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 ...

used to treat a number of

bacterial infections Pathogenic bacteria are bacteria that can cause disease. This article focuses on the bacteria that are pathogenic to humans. Most species of bacteria are harmless and are often beneficial but others can cause infectious diseases. The number of ...

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 n ...

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 Sepsis, formerly known as septicemia (septicaemia in British English) or blood poisoning, is a life-threatening condition that arises when the body's response to infection causes injury to its own tissues and organs. This initial stage is follo ...

, gonorrhea, and

cellulitis Cellulitis is usually a bacterial infection involving the inner layers of the skin. It specifically affects the dermis and subcutaneous fat. Signs and symptoms include an area of redness which increases in size over a few days. The borders of th ...

. It is given either by

injection into a vein Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrie ...

or muscle. Common side effects include nausea,

allergic reactions Allergies, also known as allergic diseases, refer a number of conditions caused by the hypersensitivity of the immune system to typically harmless substances in the environment. These diseases include hay fever, food allergies, atopic dermati ...

, 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 Anaphylaxis is a serious, potentially fatal allergic reaction and medical emergency that is rapid in onset and requires immediate medical attention regardless of use of emergency medication on site. It typically causes more than one of the follow ...

to a penicillin. It is relatively safe for use during pregnancy and

breastfeeding Breastfeeding, or nursing, is the process by which human breast milk is fed to a child. Breast milk may be from the breast, or may be expressed by hand or pumped and fed to the infant. The World Health Organization (WHO) recommends that brea ...

. It is in the

third-generation cephalosporin The cephalosporins (sg. ) are a class of β-lactam antibiotics originally derived from the fungus ''Acremonium'', which was previously known as ''Cephalosporium''. Together with cephamycins, they constitute a subgroup of β-lactam antibiotics ...

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 me ...

. 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.

Medical uses

It is a

broad-spectrum antibiotic A broad-spectrum antibiotic is an antibiotic that acts on the two major bacterial groups, Gram-positive and Gram-negative, or any antibiotic that acts against a wide range of disease-causing bacteria. These medications are used when a bacterial in ...

with activity against numerous gram-positive and

gram-negative bacteria Gram-negative bacteria are bacteria that do not retain the crystal violet stain used in the Gram staining method of bacterial differentiation. They are characterized by their cell envelopes, which are composed of a thin peptidoglycan cell wall ...

. 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 Sepsis, formerly known as septicemia (septicaemia in British English) or blood poisoning, is a life-threatening condition that arises when the body's response to infection causes injury to its own tissues and organs. This initial stage is follo ...

– 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 Ventriculitis is the inflammation of the ventricles in the brain. The ventricles are responsible for containing and circulating cerebrospinal fluid throughout the brain. Ventriculitis is caused by infection of the ventricles, leading to swelling ...

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 Methicillin-resistant ''Staphylococcus aureus'' (MRSA) is a group of Gram-positive bacteria that are genetically distinct from other strains of ''Staphylococcus aureus''. MRSA is responsible for several difficult-to-treat infections in humans. ...

) 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 ''Pseudomonas'' is a genus of Gram-negative, Gammaproteobacteria, belonging to the family Pseudomonadaceae and containing 191 described species. The members of the genus demonstrate a great deal of metabolic diversity and consequently are able to ...

'' and '' Enterococcus''. As listed, it has modest activity against the anaerobic ''

Bacteroides fragilis ''Bacteroides fragilis'' is an anaerobic, Gram-negative, pleomorphic to rod-shaped bacterium. It is part of the normal microbiota of the human colon and is generally commensal, but can cause infection if displaced into the bloodstream or surroun ...

''. 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

lyse Lyse may refer to: * Lyse Abbey, a former Cistercian abbey in Norway * Lyse, an alternative name of Lysebotn, Norway * Lyse Energi, a Norwegian power company * Łyse, Masovian Voivodeship, a village in east-central Poland * Łyse, Podlaskie Voi ...

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 In organic chemistry, a methoxy group is the functional group consisting of a methyl group bound to oxygen. This alkoxy group has the formula . On a benzene ring, the Hammett equation classifies a methoxy substituent at the ''para'' position as ...

imino In organic chemistry, an imine ( or ) is a functional group or organic compound containing a carbon–nitrogen double bond (). The nitrogen atom can be attached to a hydrogen or an organic group (R). The carbon atom has two additional single bon ...

moiety confers stability against

β-lactamase Beta-lactamases, (β-lactamases) are enzymes () produced by bacteria that provide multi-resistance to beta-lactam antibiotics such as penicillins, cephalosporins, cephamycins, monobactams and carbapenems ( ertapenem), although carbapene ...

s. 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, but also the division of cyanelles, the photosynthetic

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

bryophyte The Bryophyta s.l. are a proposed taxonomic division containing three groups of non-vascular land plants (embryophytes): the liverworts, hornworts and mosses. Bryophyta s.s. consists of the mosses only. They are characteristically limited in s ...

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

vascular plants Vascular plants (), also called tracheophytes () or collectively Tracheophyta (), form a large group of land plants ( accepted known species) that have lignified tissues (the xylem) for conducting water and minerals throughout the plant. They a ...

. 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,cefotaxime for plant tissue culture
while

vancomycin Vancomycin is a glycopeptide antibiotic medication used to treat a number of bacterial infections. It is recommended intravenously as a treatment for complicated skin infections, bloodstream infections, endocarditis, bone and joint infection ...

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

References

External links

* {{portal bar, Medicine Cephalosporin antibiotics Thiazoles Ketoximes Acetate esters World Health Organization essential medicines Wikipedia medicine articles ready to translate Sanofi