Cefotiam
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| Systematic (IUPAC) name | |
|---|---|
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(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 | International Drug Names |
| Routes of administration | Intravenous, intramuscular |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 60% (intramuscular) |
| Protein binding | 40% |
| Metabolism | Nil |
| Biological half-life | Approximately 1 hour |
| Excretion | Renal |
| Identifiers | |
| CAS Number |
61622-34-2  |
| ATC code | J01DC07 (WHO) |
| PubChem | CID 43708 |
| DrugBank |
DB00229 |
| ChemSpider |
39831 |
| UNII |
91W6Z2N718 |
| KEGG |
D07648 |
| ChEBI |
CHEBI:355510 |
| ChEMBL |
CHEMBL1296 |
| Chemical data | |
| Formula | C18H23N9O4S3 |
| Molar mass | 525.631 g/mol |
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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
Indications
This drug is indicated for prophylaxis for surgical infection, postoperative infections, bacterial septicaemia, bone and joint infections, cholangitis, cholecystitis, peritonitis, prostatitis, pyelonephritis, respiratory tract infections, skin and soft tissue infections, cystitis, urethritis, and infections caused by susceptible organisms. It does not have activity against 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
- Müller R, Böttger C, Wichmann G (2003). "Suitability of cefotiam and cefuroxime axetil for the perioperative short-term prophylaxis in tonsillectomy patients.". Arzneimittelforschung 53 (2): 126–32. doi:10.1055/s-0031-1297083. PMID 12642969.
- Kolben M, Mandoki E, Ulm K, Freitag K (2001). "Randomized trial of cefotiam prophylaxis in the prevention of postoperative infectious morbidity after elective cesarean section.". Eur J Clin Microbiol Infect Dis 20 (1): 40–2. doi:10.1007/s100960000365. PMID 11245321.
- Shimizu S, Chen K, Miyakawa S (1996). "Cefotiam-induced contact urticaria syndrome: an occupational condition in Japanese nurses.". Dermatology 192 (2): 174–6. doi:10.1159/000246352. PMID 8829507.
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