Cefotiam
Systematic (IUPAC) name
(6R,7R)-7-{[2-(2-amino-1,3-thiazol-4-yl)acetyl]
amino}-3-{[1-(2-dimethylaminoethyl)tetrazol-5-yl]
sulfanylmethyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]
oct-2-ene-2-carboxylic acid
Clinical data
Trade names Pansporin
AHFS/Drugs.com
Legal status
  • (Prescription only)
Routes of
administration
Intravenous, intramuscular
Pharmacokinetic data
Bioavailability 60% (intramuscular)
Protein binding 40%
Metabolism Nil
Biological half-life Approximately 1 hour
Excretion Renal
Identifiers
CAS Registry Number  YesY
ATC code J01
PubChem CID:
DrugBank  YesY
ChemSpider  YesY
UNII  YesY
KEGG  YesY
ChEBI  YesY
ChEMBL  YesY
Chemical data
Formula C18H23N9O4S3
Molecular mass 525.631 g/mol
 YesY   

Cefotiam is a parenteral second-generation cephalosporin antibiotic. It has broad-spectrum activity against Gram-positive and Gram-negative bacteria. As a beta-lactam, its bactericidal activity results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins.

Cefotiam was launched as Pansporin in February 1981 by Takeda Pharmaceutical of Japan and has been available as a generic since February 1993.

Mechanism of action

Cefotiam inhibits final cross-linking stage of peptidoglycan production, thus inhibiting bacterial cell wall synthesis. It has similar or less activity against Gram-positive staphylococci and streptococci, but is resistant to some beta-lactamases produced by Gram-negative bacteria. It is more active against many of the Enterobacteriaceae including Enterobacter, E. coli, Klebsiella, Salmonella and indole-positive Proteus species.

In clinical use, high concentrations of cefotiam are observed in several tissues (kidney, heart, ear, prostate, and genital tract), as well as in fluids and secretions (bile, ascitic fluid).

Spectrum of bacterial susceptibility

Cefotiam has a broad spectrum of activity and has been used to treat infections caused by a number of enteric bacteria and bacteria responsible for causing skin infections. The following represents MIC susceptibility data for a few medically significant bacteria.

  • Bacteroides fragilis: - 16 - >128 μg/ml
  • Clostridium difficile: >128 μg/ml
  • Staphylococcus aureus: 0.25 - 32 μg/ml

[1]

Indications

This drug is indicated for prophylaxis for surgical infection, postoperative infections, bacterial Pseudomonas aeruginosa.

Dosage

For adults, the dose is up to 6 grams daily by intravenous or intramuscular route in divided doses according to severity of infection. In patients with renal impairment a dose reduction may be needed.

Adverse effects

Side effects include nausea and vomiting, diarrhoea, hypersensitivity reactions, nephrotoxicity, convulsions, CNS toxicity, hepatic dysfunction, haematologic disorders, pain at injection site, thrombophloebitis, pseudomembranous colitis, and superinfection with prolonged use.

External links

  1. ^ http://www.toku-e.com/Assets/MIC/Cefotiam%20hydrochloride.pdf