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Properties

Product Name : Toltrazuril
CAS NO : 69004-03-1
Molecular Formula : C18H14F3N3O4S
Structural Formula:

Toltrazuril and its uses

Toltrazuril is an antiprotozoal medication used to treat coccidiosis in chickens, turkeys, dogs, cats, birds, reptiles, and all small animals. It is administered orally in the drinking water and has been found to be effective against intracellular parasite stages and many different types of coccidia at all stages. However, it is illegal to use in food animals in the United States in any form because there is no FDA-approved toltrazuril product in the country. Some characteristics of immune sera after toltrazuril treatment which may be involved in the enhancement of immunity are higher IgG response, higher antibody titre in IFAT, immunoblot, and ELISA, and a higher reduction in oocyst excretion, lesion scoring, and increased weight gains in toltrazuril-treated animals. Toltrazuril treatment is suitable for controlling cystoisosporosis under experimental and field conditions. A single oral treatment for puppies in the 3rd or 4th week of age is recommended.

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1. Metabolism and Elimination:

   • In chickens, 50% and 90% of the administered toltrazuril is eliminated by 4.5 and 15.5 days after dosing, respectively.
   • Toltrazuril sulfone is the major metabolite, representing a significant portion of the total radioactivity in muscle, fat, and liver.
   • The metabolite Toltrazuril sulfone is considered the most appropriate marker residue for chickens and turkeys.

2. Maximum Residue Limits (MRL) in Poultry:

   • MRL has been established for toltrazuril in poultry, with specific limits for different tissues: 200 μg kg?1 (skin/fat), 600 μg kg?1 (liver), and 400 μg kg?1 (kidney).

3. Efficacy Against Protozoa:

   • Toltrazuril and its major metabolite ponazuril are effective against apicomplexan coccidial infections in animals.
   • They have been used to treat isosporiasis, toxoplasmosis, neosporosis, and equine protozoal meningoencephalitis.

4. Mechanism of Action:

   • Toltrazuril and ponazuril appear to act on a plastid-like chloroplast organelle (the apicoplast) in apicomplexan protozoa.
   • The exact mechanism of action is unclear, but it may involve inhibition of metabolic enzymes or a decrease in pyrimidine synthesis within the apicoplast.

5. Use in Animals:

   • Toltrazuril has historical use as a coccidiostat against coccidia infections in production animals.
   • It is known to be efficacious against canine Isospora infections.
   • Ponazuril, a metabolite of toltrazuril, has been specifically approved for treating equine protozoal myeloencephalitis (EPM) in horses.

6. Long Half-Life in Horses:

   • Ponazuril has a long half-life in horses, and concentrations in cerebrospinal fluid (CSF) are sufficient to inhibit protozoa.
   • It has been successfully used to treat equine protozoal myeloencephalitis in horses.

7. Limited Information on Use in Other Animals:

   • There is limited information available on the use of toltrazuril and ponazuril in animals other than those mentioned above.
   • Some anecdotal accounts suggest their use in treating toxoplasmosis in cats and protozoa in other species.

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