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Ilium Sulprim Oral Antibiotic Paste for Horses

Registered Name: Ilium Sulprim Oral Paste for Horses

Composition: Sulfadimidine 315mg/g, Trimethoprim 63mg/g

Actions: Microbiology. Sulfadimidine and trimethoprim have similar antibacterial spectra, trimethoprim being approximately 20 times more potent than sulfadimidine. The combination blocks two sequential obligate enzymatic reactions in the microbial folate synthetic pathway. A synergistic action is demonstrated by the enhanced antimicrobial activity (potentiation) of the combination, compared with the antimicrobial activity of either agent singly. The minimum inhibitory concentrations of the combination for susceptible bacteria are substantially lower than those of either of the individual agents. The combination of sulphonamide and trimethoprim is bactericidal while either drug alone is bacteriostatic. Folate synthesising bacteria which are resistant or moderately resistant to either drug alone are frequently susceptible to the combination.

The correlation of antibacterial sensitivity in vitro compared with in vivo is among the highest of all antimicrobial agents. The spectrum of bacteria sensitive to the combination includes Staphylococci, Streptococci, Fusobacterium, Enterobacter, Corynebacterium (excluding Corynebacterium (Rhodoccus) equi), Salmonella, Shingella, Klebsiella, Pasturella, Haemophilus, Proteus sp. And most Escherichia coli, and some Brucella and Norcardia sp. Most Pseudomonas sp. are insensitive.

Resistance to the combination by Gram-negative bacteria is associated with the presence of R Factors. Resistance by Staphylococcus aureus and Haemophilus sp. Is chromosomal, and is rarely encountered except in patients previously exposed to the combination.

Pharamcology. Sulfadimidine. Sulfadimidine is a pyrimidine sulphonamide antimicrobial agent. Sulfonamides, being structural analogues of PABA (para-aminobenoic acid), competitively inhibit the incorporation of PABA into dihydropteric acid, the precursor of folic acid. The subsequent reduction in the level of folic acid reduces the production of nucleic acids in sensitive bacteria. Mammalian cells require preformed folic acid and thus are unaffected by sulphonamides. The antibacterial actions of sulphonamides are reduced in the presence of blood, pus and tissue breakdown products, which contain purines and thymidine, as the bacterial requirement for folic acid is decreased in such media.

Trimethoprim. Trimethoprim is a diaminopyrimidine antimicrobial agent. It acts by preventing the reduction of dihydrofolate to tetrahydrofolate which is required by bacteria for biosynthesis of purines, pyrimidines and some amino acids.

Pharmacokinetics. Sulfadimidine. Sulfadimidine is readily absorbed following oral administration, and therapeutic plasma levels are rapidly attained. Sulfadimidine is widely distributed to all body tissues and fluids. Concentrations are above plasma levels in the kidney; similar to plasma levels in pleural, peritoneal, synovial and ocular fluids; and slightly lower in cerebrospinal fluid, muscle and milk.

Sulfadimidine undergoes extensive metabolism via acetylation, hydroxylation, oxidation and conjugation. The parent compound and its metabolites are excreted predominantly in the urine by glomerular filtration. Sulfadimidine undergoes passive tubular resorption, thus prolonging the time course of drug action. Plasma half-life in the horse has been variously estimated as between 6.4 and 9.8 hours.

Trimethoprim. Trimethoprim is readily absorbed from the gastro-intestinal tract and, like sulfadimidine, rapidly reaches therapeutic levels in plasma. It is widely distributed in body tissues/fluids including bone, prostate, CSF, pleural, peritoneal, synovial and ocular fluids. Studies in humans and several animal species have demonstrated that trimethoprim reaches higher concentrations in all tissues, except brain, than those achieved in plasma. Trimethoprim is extensively metabolised in the horse and is excreted in the urine by glomerular filtration and active tubular secretion. Plasma half-life in the horse has been variously estimated as between 4.1 and 4.6 hours.

Indications: For the treatment of infections in horses due to organisms susceptible to the combination of Sulfadimidine and Trimethoprim.

Withholding Periods: Horses Meat 28 days

Contraindications: Do not use in horses with hepatic parenchymal damage, blood dyscrasia, renal disease, urolithiasis.
Administration to animals with a history of sulfonamide or trimethoprim sensitivity.

Precautions: In cases where the infection is non-responsive or chronic, culture and sensitivity test should be undertaken.

Dosage and Administration: For oral use only.

Administer 4ml/50kg bodyweight twice daily for up to 7 days or as directed by your veterinarian.

Presentation: Paste 30g, 250g

Storage: Store below 30`C (Room Temperature)

Poisons Schedule:
S4

Registration: All States

APVMA Number: 62878