Ceftriaxone Sodium

Ceftriaxone is a broad-spectrum third-generation cephalosporin antibiotic. It has a very long half-life compared to other cephalosporins and is high penetrable into the meninges, eyes, and inner ear. Ceftriaxone has broader and stronger gram-negative coverage then first or second-generation cephalosporins, but worse activity against methicillin-susceptible S.aureus. Ceftriaxone is a commonly used antimicrobial due to its good activity against multi-drug resistant Enterobacteriaceae, its relatively safe adverse effect profile, and its long half-life which allows for the convenience of daily or twice-daily dosing.

Ceftriaxone is a broad-spectrum cephalosporin antibiotic used for the treatment of bacterial infections in various locations, such as in the respiratory tract, skin, soft tissue, and urinary tract.

Ceftriaxone is used for the treatment of the infections (respiratory, skin, soft tissue, UTI, ENT) caused by susceptible organisms. Organisms that are generally susceptible to ceftriaxone include S. pneumoniae, S. pyogenes (group A beta-hemolytic streptococci), coagulase-negative staphylococci, Some Enterobacter spp, H. influenzae, N. gonorrhoeae, P. mirabilis, E. coli, Klebsiella spp, M. catarrhalis, B. burgdorferi, and some oral anaerobes.

• Arthritis gonococcal
• Bacterial Endocarditis
• Bacterial Infections
• Bacterial Sepsis
• Bacterial Sinusitis
• Bone and Joint Infections
• Brain abscess
• Chancroid
• Community Acquired Pneumonia (CAP)
• Conjunctivitis gonococcal neonatal
• Epididymitis
• Epiglottitis
• Gonococcal infection of pharynx
• Gonococcal pelvic inflammatory disease
• Intra-Abdominal Infections
• Lower respiratory tract infection bacterial
• Lyme Neuroborreliosis
• Meningitis
• Bacterial
• Ophthalmia neonatorum due to gonococcus
• Postoperative Infections
• Prosthetic Joint Infection
• Salmonella Typhi Infection
• Septic Arthritis
• Shigellosis
• Skin and Subcutaneous Tissue Bacterial Infections
• Syphilis
• Vulvovaginitis gonococcal
• Whipple Disease
• Bacterial otitis media
• Complicated Bacterial Urinary Tract Infections
• Susceptible Bacterial Infections
• Uncomplicated Gonorrhea
• Uncomplicated Urinary tract infection bacterial

Ceftriaxone is a cephalosporin/cephamycin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. Ceftriaxone has in vitro activity against gram-positive aerobic, gram-negative aerobic, and anaerobic bacteria. The bactericidal activity of ceftriaxone results from the inhibition of cell wall synthesis and is mediated through ceftriaxone binding to penicillin-binding proteins (PBPs). Ceftriaxone is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended-spectrum beta-lactamases. However, resistance to ceftriaxone usually occurs through beta-lactamase hydrolysis, altered PBPs, or reduced bacterial cell permeability. Ceftriaxone should not be mixed with or giving in the same IV line as diluents/products containing calcium as they may cause ceftriaxone to precipitate. Ceftriaxone use may also cause biliary sludge or gallbladder pseudolithiasis.

Ceftriaxone works by inhibiting the mucopeptide synthesis in the bacterial cell wall. The beta-lactam moiety of ceftriaxone binds to carboxypeptidases, endopeptidases, and transpeptidases in the bacterial cytoplasmic membrane. These enzymes are involved in cell-wall synthesis and cell division. Binding of ceftriaxone to these enzymes causes the enzyme to lose activity; therefore, the bacteria produce defective cell walls, causing cell death.

Ceftriaxone is only given as an injection, either intramuscularly or intravenously. Ceftriaxone is less than 1% bioavailable if given orally.

The apparent volume of distribution of an intravenous or intramuscular dose in healthy patients is 5.78 to 13.5 L. The volume of distribution of an intravenous or intramuscular dose in septic patients is 6.48 to 35.2 L. Ceftriaxone has good enough CSF penetration to be used as an effective treatment of bacterial meningitis.

Ceftriaxone is 95% protein bound.

Ceftriaxone is primarily eliminated in the urine (33-67%). The remainder is eliminated through secretion in the bile and removed from the body via the feces.

The elimination half-life of ceftriaxone is 5.8-8.7 hours. The half-life of ceftriaxone in the middle ear fluid has been estimated to be 25 hours.

The plasma clearance of ceftriaxone in healthy adults receiving a 0.15-3g dose is 0.58 to 1.45 L/hour. The renal clearance of ceftriaxone is 0.32 to 0.73 L/hour. In intensive care unit patients, ceftriaxone's total drug clearance was 0.96L/h (0.55-1.28 L/h), and unbound drug clearance was 1.91 L/h (1.46-6.20 L/h).

Ceftriaxone overdose may increase the risk of urolithiasis and subsequent post-renal acute renal failure (PARF). Other symptoms of overdose unavailable in the literature. However, they are likely similar to the adverse effects of the medication. If overdose of ceftriaxone occurs, treat with symptomatic and supportive treatment, as ceftriaxone levels will not be reduced by dialysis.

No interactions found.

• Pneumonia, Bronchitis, Acute bacterial otitis media, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections, Meningitis: 1 to 2 g IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 4 gm/day
• Uncomplicated gonococcal infections: 250 mg IM as a single dose
• Surgical prophylaxis: 1 g IV as a single dose 30 to 120 minutes before surgery

• Pneumonia, Bronchitis, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections: 50 to 75 mg/kg IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 2 gm/day
• Acute bacterial otitis media: 50 mg/kg IM in single dose; Maximum dose: 1 gm/day
• Meningitis: 100 mg/kg IV or IM in single daily dose or (or in equally divided doses twice a day); Maximum dose: 4 gm/day