic investigations of the marker active metabolites 4‐methylamino‐antipyrine and 4‐amino‐antipyrine after intramuscular injection of metamizole in healthy piglets
Author(s) -
Burmańczuk A.,
Kowalski C.,
Giorgi M.,
Owen H.,
Grabowski T.
Publication year - 2016
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/jvp.12317
Subject(s) - metamizole , pharmacokinetics , chemistry , pharmacology , plasma concentration , drug , metabolite , high performance liquid chromatography , analgesic , chromatography , medicine , biochemistry
Metamizole ( MT ) is a pyrazolone nonsteroidal anti‐inflammatory drug labelled for humans and animals. The aim of this study was to assess the pharmacokinetics of its active metabolites 4‐methylamino‐antipyrine ( MAA ) and 4‐amino‐antipyrine ( AA ) in male piglets after a single intramuscular injection of MT . Eight healthy male piglets were administered MT (100 mg/kg) intramuscularly. Blood was sampled at scheduled time intervals, and drug plasma concentrations evaluated by a validated HPLC method. MAA and AA plasma concentrations were quantitatively detectable from 0.25 to 48 h and 0.50 to 72 h, respectively, in 6 of 8 and 7 of 8 animals. The average maximum concentrations of MAA and AA were of 47.59 and 4.94 mg/ mL , respectively. The average half‐lives were 8.57 and 13.3 h for MAA and AA , respectively. This study showed that the amount of MAA and AA produced in piglets is different to that in the animal species previously investigated. Further studies are necessary to understand whether these differences in MAA and AA plasma concentrations between animal species necessitate diverse therapeutic drug dosing.