Cefotaxime is an

antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of ...

used to treat a number of bacterial infections in human, other animals and plant tissue culture. Specifically in humans it is used to treat

joint infections Acute septic arthritis, infectious arthritis, suppurative arthritis, osteomyelitis, or joint infection is the invasion of a joint by an infectious agent resulting in joint inflammation. Generally speaking, symptoms typically include redness, hea ...

pelvic inflammatory disease Pelvic inflammatory disease, also known as pelvic inflammatory disorder (PID), is an infection of the upper part of the female reproductive system, namely the uterus, fallopian tubes, and ovaries, and inside of the pelvis. Often, there may be no ...

meningitis Meningitis is acute or chronic inflammation of the protective membranes covering the brain and spinal cord, collectively called the meninges. The most common symptoms are fever, headache, and neck stiffness. Other symptoms include confusion or ...

, pneumonia, urinary tract infections, sepsis, gonorrhea, and cellulitis. It is given either by injection into a vein or

muscle Skeletal muscles (commonly referred to as muscles) are organs of the vertebrate muscular system and typically are attached by tendons to bones of a skeleton. The muscle cells of skeletal muscles are much longer than in the other types of muscl ...

. Common side effects include nausea, allergic reactions, and inflammation at the site of injection. Another side effect may include ''Clostridium difficile'' diarrhea. It is not recommended in people who have had previous anaphylaxis to a

penicillin Penicillins (P, PCN or PEN) are a group of β-lactam antibiotics originally obtained from ''Penicillium'' moulds, principally '' P. chrysogenum'' and '' P. rubens''. Most penicillins in clinical use are synthesised by P. chrysogenum using ...

. It is relatively safe for use during pregnancy and breastfeeding. It is in the third-generation cephalosporin family of medications and works by interfering with the bacteria's

cell wall A cell wall is a structural layer surrounding some types of cells, just outside the cell membrane. It can be tough, flexible, and sometimes rigid. It provides the cell with both structural support and protection, and also acts as a filtering mech ...

. Cefotaxime was discovered in 1976, and came into commercial use in 1980. It is on the World Health Organization's List of Essential Medicines. It is available as a

generic medication A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active ch ...

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: * 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.

, 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'' 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. Cefotaxima

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):U.S. Food and Drug Administration. U.S. Department of Health and Human Services. ''Claforan Sterile (cefotaxime for injection, USP) and Injection (cefotaxime injection, USP)''. 19 June 2009. * ''Staphylococcus aureus'' (not including MRSA) and ''S. epidermidis'' * ''Streptococcus pneumoniae'' and ''S. pyogenes'' * ''Escherichia coli'' * ''Haemophilus influenzae'' * ''Neisseria gonorrhoeae'' and ''N. meningitidis'' * ''Klebsiella'' spp. * ''Burkholderia cepacia'' * ''Proteus mirabilis'' and ''P. vulgaris'' * ''Enterobacter'' spp. * ''Bacteroides'' spp. * ''Fusobacterium'' spp. Notable organisms against which cefotaxime is not active include '' Pseudomonas'' and '' Enterococcus''. As listed, it has modest activity against the anaerobic '' Bacteroides fragilis''. The following represents MIC susceptibility data for a few medically significant microorganisms: * ''H. influenzae'': ≤0.007 – 0.5 µg/mL * ''S. aureus'': 0.781 – 172 µg/mL * ''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. 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. Considering regional microbial sensitivities is also important when choosing any antimicrobial agent for the treatment of infection.

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%)

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

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due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) in the absence of cell wall assembly.Cefotaxime drug information
Due to the mechanism of their attack on bacterial cell wall synthesis, β-lactams are considered to be

bactericidal A bactericide or bacteriocide, sometimes abbreviated Bcidal, is a substance which kills bacteria. Bactericides are disinfectants, antiseptics, or antibiotics. However, material surfaces can also have bactericidal properties based solely on their ...

. 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 methoxy imino moiety confers stability against β-lactamases. 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 β-lactam antibiotics, does not only block the division of bacteria, including

cyanobacteria Cyanobacteria (), also known as Cyanophyta, are a phylum of gram-negative bacteria that obtain energy via photosynthesis. The name ''cyanobacteria'' refers to their color (), which similarly forms the basis of cyanobacteria's common name, blu ...

, but also the division of cyanelles, the

photosynthetic Photosynthesis is a process used by plants and other organisms to convert light energy into chemical energy that, through cellular respiration, can later be released to fuel the organism's activities. Some of this chemical energy is stored in c ...

organelle In cell biology, an organelle is a specialized subunit, usually within a cell, that has a specific function. The name ''organelle'' comes from the idea that these structures are parts of cells, as organs are to the body, hence ''organelle,'' the ...

s of the glaucophytes, and the division of

chloroplast A chloroplast () is a type of membrane-bound organelle known as a plastid that conducts photosynthesis mostly in plant and algal cells. The photosynthetic pigment chlorophyll captures the energy from sunlight, converts it, and stores it in ...

s of bryophytes. In contrast, it has no effect on the

plastid The plastid (Greek: πλαστός; plastós: formed, molded – plural plastids) is a membrane-bound organelle found in the Cell (biology), cells of plants, algae, and some other eukaryotic organisms. They are considered to be intracellular endosy ...

s of the vascular plants. This supports the

endosymbiotic theory Symbiogenesis (endosymbiotic theory, or serial endosymbiotic theory,) is the leading evolutionary theory of the origin of eukaryotic cells from prokaryotic organisms. The theory holds that mitochondria, plastids such as chloroplasts, and possibl ...

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,cefotaxime for plant tissue culture
while vancomycin is used to treat the plant tissue infections with Gram-positive bacteria.vancomycin for plant cell culture

References

External links

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