Daily Medication Pearl: Ceftolozane and Tazobactam (Zerbaxa)

Zerbaxa is a combination of ceftolozane, a cephalosporin-like antibacterial, and tazobactam, a beta-lactamase inhibitor.

Indication: Zerbaxa is a combination of ceftolozane, a cephalosporin-like antibacterial, and tazobactam, a beta-lactamase inhibitor, indicated for the treatment of patients 18 years of age and older with hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (HABP). /VABP), caused by susceptible Gram-negative microorganisms Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, and Serratia marcescens; for treatment of patients 18 years of age and older with complicated urinary tract infections (cUTI) caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Pseudomonas aeruginosa; and in combination with metronidazole for the treatment of patients 18 years of age and older with complicated intra-abdominal infections (cIAI) caused by susceptible Gram-negative and Gram-positive microorganisms Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Bacteroides fragilis, Streptococcus anginosus, Streptococcus constellatus, and Streptococcus salivarius.

Insight:

  • Dosage: 1.5 to 3g.
  • Dosage forms: Zerbaxa 1.5 g for injection is supplied as a sterile powder for reconstitution in single-dose vials containing ceftolozane 1 g (equivalent to 1.147 g ceftolozane sulfate) and tazobactam 0.5 g (equivalent to 0.537 g tazobactam sodium).
  • Adverse events: The most frequent adverse reactions in adult patients (≥ 5% in the cIAI or cUTI indication) are nausea, diarrhoea, headache and pyrexia.
  • Action mechanism: Ceftolozane belongs to the cephalosporin class of antibacterial drugs. The bactericidal action of ceftolozane results from inhibition of cell wall biosynthesis and is mediated by binding to penicillin-binding proteins (PBPs). Ceftolozane is a PBP inhibitor of P. aeruginosa (for example, PBP1b, PBP1c and PBP3) and E.coli (for example, PBP3). Tazobactam sodium has little clinically relevant in vitro activity against bacteria due to its reduced affinity for penicillin-binding proteins. It is an irreversible inhibitor of certain beta-lactamases (eg, certain penicillinases and cephalosporinases) and can covalently bind to certain bacterial chromosomal and plasmid beta-lactamases.

Source: zerbaxa_pi.pdf (merck.com)

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