Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses

Abstract

According to in vitro and in vivo investigations, firocoxib (FX), a second-generation coxib, is a highly selective COX-2 inhibitor in horses. With a COX-1/COX-2 IC50 ratio of 643 in horses, FX spares the COX-1 inhibitory effects. It is approved for the treatment of musculoskeletal problems and lameness in horses and dogs with osteoarthritis (OA). For the treatment of OA in horses, both an injectable formulation for IV administration at a dose of 0.09 mg/kg for five days and an oral paste formulation at a dose of 0.1 mg/kg for 14 days are licensed. Numerous analytical methods were reported in the literature to quantify FX in biological fluids, using HPLC and LC-MS. FX presents remarkable pharmacokinetics and pharmacodynamics compared to other coxibs. It has an oral bioavailability of 80% or higher and is effectively absorbed by horses. Its volume of distribution is around 2 L/kg, and it is slowly eliminated. Due to the long elimination half-life (around 2 days), which allows a once daily dosing, a single 0.3 mg/kg loading dose has been recommended. This enables the establishment of steady-state drug concentrations within 24 h, making it appropriate for acute treatment as well. Its IC80 is equal to 103 ng/mL in whole blood and, with an EC50 of 27 ng/mL, it has the highest affinity for its receptor compared to the other commonly administered NSAIDs in horses.

Keywords

• Coxib
• Firocoxib
• Horses
• Pain management
• Pharmacodynamics
• Pharmacokinetics