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| Pronunciation | /ˌsɛfəˈtækˌsiːm/[1] |
| Trade names | Claforan, others |
| Other names | cefotaxime sodium |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a682765 |
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| Routes of administration | Intravenous andintramuscular |
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| Pharmacokinetic data | |
| Bioavailability | n/a |
| Metabolism | liver |
| Eliminationhalf-life | 0.8–1.4 hours |
| Excretion | 50–85%kidney |
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| ECHA InfoCard | 100.058.436 |
| Chemical and physical data | |
| Formula | C16H17N5O7S2 |
| Molar mass | 455.46 g·mol−1 |
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Cefotaxime is anantibiotic used to treat severalbacterial infections in humans, other animals, and plant tissue culture.[3] Specifically in humans it is used to treatjoint infections,pelvic inflammatory disease,meningitis,pneumonia,urinary tract infections,sepsis,gonorrhea, andcellulitis.[3] It is given either byinjection into a vein ormuscle.[3]
Common side effects include nausea,allergic reactions, and inflammation at the site of injection.[3] Another side effect may includeClostridioides difficile diarrhea.[3] It is not recommended in people who have had previousanaphylaxis to apenicillin.[3] It is relatively safe for use duringpregnancy andbreastfeeding.[3][4] It is in thethird-generation cephalosporin family of medications and works by interfering with the bacteria'scell wall.[3]
Cefotaxime was discovered in 1976 and came into commercial use in 1980.[5][6] It is on theWorld Health Organization's List of Essential Medicines.[7] It is available as ageneric medication.[3]
It is abroad-spectrum antibiotic with activity against numerousgram-positive andgram-negative bacteria.[citation needed]
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.[citation needed]
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):[8]
Notable organisms against which cefotaxime is not active includePseudomonas andEnterococcus.[9] As listed, it has modest activity against the anaerobicBacteroides fragilis.
The following represents MIC susceptibility data for a few medically significant microorganisms:
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.[12][13][14] The majority of these infections are caused by organisms traditionally sensitive to both cephalosporins. However, ceftriaxone has the advantage of once-daily dosing, whereas the shorter half-life of cefotaxime necessitates two or three daily doses for efficacy. Changing patterns in microbial resistance suggest cefotaxime may be suffering greater resistance than ceftriaxone, whereas the two were previously considered comparable.[15] Considering regional microbial sensitivities is also important when choosing any antimicrobial agent for the treatment of infection.[citation needed]
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.[citation needed]
The most common adverse reactions experienced are:
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 eventuallylyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) in the absence of cell wall assembly.[9] Due to the mechanism of their attack on bacterial cell wall synthesis, β-lactams are considered to bebactericidal.[8]
Unlike β-lactams such as penicillin and amoxicillin, which are highly susceptible to degradation by β-lactamase enzymes (produced, for example, nearly universally byS. aureus), cefotaxime boasts the additional benefit of resistance to β-lactamase degradation due to the structural configuration of the cefotaxime molecule. Thesyn-configuration of themethoxyimino moiety confers stability againstβ-lactamases.[16] 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.[citation needed]
Cefotaxime, like otherβ-lactam antibiotics, does not only block the division of bacteria, includingcyanobacteria, but also the division of cyanelles, thephotosyntheticorganelles of theglaucophytes, and the division ofchloroplasts ofbryophytes. In contrast, it has no effect on theplastids of thevascular plants. This supports theendosymbiotic theory and indicates anevolution of plastid division in land plants.[17]
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.[8][18][19]
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,[20] whilevancomycin is used to treat the plant tissue infections with Gram-positive bacteria.[21][22]
