Cefotaxime

Cefotaxime is an antibiotic used to treat several bacterial infections in humans, other animals, and plant tissue culture. Specifically in humans it is used to treat joint infections, pelvic inflammatory disease, meningitis, pneumonia, urinary tract infections, sepsis, gonorrhea, and cellulitis. It is given either by injection into a vein or muscle.[2]

Common side effects include nausea, allergic reactions, and inflammation at the site of injection.[2] Another side effect may include Clostridioides difficile diarrhea.[2] It is not recommended in people who have had previous anaphylaxis to a penicillin.[2] It is relatively safe for use during pregnancy and breastfeeding.[2][3] It is in the third-generation cephalosporin family of medications and works by interfering with the bacteria's cell wall.[2]

Cefotaxime was discovered in 1976 and came into commercial use in 1980.[4][5] It is on the World Health Organization's List of Essential Medicines.[6] It is available as a generic medication.[2]

Medical uses

It is a broad-spectrum antibiotic with activity against numerous gram-positive and Gram-negative bacteria.

Given its broad spectrum of activity, cefotaxime is used for a variety of infections, including:

Although cefotaxime has demonstrated efficacy in these infections, it is not necessarily considered to be the first-line agent. In meningitis, cefotaxime crosses the blood–brain barrier better than cefuroxime.

• Lower respiratory tract infections – e.g. pneumonia (most commonly caused by S. pneumoniae)
• Genitourinary system infections – urinary tract infections (e.g. E. coli, S. epidermidis, P. mirabilis) and cervical/urethral gonorrhea
• Gynecologic infections – e.g. pelvic inflammatory disease, endometritis, and pelvic cellulitis
• Sepsis – secondary to Streptococcus spp., S. aureus, E. coli, and Klebsiella spp.
• Intra-abdominal infections – e.g. peritonitis
• Bone and joint infections – S. aureus, Streptococcus spp.
• CNS infections – e.g. meningitis/ventriculitis secondary to N. meningitidis, H. influenzae, S. pneumoniae

Adverse reactions

Cefotaxime is contraindicated in patients with a known hypersensitivity to cefotaxime or other cephalosporins. Caution should be used and risks weighed against potential benefits in patients with an allergy to penicillin, due to cross-reactivity between the classes.

The most common adverse reactions experienced are:

• Pain and inflammation at the site of injection/infusion (4.3%)
• Rash, pruritus, or fever (2.4%)
• Colitis, diarrhea, nausea, vomiting (1.4%)[7]

Mechanism of action

Cefotaxime is a β-lactam antibiotic (which refers to the structural components of the drug molecule itself). As a class, β-lactams inhibit bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs). This inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) in the absence of cell wall assembly.[14] Due to the mechanism of their attack on bacterial cell wall synthesis, β-lactams are considered to be bactericidal.[7]

Unlike β-lactams such as penicillin and amoxicillin, which are highly susceptible to degradation by β-lactamase enzymes (produced, for example, nearly universally by S. aureus), cefotaxime boasts the additional benefit of resistance to β-lactamase degradation due to the structural configuration of the cefotaxime molecule. The syn-configuration of the methoxyimino moiety confers stability against β-lactamases.[15] Consequently, the spectrum of activity is broadened to include several β-lactamase-producing organisms (which would otherwise be resistant to β-lactam antibiotics), as outlined below.

Cefotaxime, like other

Administration

Cefotaxime is administered by intramuscular injection or intravenous infusion. As cefotaxime is metabolized to both active and inactive metabolites by the liver and largely excreted in the urine, dose adjustments may be appropriate in people with renal or hepatic impairment.[7][17][18]

Plant tissue culture

Cefotaxime is the only cephalosporin which has very low toxicity in plants, even at higher concentration (up to 500 mg/L). It is widely used to treat plant tissue infections with Gram-negative bacteria,[19] while vancomycin is used to treat the plant tissue infections with Gram-positive bacteria.[20][21]

See also

• Ceftazidime

External links