Acinetobacter calcoaceticus Enterobacter aerogenes Enterobacter cloacae
Escherichia coli Hemophilus influenzae (including ampicllin resistant and beta lactamase producing strains) Hemophilus parainfluenzae Kleibsella oxytoca Kleibsella pneumoniae Moraxella catarhalis (including beta lactamase producing strains) Morganella morganii Neiserria gonorrhoeae (including penicillinase and non penicillinase producing strains Neiserria meningitides Proteus mirabilis Serratia marcescens Ceftriaxone is also active against many strains of Pseudomonas aeruginosa

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.

The usual adult dose is 1000/500/250 mg of Ceftriaxone/tazobactam given once a day (or equally in divided doses) depending upon the severity of the infection. The total daily dose should not exceed 4g.

For the treatment of serious infections, the recommended dose is 50-75 mg/kg (in terms of ceftriaxone) given every 12 hours. The total dose should not exceed 2g.

Although the transient elevations of BUN and serum creatinine have been observed at the recommended dosage the nephrotoxic potential of Ceftriaxone / Tazobactam is similar to that of other cephalosporins. Ceftriaxone / Tazobactam should be prescribed with caution in individuals with a history of gastrointestinal disease especially colitis. Alterations in prothrombin times have occurred rarely in patients treated with ceftriaxone tazobactam.

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.

Reproductive studies have been performed in mice and rats at doses upto 20 times the usual human dose and have no evidence of embryotoxicity, fetotoxicity or teratogenicity. In primates no embryotoxicity or teratogenicity was demonstrated at a dose of approximately 3 times the human dose. There are however no adequate and well controlled studies in pregnant women. Because animal reproductive studies are not always predictive of human response this drug should be used during pregnancy only if clearly needed.

Low concentration of Ceftriaxone-tazobactam is excreted in human milk. Caution should be exercised when ceftriaxone /tazobactam is administered to a nursing woman.

Limited information is present on the acute toxicity of Ceftriaxone/Tazobactam. There is no specific antidote. If acute overdosage of ceftriaxone/tazobactam occurs, supportive and symptomatic treatment should be initiated.

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