Ceforanide

Absorption

Rapidly absorbed following intramuscular injection.

Toxicity

Adverse effects following overdosage include nausea, vomiting, epigastric distress, diarrhea, and convulsions.

Description

Ceforanide is a second generation cephalosporin with good β-lactamase resistance. It has a serum half-life of about three hours, allowing twice-daily dosing.

Originator

Bristol (USA)

The Uses of Ceforanide

Ceforanide is a cephalosporin based antibiotic used in the sterilization in various medical procedures.

The Uses of Ceforanide

Cephalosporin antibiotic

Background

Ceforanide is administered parenterally. It has a longer elimination half-life than any currently available cephalosporin. Its activity is very similar to that of cefamandole, another second-generation cephalosporin antibiotic, except that ceforanide is less active against most gram-positive organisms. Many coliforms, including Escherichia coli, Klebsiella, Enterobacter, and Proteus, are susceptible to ceforanide, as are most strains of Salmonella, Shigella, Hemophilus, Citrobacter and Arizona species.

Indications

For the treatment of infections caused by susceptible organisms.

Definition

ChEBI: A second-generation cephalosporin antibiotic with {[1-(carboxymethyl)-1H-tetrazol-5-yl]sulfanyl}methyl and 2-(aminomethyl)phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. It is effective against many col forms, including Escherichia coli, Klebsiella, Enterobacter and Proteus, and most strains of Salmonella, Shigella, Hemophilus, Citrobacter and Ari ona species.

brand name

Precef (Apothecon).

Antimicrobial activity

A semisynthetic parenteral cephalosporin with activity broadly similar to that of cefalotin. Its activity in vitro is significantly reduced in the presence of serum. A 1 g intravenous dose achieves a concentration of c. 135 mg/L at the end of infusion. The response after 0.25, 0.5 and 1 g intravenous doses is essentially linear. A 1 g intramuscular dose produces mean peak values of around 70 mg/L. Plasma protein binding is around 85%.
It is almost entirely eliminated in the urine with a halflife of about 2.5 h, 80–95% being recovered in the first 12 h. The half-life is inversely related to renal function, rising to around 20 h when the creatinine clearance falls below 5 mL/min. About half the dose is removed by hemodialysis over 6 h.
It is generally well tolerated; phlebitis and pain at the site of injection are reported in some patients with occasional transient neutropenia and increased transaminase levels. It has been used principally for the treatment of infections due to Gram-positive cocci, including staphylococcal and streptococcal soft-tissue infections, but is no longer widely available.

Pharmacokinetics

Ceforanide is a semisynthetic 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.

Metabolism

The major drug elimination route was urinary excretion with 85% of the dose being excreted unchanged in the urine within 12 hr, and no metabolites with antibiotic activity were observed in urine.