indication

For treatment of infections caused by susceptible bacteria.

pharmacology

Cephapirin is a first-generation cephalosporin that has a wide spectrum of activity against gram-positive and gram-negative organisms. Cephapirin is more resistant to beta-lactamases than are the penicillins and so is effective against staphylococci, with the exception of methicillin-resistant staphylococci.

mechanism of action

The bactericidal activity of cephapirin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).

toxicity

Rats exposed via the oral route to cephapirin displayed low acute toxicity (LD₅₀ = 14000 mg/kg). The most common adverse reactions are hypersensitivity reactions and alterations to liver function. Evidence of white blood cell disorders and anaemia were noted in some subjects.

biotransformation

Major metabolite detected is desacetylcephapirin.

drug interactions

Amikacin: Increased risk of nephrotoxicity

Gentamicin: Increased risk of nephrotoxicity

Netilmicin: Increased risk of nephrotoxicity

Tobramycin: Increased risk of nephrotoxicity