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 intramuscular.]
Common side effects include nausea, allergic reactions, and inflammation at the site of injection.[ Another side effect may include Clostridioides difficile diarrhea.][ It is not recommended in people who have had previous anaphylaxis to a penicillin.][ It is relatively safe for use during pregnancy and breastfeeding.][
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Cefotaxime was discovered in 1976 and came into commercial use in 1980.[
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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:
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Lower respiratory tract infections – e.g. pneumonia (most commonly caused by S. pneumoniae)
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Genitourinary system infections – urinary tract infections (e.g. E. coli, S. epidermidis, P. mirabilis) and cervical/urethral gonorrhea
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Gynecologic infections – e.g. pelvic inflammatory disease, endometritis, and pelvic cellulitis
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Sepsis – secondary to Streptococcus spp., S. aureus, E. coli, and Klebsiella spp.
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Intra-abdominal infections – e.g. peritonitis
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Bone and joint infections – S. aureus, Streptococcus spp.
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CNS infections – e.g. meningitis/ventriculitis secondary to N. meningitidis, H. influenzae, S. pneumoniae
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.
Spectrum of activity
As a β-lactam antibiotic in the third-generation class of cephalosporins, cefotaxime is active against numerous Gram-positive and Gram-negative bacteria, including several with resistance to classic β-lactams such as penicillin. These bacteria often manifest as infections of the lower respiratory tract, skin, central nervous system, bone, and intra-abdominal cavity. While regional susceptibilities must always be considered, cefotaxime typically is effective against these organisms (in addition to many others):
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Staphylococcus aureus (not including MRSA) and S. epidermidis
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Streptococcus pneumoniae and S. pyogenes
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Escherichia coli
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Haemophilus influenzae
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Neisseria gonorrhoeae and N. meningitidis
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Klebsiella spp.
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Burkholderia cepacia
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Proteus mirabilis and P. vulgaris
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Enterobacter spp.
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Bacteroides spp.
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Fusobacterium spp.
Notable organisms against which cefotaxime is not active include Pseudomonas and Enterococcus.
The following represents MIC susceptibility data for a few medically significant microorganisms:
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H. influenzae: ≤0.007 – 0.5 μg/mL
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S. aureus: 0.781 – 172 μg/mL
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S. pneumoniae: ≤0.007 – 8 μg/mL
Historically, cefotaxime has been considered to be comparable to ceftriaxone (another third-generation cephalosporin) in safety and efficacy for the treatment of bacterial meningitis, lower respiratory tract infections, skin and soft tissue infections, genitourinary tract infections, and bloodstream infections, as well as prophylaxis for abdominal surgery.
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:
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Pain and inflammation at the site of injection/infusion (4.3%)
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Rash, pruritus, or fever (2.4%)
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Colitis, diarrhea, nausea, vomiting (1.4%)
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 lysis due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) in the absence of cell wall assembly.
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 beta lactamase.
Cefotaxime, like other beta-lactam antibiotics, does not only block the division of bacteria, including cyanobacteria, but also the division of cyanelles, the Photosynthesis of the , and the division of of . In contrast, it has no effect on the of the vascular plants. This supports the endosymbiotic theory and indicates an evolution of plastid division in land plants.
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.
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,
See also
External links
