Cefmetazole

Absorption

Bioavailability is approximately 100% following intramuscular injection.

Toxicity

Oral LD50 in rats is 3,204 mg/kg. With other b-lactam antibiotics, adverse effects following overdosage have included nausea, vomiting, epigastric distress, diarrhea, and convulsions.

Description

Cefmetazole is a cephamycin with a nonaromatic side chain at C-7. In addition to a fairly characteristic second-generation cephalosporin antimicrobial spectrum, it possess fairly significant anti-antiaerobic activity. The ejection of its C-3 side chain leads to alcohol intolerance of the disulfuram type and prolonged clotting times.

General Description

Cefmetazole was synthesized by Sankyo Co. in 1976starting with a biosynthetic cephamycin. It shows excellent activity against Serratia and Proteus, against which cefazolin is not active, and it has stronger activity than cefoxitin, another derivative of cephamycin. Cefmetazole is active against anaerobes and resistant to β-lactamase, but it is not active against Pseudomonas aeruginosa.

Chemical properties

White Solid

The Uses of Cefmetazole

Semi-synthetic antibiotic derived from Cephamycin. Antibacterial.

The Uses of Cefmetazole

A broad spectrum second generation cephalosporin antibiotic

What are the applications of Application

Cefmetazole is a semi-synthetic antibiotic

Indications

For the treatment of infections caused by susceptible organisms.

Background

A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.

Definition

ChEBI: A cephalosporin antibiotic containg an N1-methyltetrazol-5-ylthiomethyl side-chain at C-3 of the parent cephem bicyclic structure.

Antimicrobial activity

It is active against Pr. mirabilis, Pr. vulgaris, Morganella morganii, Yersinia spp.and most anaerobes. S. marcescens is moderately susceptible, but Ps. aeruginosa and E. faecalis are resistant. It is active against Mycobacterium fortuitum and some strains of M. chelonei. It is resistant to a wide range of β-lactamases.
The serum concentration at the end of a 1 g intravenous infusion is around 77 mg/L. Plasma protein binding is 68%. It is principally excreted in the urine with a plasma half-life of c. 1.3 h; 70% is recovered over the first 6 h. In patients whose creatinine clearance is less than 10 mL/min, plasma levels are elevated and the plasma half-life is increased to around 15 h.
Side effects associated with the methylthiotetrazole group at position C-3 have been reported. Uses are similar to those of cefoxitin, but it is not widely available.

Pharmacokinetics

Cefmetazole is a second-generation cephalosporin. The cephalosporins are bactericidal drugs with both gram-positive and gram-negative activity. They inhibit bacterial cell wall synthesis in a way similar to the penicillins. Cefmetazole is more active than 1st-generation cephalosporins against indole-positive Proteus, Serratia, anaerobic gram-negative bacilli (including B. fragilis), and some E. coli, Klebsiella, and P. mirabilis, but is less active than cefoxitin or cefotetan against most gram-negative bacilli.

Metabolism

No appreciable metabolism.