What is piperacillin/tazobactam sodium injection, and how does it work (mechanism of action)?

Zosyn is an injectable combination of two antibiotics, piperacillin and tazobactam, with broad spectrum activity against an extended range of bacterial species. Piperacillin is an extended-spectrum penicillin antibiotic, but it can be destroyed by an enzyme produced by bacteria called beta lactamase. Tazobactam inhibits beta lactamase and prevents the destruction of piperacillin. Therefore, tazobactam is given with piperacillin to enhance the activity of piperacillin in eradicating bacterial infections.

Piperacillin kills bacteria by inhibiting the synthesis of bacterial cell walls. It binds preferentially to specific penicillin-binding proteins (PBPs) located inside bacterial cell walls. PBPs vary among bacterial species, and thus susceptibility to piperacillin depends on the ability of piperacillin to bind to each species' specific PBPs.

In-vitro studies of piperacillin and tazobactam have shown that the combination has activity against a variety of gram-positive and gram-negative aerobic and anaerobic bacteria.

Susceptible bacteria include:

  • Aerobic and facultative gram-positive microorganisms: Staphylococcus aureus
  • Aerobic and facultative gram-negative microorganisms: Acinetobacter baumannii, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, and Pseudomonas aeruginosa
  • Gram-negative anaerobes: Bacteroides fragilis group (B.fragilis, B. ovatus, B. thetaiotaomicron, and B. vulgatus)
  • Piperacillin and tazobactam was approved by the US Food and Drug Administration (FDA) in October 1993.

What brand names are available for piperacillin/tazobactam sodium injection?

Zosyn

Is piperacillin/tazobactam sodium injection available as a generic drug?

GENERIC AVAILABLE: Yes

Do I need a prescription for piperacillin/tazobactam sodium injection?

Yes

What are the uses for piperacillin/tazobactam sodium injection?

The combination of piperacillin and tazobactam (Zosyn) is used to treat a variety of bacterial infections, including:

What are the side effects of piperacillin/tazobactam sodium injection?

Common side effects associated with piperacillin/tazobactam include:

Rare side effects occurring with a frequency of less than 1% are:

SLIDESHOW

Bacterial Infections 101: Types, Symptoms, and Treatments See Slideshow

What is the dosage for piperacillin/tazobactam sodium injection?

Zosyn should be administered by intravenous infusion over 30 minutes.

The usual daily dose of Zosyn for adults is 3.375 g every six hours totaling 13.5 g (12.0 g piperacillin/1.5 g tazobactam).

Initial presumptive treatment of patients with nosocomial pneumonia should start with Zosyn at a dosage of 4.5 g every six hours plus an aminoglycoside, totaling 18.0 g (16.0 g piperacillin/2.0 g tazobactam).

Dosage in patients with renal impairment (≤40 mL/min of CRCL) and dialysis patients should be reduced, based on the degree of actual renal function impairment.

For children with appendicitis and/or peritonitis the recommended Zosyn dosage is 100 mg piperacillin/12.5 mg tazobactam per kilogram of body weight, every 8 hours in pediatric patients 9 months of age and older. For pediatric patients 2 to 9 months of age, the recommended dosage is 80 mg piperacillin/10 mg tazobactam per kilogram of body weight, every 8 hours.

Zosyn and aminoglycosides should be reconstituted, diluted, and administered separately. Co-administration via Y-site can be done under certain conditions.

Which drugs or supplements interact with piperacillin/tazobactam sodium injection?

  • Probenecid may inhibit the renal tubular secretion (elimination via the kidneys) of piperacillin/tazobactam. This may cause higher, prolonged blood levels of piperacillin/tazobactam. The half-life of piperacillin is prolonged by 21% and the half-life of tazobactam by 71%.
  • Piperacillin/tazobactam may inhibit platelet aggregation (formation of a blood clot) which may increase the risk for bleeding. Co-administration with blood thinning agents such as warfarin (Coumadin) requires close monitoring for signs or symptoms of bleeding.
  • Piperacillin/tazobactam may prolong the neuromuscular blockade of vecuronium (Norcuron).
  • Piperacillin/tazobactam may decrease the renal (kidney) elimination of methotrexate (Trexall). Patients on concurrent therapy with methotrexate should be monitored frequently for signs or symptoms of methotrexate toxicity.

QUESTION

Bowel regularity means a bowel movement every day. See Answer

Is piperacillin/tazobactam sodium injection safe to take if I'm pregnant or breastfeeding?

No evidence of fetal harm has been reported from use of piperacillin/tazobactam, piperacillin alone, and tazobactam alone in mice and rats (animal studies). Piperacillin/tazobactam is known to cross the placenta. Piperacillin/tazobactam is approved for the treatment of postpartum infections. As with all medications, piperacillin/tazobactam should be used cautiously in pregnancy. Potential benefits of treatment should be weighed against any potential risk to the fetus. Piperacillin and tazobactam is classified as FDA pregnancy risk category C.

Piperacillin is excreted into human milk in small amounts. Excretion of tazobactam in human milk has not been studied. Due to the lack of safety data, piperacillin/tazobactam should be used cautiously in females who are breastfeeding.

What else should I know about piperacillin/tazobactam sodium injection?

What preparations of piperacillin/tazobactam sodium injection are available?

  • Piperacillin and tazobactam for injection is supplied as a powder for reconstitution (mixing).
  • Powder for solution for injection: 2.25, 3.375, 4.5, 40.5 g

How should I keep piperacillin/tazobactam sodium injection stored?

Piperacillin and tazobactam vials should be stored at controlled room temperature, between 20 C to 25 C (68 F to 77 F), before reconstitution.

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Summary

Piperacillin and tazobactam (Zosyn) is a combination of two antibiotics prescribed to treat a variety of bacterial infections such as pneumonia, appendicitis, pelvic inflammatory disease, E. coli infection, cellulitis, and postpartum endometriosis. Review side effects, drug interactions, dosage, and pregnancy safety information prior to taking this medication.

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Medically Reviewed on 10/15/2019
References
Medically reviewed by John P. Cunha, DO, FACOEP

REFERENCE:

FDA Prescribing information.
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