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Ceftriaxone is a third-generation cephalosporin antibiotic. Like other third-generation cephalosporins, it has broad spectrum activity against Gram positive and Gram negative bacteria. In most cases, it is considered to be equivalent to cefotaxime in terms of safety and efficacy.
It must not be mixed or administered simultaneously (within 48 hours) with calcium-containing solutions or products, even via different infusion lines (rare fatal cases of calcium-ceftriaxone precipitates in lung and kidneys in neonates have been described). To reduce the pain of intramuscular injection, ceftriaxone may be reconstituted with 1% lidocaine.
Ceftriaxone has also been investigated for efficacy in preventing relapse to cocaine addictions.
Tazobactam is a penicillanic acid sulfone derivative with β-lactamase inhibitory properties. It enhances the activity of β-lactam antibacterials against β-lactamase-producing bacteria.
Ceftriaxone is completely absorbed following IM administration with mean maximum plasma concentration occurring between 2-3 hours post dose. Ceftriaxone achieves high concentrations in urine. 33% to 67% of ceftriaxone was excreted as unchanged drug and the remainder is excreted in bile and faeces. Average concentrations of ceftriaxone achieved after 1 g of IV dose in gall bladder bile is 581mcg/ml, 788mcg/ml in common bile duct, 898 mcg/ml in cystic bile duct, 78.2 mcg/ml in gall bladder wall and 62.1 mcg/ml in concurrent plasma. Elimination half life was 8.7 hours. Ceftriaxone is 98% bound to plasma proteins. Ceftriaxone crosses the blood brain barrier.
Tazobactam is metabolized to a single metabolite that lacks pharmacological and antibacterial activities. Tazobactam is eliminated via the kidney by glomerular filtration and tubular secretion. Tazobactam and its metabolite are eliminated via the kidney by glomerular filtration and tubular secretion. Tazobactam and its metabolite are eliminated primarily by renal excretion with 80 % of the ministered dose excreted as unchanged drug and the remainder as a single metabolite. Tazobactam is also secreted into the bile. Tazobactam is approximately 30% bound to plasma proteins. Protein binding of the tazobactam metabolite is negligible. Tazobactam is widely distributed into tissues and body fluids including intestinal mucosa, gall bladder, lung, female reproductive tissues, interstitial fluid and bile.
Ceftriaxone interferes with the biosynthesis of the Peptidoglycan component of the bacterial cell wall by binding to and inactivating Penicillin Binding Proteins (PBPs). Tazobactam is a penicillanic acid sulfone derivative with beta lactamase inhibitory properties. It enhances the activity of beta lactam antibacterials against beta lactamase producing bacteria.
Hypersensitivity to cephalosporins and beta lactamase inhibitors.
Dibact is generally well tolerated. Local reactions: Induration and tenderness, Phlebitis, hypersensitivity, rash; Hematologic: Eosinophilia, thrombocytosis and leucopenia; Gastrointestinal: Diarrhoea, nausea, vomiting, dysgeusia; Hepatic: Elevations of AST or ALT; Renal: elevations of the BUN.
