Cimicoxib is a novel cyclooxygenase 2 inhibitor drug approved for use in dogs. Assessing pharmacokinetic profiles in target species is pivotal for extra-label applications. The purpose of the present study was to evaluate the pharmacokinetic profiles of cimicoxib after intragastric administration in six healthy jennies. Plasma concentrations of cimicoxib were determined by high performance liquid chromatography with fluorescence detector. A pilot study was carried out with two animal groups (n = 3) in fasted or fed conditions receiving 2 mg/kg of cimicoxib. Because of the relatively low Cmax (0.03 μg/mL) from the pilot study, the dose was increased (5 mg/kg) for the subsequent full-scale crossover study. Single administration of 5 mg/kg did not show any adverse effects. However, the Cmax (0.02 μg/mL) and area under the curve (0.14 hour × μg/mL) values obtained after 5 mg/kg administration were not dose dependent compared with those in the 2 mg/kg pilot study. The results from this study could provide basic but essential information for the use of cimicoxib. Further pharmacodynamic studies are required to assess clinical efficacy in donkeys at these low plasma concentrations.
Pharmacokinetics of the novel COX-2 inhibitor cimicoxib in donkeys
DELLA ROCCA, Giorgia;DI SALVO, Alessandra;
2014
Abstract
Cimicoxib is a novel cyclooxygenase 2 inhibitor drug approved for use in dogs. Assessing pharmacokinetic profiles in target species is pivotal for extra-label applications. The purpose of the present study was to evaluate the pharmacokinetic profiles of cimicoxib after intragastric administration in six healthy jennies. Plasma concentrations of cimicoxib were determined by high performance liquid chromatography with fluorescence detector. A pilot study was carried out with two animal groups (n = 3) in fasted or fed conditions receiving 2 mg/kg of cimicoxib. Because of the relatively low Cmax (0.03 μg/mL) from the pilot study, the dose was increased (5 mg/kg) for the subsequent full-scale crossover study. Single administration of 5 mg/kg did not show any adverse effects. However, the Cmax (0.02 μg/mL) and area under the curve (0.14 hour × μg/mL) values obtained after 5 mg/kg administration were not dose dependent compared with those in the 2 mg/kg pilot study. The results from this study could provide basic but essential information for the use of cimicoxib. Further pharmacodynamic studies are required to assess clinical efficacy in donkeys at these low plasma concentrations.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.