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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.
Ceftriaxone binds to one or more of the penicillin-binding proteins (PBPs) which inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell wall, thus inhibiting biosynthesis and arresting cell wall assembly resulting in bacterial cell death.
Absorption: Peak plasma concentrations after 2 hr (IM).
Absorption: Peak plasma concentrations after 2 hr (IM).
Distribution: Distributed widely into body tissues and fluids; CSF (therapeutic concentrations). Crosses the placenta and enters breast milk; bile (high concentrations).
Protein-binding: 85-95%.
Excretion: Via the urine (40-65% as unchanged); via the bile to the faeces (remainder as unchanged and microbiologically inactive compounds); 6-9 hr (elimination half-life).
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. By binding to these enzymes, Ceftriaxone results in the formation of of defective cell walls and cell death.
