Pharmacokinetic Profiles of Metamizole Metabolites after Intramuscular and Intravenous Administration in Healthy Arabian Horses
Date
2021Author
Yılmaz, İsmetMaraş,Zeynep
Uğur, Yılmaz
Özgür, Mustafa Erkan
Durmaz, Murat
Ulusoy, Halil İbrahim
Erdoğan, Selim
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Show full item recordAbstract
Metamizole sodium (MT) is an analgesic and antipyretic drug molecule used in humans,
horses, cattle, swine, and dogs. Metamizole rapidly hydrolyzes and turns into methyl amino antipyrine (MAA), an active primary metabolite of MT. The present study aims
to determine the pharmacokinetic (PK) profiles of MT metabolites after intravenous
(IV) and intramuscular (IM) administration into sex of Arabian horses (Equus ferus ca ballus) using a cross-over study design. The plasma samples were extracted by solid phase extraction (SPE) method, and plasma concentrations of MT metabolites were
analyzed by high-performance liquid chromatography (HPLC). After administrations
of MT, plasma concentrations of methylamino antipyrine (MAA), amino antipyrone
(AA), and acetylamino antipyrone (AAA) were determined within range of 15 min 12 h. Plasma concentrations of AA and AAA were lower than the plasma concen trations of major metabolite MAA at each sampling point. The PK parameters were
statistically evaluated for MT’s metabolites between male and female horses and also
between IM and IV administrations of PK parameters such as Cmax, tmax, t1/2λz, AUC0-t
,
AUC0-∞, λz, Cl and Vss (p < .05). The AUCIM/AUCIV ratio in female and male horses for
MAA was 1.19 and 1.13, respectively. The AUCIM/AUCIV ratio for AA was lower than
those found for MAA. AUCIM/AUCIV ratio was statistically significantly different be tween male and female horses for AA (p < .05). According to these results, some PK
parameters such as Cmax, AUC, and MRT, MAA and AA concentrations have shown
statistically significant differences by MT administrations.