2023 journal article

Pharmacokinetics of a FDA-labeled dose of diclazuril administered orally once weekly to adult horses


By: N. Pusterla *, W. Vaala*, F. Bain*, D. Chappell*, B. Craig*, C. Schneider*, D. Barnett*, E. Gaughan*, M. Papich n 

co-author countries: United States of America πŸ‡ΊπŸ‡Έ
author keywords: Sarcocystis neurona; diclazuril; pharmacokinetic; prevention; horses
MeSH headings : Horses; Animals; Coccidiostats / pharmacology; Coccidiostats / therapeutic use; Seroepidemiologic Studies; Sarcocystis; Nitriles / pharmacology; Nitriles / therapeutic use
Source: Web Of Science
Added: January 23, 2023

Equine protozoal myeloencephalitis (EPM) has remained a devastating neurological disease of the Americas, especially in young performance horses. Prophylactic treatment strategies with diclazuril have shown to reduce seroprevalence and titer levels to Sarcocystis neurona in healthy horses continuously exposed to the apicomplexan parasite. The goal of this study was to determine if the FDA-labeled dose of 1 mg/kg of 1.56% diclazuril (ProtazilTM) given once weekly to healthy adult horses would achieve steady-state concentrations in plasma known to be inhibitory to S. neurona in cell culture. Five individual diclazuril doses were administered at weekly intervals to 8 adult horses. Blood was collected via venipuncture immediately before (trough concentration) and 10 hours after (peak concentration) each diclazuril administration. Following the fifth dose, additional blood samples were collected every 24 hours after the peak blood collection for 7 days. All plasma samples were analyzed by high-pressure liquid chromatography. The pharmacokinetic analysis was performed using a nonlinear mixed effects model. The mean population-derived peak concentration was 264 ng/mL and the mean terminal half-life was 3.6 days. Thus, the oral administration of an FDA-labeled dose of diclazuril to healthy horses once a week was able to produce steady-state plasma drug concentrations known to inhibit S. neurona in vitro.