Cefoxitin

Chemical formula: C₁₆H₁₇N₃O₇S₂  Molecular mass: 427.452 g/mol  PubChem compound: 441199

Mechanism of action

Cefoxitin is a beta-lactam antibiotic of the group of the second-generation cephalosporins.

Pharmacodynamic properties

Spectrum of antibacterial activity

No European breakpoints for cefoxitin are recommended by EUCAST.

Acquired resistance prevalence may vary geographically and with time for some species. Therefore, information on the prevalence of local resistance is desirable, particularly for the treatment of severe infections. Data can give orientation on the susceptibility probabilities of a bacterial strain to this antibiotic.

Cefoxitin is active (in vitro) against the following microorganisms:

SUSCEPTIBLE SPECIES

Gram-positive aerobes:

Methicillin-Susceptible Staphylococcus
Streptococcus
Streptococcus pneumoniae

Gram-negative aerobes:

Moraxella catarrhalis
Citrobacter koseri
Escherichia coli
Haemophilus influenzae
Klebsiella oxytoca
Klebsiella pneumoniae
Neisseria gonorrhoeae
Proteus mirabilis
Proteus vulgaris
Providencia rettgeri
Providencia stuartii
Salmonella spp.
Shigella spp.

Anaerobes:

Bacteroides fragilis
Clostridium perfringens
Fusobacterium spp.
Peptostreptococcus spp.
Prevotella
Propionibacterium acnes
Veillonella spp.

Others:

Actinomyces

MODERATELY SUSCEPTIBEL SPECIES

(moderate in-vitro susceptibility)

Gram-negative aerobes:

Morganella morganii
Anaerobes
Eubacterium

RESISTANT SPECIES

Gram-positive aerobes:

Enterococcus
Listeria monocytogenes
Methicillin-Resistant Staphylococcus*

Gram-negative aerobes:

Acinetobacter
Campylobacter
Citrobacter freundii
Enterobacter aerogenes
Enterobacter cloacae
Legionella
Pseudomonas aeruginosa
Serratia marcescens
Vibrio
Yersinia enterocolitica

Anaerobes:

Clostridium difficile

Others:

Chlamydia
Mycobacteria
Mycoplasma

Pharmacokinetic properties

Distribution

In adults:

  • After an intravenous injection of 1 g, plasma concentrations of cefoxitin reached 125 µg/mL in 3 minutes, 72 µg/ml in 30 minutes and 15 µg/mL in 120 minutes.
  • After an intravenous injection of 2 g, plasma concentrations of cefoxitin reached 220 µg/mL in 3 minutes.
  • Elimination half-life is 45 minutes.

In patients with renal impairment whose creatinine clearance is between 10 and 30 mL/min, half-life exceeds 6 hours.

In patients with renal impairment whose creatinine clearance is <10 mL/min, half-life exceeds 13 hours.

Diffusion:

  • Extracellular fluid;
  • Synovial fluid;
  • Pericardial fluid;
  • Pleural fluid;
  • Mucus;
  • Aqueous humour;
  • Bile;
  • Human milk;
  • Umbilical cord and amniotic fluid;
  • Bone,
  • Gallbladder,
  • Heart,
  • Liver,
  • Lungs,
  • Myometrium,
  • Cerebrospinal fluid

Plasma protein binding: 65-80%.

Biotransformation

Cefoxitin does not undergo significant biotransformation.

Elimination

Cefoxitin is eliminated unchanged by the kidney.

In a number of studies investigating cefoxitin at intravenous doses of 1 g, the average amount of cefoxitin recovered in the urine ranged from 77-99% of the injected cefoxitin dose.

Preclinical safety data

Repeated dose toxicity studies and studies on reproduction and development did not reveal special hazard for humans. No safety pharmacology studies, genotoxicity assays nor carcinogenic study were performed.

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