Oral and intravenous administration of nimesulide in the horse: rational dosage regimen from pharmacokinetic and pharmacodynamic data

Abstract

The findings suggest that 1.5 mg/kg bwt may produce adequate clinical effects, and the dosing interval should be 12-24 h depending on condition severity. However, at that dose, the concentration in the animal exceeds the in vitro IC50 for both isoforms, so that COX-1/COX-2 selectivity is lost and side-effects due to COX-1 inhibition are a possibility. Nimesulide should therefore be used with caution in equine clinical practice.

Association Between Nonsteroidal Anti-Inflammatory Drugs and Gastric Ulceration in Horses and Ponies

“…Studies describing the side effects of flunixin meglumine, ketoprofen and phenylbutazone started to be published in the 1980s (Trillo et al, 1984;MacAllister et al, 1992;MacAllister, 1994;MacAllister & TaylorMacAllister, 1994). Other drugs, such as suxibuzone (a prophenylbutazone drug), firocoxib, monophenylbutazone (phenylbutazone-derivate), acetylsalicylic acid, eltenac, nimesulide and meloxicam, have also been studied (Prügner et al, 1991;Goodrich et al, 1998;Monreal et al, 2004;Villa et al, 2007;Andrews et al, 2009;Sabaté et al, 2009;Videla & Andrews, 2009;Pozzobon, 2010). Nevertheless, studies of phenylbutazone (or derivatives) have not been abandoned, possibly because of ulcerogenic effect and therapeutic efficacy (Vicente, 2004;Driessen, 2007).…”

“…As mentioned previously, decreased prostaglandin levels result in loss of balance in mucosal protective factors; this is commonly stated as the primary cause of ulcers in foals and adult horses (Andrews & Nadeau, 1999;Andrews et al, 2005). Villa et al (2007) evaluated the pharmacokinetics and pharmacodynamics of nimesulide in 15 healthy horses aged from 3 to 6 years. The animals were divided into three groups.…”