| 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 |
| Pharmacodynamics |
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. |
| Absorption |
Not Available |
| Volume of distribution |
|
| Protein binding |
95% |
| Metabolism |
Not Available |
| 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. |
| Half life |
5.8-8.7 hours |
| Clearance |
- 0.58 – 1.45 L/h [healthy adults receiving 0.15-3 g of CEFTRIAXONE]
|
| Toxicity |
Not Available |
