Sulprim Paste 250g
Trimethoprim 86 mg/g
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|Drug Name and Strength||Sulfadimidine 315 mg/g,
Trimethoprim 63 mg/g
|Indication||Treatment of infections in horses due to organisms susceptible to the combination of sulfadimidine and trimethoprim.|
|Contraindications||Do not use in horses with hepatic parenchymal damage, blood dyscrasia, renal disease or urolithiasis, or to animals with a history of sulfonamide or trimethoprim sensitivity.|
|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 sulfonamide 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 (Rhodococcus) equi ), Salmonella, Shigella, Klebsiella, Pasteurella, Haemophilus and Proteus sp. Most Escherichia coli and some Brucella and Nocardia sp. are also sensitive to the combination. Most Pseudomonas sp. are insensitive to the combination. 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 animals previously exposed to the combination.Pharmacology Sulfadimidine. Sulfadimidine is a pyrimidine sulfonamide antimicrobial agent. Sulfonamides, being structural analogues of para-aminobenzoic acid (PABA), 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 are thus unaffected by sulfonamides. The antibacterial actions of sulfonamides 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 gastrointestinal tract and, like sulfadimidine, rapidly reaches therapeutic levels in plasma. It is widely distributed in body tissues and fluids including bone and prostate, and cerebrospinal, 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.|
|Precautions||In cases when the infection is nonresponsive or chronic, culture and sensitivity tests should be undertaken.|
|Dosage and Administration||For oral use only. Administer 4 mL/50 kg bodyweight twice daily for up to seven days or as directed by a veterinarian.|
|Storage||Store below 30°C (room temperature).|
|MSDS (external link)||Sulprim Paste 250g MSDS|
|Label (external link)||Sulprim Paste 250g Label|
|Manufacturer||Ilium Veterinary Products|