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Pharmacokinetic profiles of the two major active metabolites of metamizole (dipyrone) in cats following three different routes of administration
Author(s) -
LebkowskaWieruszewska B.,
Kim T. W.,
Chea B.,
Owen H.,
Poapolathep A.,
Giorgi M.
Publication year - 2018
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.12471
Subject(s) - metamizole , pharmacokinetics , cats , oral administration , pharmacodynamics , pharmacology , active metabolite , plasma concentration , crossover study , analgesic , vomiting , medicine , adverse effect , chemistry , anesthesia , alternative medicine , pathology , placebo
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 AUC EV /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.