Piperacillin is a broad-spectrum semi-synthetic penicillin with antibacterial activity against many gram-positive and gram-negative aerobic and anaerobic bacteria, and it acts as a bactericidal by inhibiting the synthesis of bacterial septums and cell walls.
Tazobactam, also known as triazol methylpenicillin sulfone, has a low affinity for penicillin-binding proteins and has little clinically relevant antimicrobial activity in vitro, but it is an inhibitor of a variety of β-lactamase. However, it is not possible to inhibit AmpC enzymes or metal β-lactamase. β-lactamases include plasmids and chromosome-mediated enzymes that often cause bacterial resistance to penicillins and cephalosporins, including third-generation cephalosporins. It has inhibitory effects on β-lactamase enzymes of molecular classification A [including Richmond-Sykes classification III (Bush classifications 2b and 2b') penicillinase and cephalosporin enzymes], which have a large difference in inhibition capacity of II and IV (2a and 4) penicillinase, and have no inducing effect on chromosomally-mediated β-lactamase at tazobactam concentrations achieved by the recommended dosage regimen.
In the piperacillin /tazobactam formulation, the antimicrobial profile of piperacillin is enhanced and expanded due to the presence of tabactam, making it effective against many β-lactamase bacteria that were previously resistant to piperacillin and other β-lactam antibiotics. Thus, the piperacillin/tazobactam combination formulation has the dual characteristics of a broad-spectrum antibiotic and a β-lactamase inhibitor.
Instructions before antimicrobial spectrum comparison (taking Pfizer as an example):
Instructions before 2015:
Piperacillin/tazobactam has high antimicrobial activity against piperacillin-sensitive microorganisms as well as piperacillin-resistant β-lactamase organisms.
Instruction manuals after 2016:
Both in vitro studies and clinical infections have demonstrated that piperacillin/tazobactam has antimicrobial activity against most of the isolates of the following microorganisms. (indicated in red)
The following in vitro data have been obtained, but the clinical significance is unclear. For the following microorganisms, the minimum in vitro inhibitory concentration (MIC) of piperacillin / tazobactam is at least 90% less than or equal to the sensitive vertices. However, the safety and efficacy of piperacillin/tazobactam in the treatment of clinical infections caused by these bacteria has not been confirmed in adequate and well-controlled clinical trials. (indicated in green)
Sandford Guidelines for Antimicrobial Therapy (Fever 46th Edition):
Recommendation: The drug is a first-line recommended treatment drug, and the in vitro test activity is credible, clinically effective, the guidelines recommend, and the Sanford guidelines recommend the first-line drugs
Sensitivity: the drug is an alternative treatment option (in vitro tests are active, similar in efficacy compared with known active drugs, clinically may be effective, but due to ultra-broad spectrum, lack of clinical experience of toxicity, lack of direct and effective evidence, etc., for clinical applications, listed as second-line drugs)
Indeterminate: uncertain antimicrobial activity, effective in some cases, in some types of staining, but uncertain in other types or efficacy, or recommended for combination therapy or there have been reports of failure of treatment
Not recommended: poor antimicrobial activity, resistant or possibly treated, or poorly permeable or toxic or lacking evidence of effective treatment
No data available: there is a lack of supporting evidence for treatment
Gram-positive bacteria:
Includes β-lactamase-producing and β-lactamase-producing bacteria:
Staphylococcus aureus (methicillin-resistant Staphylococcus aureus), Staphylococcus epidermidis (coagulase-negative staphylococcus), Staphylococcus saprophysis
Streptococcus spp. (Streptococcus pneumoniae, Streptococcus purpurulentis, Streptococcus bovis, Streptococcus aureus, Streptococcus cymbidium, Type G)
Enterococcus (Enterococcus faecalis, Enterococcus faecalis), Corynebacterium, Listeria monocytogenes, Nukaella.
Staphylococcus aureus (methicillin-sensitive isolates only), Staphylococcus epidermidis (methicillin-sensitive isolates only)
Streptococcus pneumoniae (penicillin-sensitive isolates only), Streptococcus pyogenes, Streptococcus amassa, Streptococcus grass;
Enterococcus faecalis (ampicillin or penicillin-sensitive isolates only)
In the Guidelines for Antimicrobial Therapy at Sandford (Fever 46th Edition): Piperacillin tazobactam is sensitive to Staphylococcus saprophyllum and is recommended as amoxicillin clavulanate potassium and cefazolin. Enterococcus excreta is uncertain. Listeria monocytogenes is sensitive and the first line is ampicillin. There is no data on Nuccabacterium, and the first line recommends imipenem.
In the National Guidelines for Antimicrobial Therapy (1st Edition), the sensitivity of piperacillintazobactam to Enterococcus faecalis is 30% to 60%. There are no data on Listeria monocytogenes.
Gram-negative bacteria:
Including β-lactamase- and β-lactamase-producing strains:
Acinetobacter spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp. (including Klebsiella acid-producing, Klebsiella pneumoniae), Pseudomonas aeruginosa, Citric acid bacteria (including Bacterium fibrus, Brucellosis), Moraxella spp. (including Catalanhamella), Morganella mortisella, Neisseria gonorrhoeae, Proteus mirabilis common Proteus, Serratia spp. (including Serratia sacli, Serratia liquefied), Spiraginus, Reissidens, Reis, Salmonella
Enterobacter species (including Enterobacter gutiss, Enterobacter aerogenes), Ortho-Shiga monospores, Shigella spp., Neisseria meningitidis, Haemophilus parainfluenzae, Pasteurella multicleracidis, Yersinia spp., Campylobacter spp., Gardnerella vaginalis, Pseudomonas onion, Pseudomonas fluorescent monosporum, Monosporus flaviophilus maltophilus
In vitro studies have shown that piperacillin/tazobactam is synergistic with aminoglycoside antibiotics against pseudomonas aeruginosa.
Acinetobacter, Escherichia coli, Haemophilus influenzae (except for isolates that are β-lactamase-negative and resistant to ampicillin), Kleb's pneumoniae, Pseudomonas aeruginosa (in combination with aminoglycosides sensitive to this isolate).
Gramcilis citrates, Moraxella catarrhalis, Morganella morris, Neisseria gonorrhoeae, Proteus mirabilis, Proteus common, Serratia mucinalis, Providenceella stiflora, Profidenella recheri, Salmonella
In the Guidelines for Antimicrobial Therapy of Sandford (Fever 46th Edition): Piperacillintazobactam is sensitive to Enterobacter species; Sensitive to Shigella, the first line is recommended as ciprofloxacin, levofloxacin; sensitive to Neisseria meningitidis, the first line is recommended as amoxicillin, ampicillin, ceftriaxone; sensitive to Pasteurella polycycline, penicillin VK, amoxicillin, ampicillin clavulanate, ampicillin sulbactam, ampicillin sulbactam; and not recommended for Yersinia Not recommended for Pseudomonas onion; indeterminate for Maltophilus flaviviflora.
In the National Guidelines for Antimicrobial Therapy (1st Edition), the sensitivity of piperacillintazobactam to Enterobacter, Shigella and Neisseria meningitidis exceeds 60%,; the sensitivity to Pasteurella polyclimide is less than 30%,; pseudomonas onion is not available; and the sensitivity to Maltophilus flaviflorus is 30% to 60%.
Anaerobic bacteria:
These include β-lactamase-producing and anaerobic bacteria that do not produce β-lactamase
Bacteroides belong to the Bacteroides fragile family (including Bacteroides fragilis, Bacteroides fragilis ovate species, Bacteroides fragilis polyform species, Bacteroides fragilis common species), Clostridium aeratus- Clostridium aeratus, Bacteroides fragilis species, and Bacteroides melanin-producing species
Bacteroides are a family of Bacteroides fragile (Bacteroides fragile monoform species, Bacteroides fragile do not understand glycophilus species)
Bacteroides (including Bacteroides dipridii, glycolytic bacterium, Bacteroides polychaetes, Bacteroides oral)
Streptococcus digestion, Clostridium, Eubacterium, Clostridium spp. (including Clostridium difficile), Coccidioides fischerii (Veron) and Actinomycetes
Bacteroides fragilis (Bacteroides fragilis, Ovale, Bacteroides polyforme, and Bacteroides commonplacea)
Clostridium aerophes, Bacteroides bacterium, Prevoella heliogenes
These bacteria do not produce β-lactamase and are only sensitive to piperacillin
In the Sandford Guidelines for Antimicrobial Therapy (Fever 46th Edition): Piperacillin tazobactam is sensitive to Clostridium spp., and the first line is recommended as penicillin G; Sensitive to digestive streptococcus, the first line is recommended as penicillin G, penicillin VK, amoxicillin, ampicillin, and not recommended for Clostridium difficile.
In the National Guidelines for Antimicrobial Therapy (1st Edition), the sensitivity rate of piperacillintazobactam to Clostridium (Clostridium non-difficulty) and Streptococcus digestion exceeded 60%; there were no data on Clostridium difficile and Actinomycetes.