Ceftriaxone is a broad spectrum antibiotic which interferes with the biosynthesis of the peptidoglycan component of the bacterial cell wall by binding to and inactivating penicllin-binding proteins (PBPs).
Sulbactum is Β lactamase inhibitor.Ceftriaxone & Sulbactam For Injection is a combination of a beta-lactam antibiotic- Ceftriaxone with an inhibitor of beta lactamase, giving a highly powerful antibacterial formulation useful in the treatment of broad spectrum of infections caused by organisms resistant to the antibiotic alone.
- Sepsis, Meningitis, Abdominal Infections (e.g. Peritonitis, Infections of the Biliary tract), Infections of the Bones, Joints, Soft Tissue, Skin and of Wounds, Renal and Urinary Tract Infections, Respiratory Tract infections, particularly Pneumonia, and Ear, Nose and Throat Infections, and uncomplicated Gonorrhoea.
- May also be used for Peri-operative Prophylaxis of Infections. A single dose given Preoperatively may reduce chances of Postoperative Infection.
Mechanism of ActionCeftriaxone is a beta-lactam antibiotic like the penicillins with bactericidal action. Penicillin-binding proteins (PBPs) are responsible for several steps in the synthesis of the cell wall of bacteria and are found in large quantities.Ceftriaxone inhibits the third and final stage of bacterial cell wall synthesis by preferentially binding to the specific PBPs located inside the bacterial cell wall.
Ceftriaxone interferes with PBP-mediated cell wall synthesis leading to cell lysis, which is mediated by bacterial cell wall autolytic enzymes (autolysins), possibly through interference with an autolysin inhibitor. The presence of an aminothiazolyl-acetyl side chain with an alphaâ€"methoxyimino group at the 7-position of the beta-lactam ring provides Ceftriaxone with enhanced antibacterial activity, particularly against the Enterobacteriaceae (e.g., E. coli, Klebsiella, Proteus, and Serratia) and increased stability against many of the beta-lactamases. Many strains of Pseudomonas aeruginosa are susceptible to Ceftriaxone. Other susceptible gram-negative organisms include Enterobacter, Citrobacter, Morganella, Providencia, Moraxella (Branhamella) catarrhalis, and N. meningitidis. Ceftriaxone has exceptional activity against H. influenzae and N. gonorrhoeae and is the drug of choice for uncomplicated N. gonorrhoeae infections. Sulbactam, by irreversibly binding to the beta-lactamases produced by the common gram-positive or negative bacteria protects the beta-lactam ring of ceftriaxone, and conserves the activity. Thus on combining ceftriaxone with sulbactam, the combination product - Ceftriaxone & Sulbactam For Injection extends its utility in the treatment of broad range of infections caused by organisms resistant to the antibiotic alone, making them susceptible, possibly through lowering of MIC.
Irrespective of the dose Ceftriaxone has a half-life of between 6 to 9 hours. The half-life may be prolonged in neonates. While moderate renal impairment may not affect the half-life of Ceftriaxone appreciably, severe renal impairment does, with a longer half-life, which is further increased if accompanied with liver impairment. Ceftriaxone at 1 - 2 g dose achieves concentrations above the MICS in the lung, heart, biliary tract/liver, tonsil, middle ear and nasal mucosa, bone; and cerebral, pleural, prostatic and synovial fluids for most of the pathogens responsible for infection, even after more than 24 hours. Urinary excretion by glomerular filtration accounts for 50-60% of the elimination. The intestinal flora has been shown to convert ceftriaxone into inactive metabolites.
Biliary route accounts for 40-50% of excretion. In case of renal impairment the biliary excretion may be the major pathway for excretion.
In Infants& Children: Elimination half-life in neonates is prolonged which decreases with increasing postnatal age. In infants aged less than 8 days and in elderly persons aged over 75 years, the average elimination half-life is usually 2 - 3 times that seen in the adults.
In patients with renal failure, non-renal elimination may compensate. Sulbactam has a half-life of about 1 hour in healthy volunteers. Serum concentrations reached are proportional to the dose administered. It is predominantly eliminated through kidney in the unchanged form.
- Ceftriaxone & Sulbactam For Injection is contraindicated in patients with known allergy to Cephalosporin group of antibiotics. Hypersensitivity to penicillin may pre-dispose the patient to the possibility of allergic cross-reactions.
- Pregnancy and Lactation: No evidence of embryotoxicity, fetotoxicity or teratogenicity was observed. However, this drugshould be used during pregnancy only if clearly needed. As ceftriaxone is secreted in the breast-milk, albeit at low concentrations, caution should be exercised in nursing mothers.
- Mutagenicity/Carcinogenicity/Fertility: In vitro tests show that Ceftriaxone is not mutagenic. No animal studies have been carried out to check the carcinogenic potential of Ceftriaxone.
- Gastrointestinal: Diarrhoea, nausea & vomiting (less frequent), stomatitis, and glossitis.
- Hepatic: Elevations of SGOT/SGPT.
- Hematological:Eosinophilia, thrombocytopenia, leukopenia, granulocytopenia, hematoma or bleeding. Hemolytic anemia is observed less frequently.
- Agranulocytosis (< 500/mm3) has been reported occasionally at a total cumulative dose exceeding 20 g.
- Skin reactions: Exanthema, allergic dermatitis, pruritis, urticaria, edema, erythema multiforme. Other side effects such as headache, dizziness, increase in serum creatinine, mycosis of the genital tract, oliguria, fever, and shivering have been observed.
- Anaphylactic shock may occur which requires immediate counter-measures.