indication

For the treatment of the infections (respiratory, skin, soft tissue, UTI, ENT) caused by S. pneumoniae, H. influenzae, staphylococci, S. pyogenes (group A beta-hemolytic streptococci), E. coli, P. mirabilis, Klebsiella sp, coagulase-negative staph

pharmacology

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 and 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.

mechanism of action

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.

half life

5.8-8.7 hours

route of elimination

Thirty-three percent to 67% of a ceftriaxone dose was excreted in the urine as unchanged drug and the remainder was secreted in the bile and ultimately found in the feces as microbiologically inactive compounds.

drug interactions

Acenocoumarol: The cephalosporin, ceftriaxone, may increase the anticoagulant effect of acenocoumarol.

Amikacin: Increased risk of nephrotoxicity

Anisindione: The cephalosporin, ceftriaxone, may increase the anticoagulant effect of anisindione.

Calcium Acetate: Calcium Salts (Intravenous) may enhance the adverse/toxic effect of Ceftriaxone. Ceftriaxone binds to calcium forming an insoluble precipitate. Concurrent or sequential use (within 48 hours) of ceftriaxone with calcium-containing solutions is contraindicated in neonates (28 days of age or younger). In other patients, these solutions can be used sequentially if the infusion lines are flushed with a compatible fluid between ceftriaxone and calcium-containing solution infusion.

Calcium Chloride: Calcium Salts (Intravenous) may enhance the adverse/toxic effect of ceftriaxone. Ceftriaxone binds to calcium forming an insoluble precipitate. Concurrent or sequential use (within 48 hours) of ceftriaxone with calcium-containing solutions is contraindicated in neonates (28 days of age or younger). In other patients, these solutions can be used sequentially if the infusion lines are flushed with a compatible fluid between ceftriaxone and calcium-containing solution infusion.

Dicumarol: The cephalosporin, ceftriaxone, may increase the anticoagulant effect of dicumarol.

Gentamicin: Increased risk of nephrotoxicity

Kanamycin: Increased risk of nephrotoxicity

Neomycin: Increased risk of nephrotoxicity

Netilmicin: Increased risk of nephrotoxicity

Streptomycin: Increased risk of nephrotoxicity

Tobramycin: Increased risk of nephrotoxicity

Warfarin: The cephalosporin, ceftriaxone, may increase the anticoagulant effect of warfarin.