Tazobactam Sodium (T031) is the sodium salt form of tazobactam, a penicillanic acid sulfone derivative and beta-lactamase inhibitor with antibacterial activity. Tazobactam was discovered by Dr. R.G. Micetech at the University of Alberta in 1982. Tazobactam contains a beta-lactam ring and irreversibly binds to beta-lactamase at or near its active site. This protects other beta-lactam antibiotics from beta-lactamase catalysis. This drug is used in conjunction with beta-lactamase susceptible penicillins to treat infections caused by beta-lactamase producing organisms.
Tazobactam alone showed an MIC of ≤ 8 mg/liter (range 2 to 32 mg/liter) against several Acinetobacter baumannii strains. Tazobactam in combination with piperacillin, successfully restored the activity of piperacillin against β-lactamase-producing bacteria. Tazobactam exhibited inhibitory activity and protected piperacillin against Richmond and Sykes types II, III, IV and V β-lactamases, staphylococcal penicillinase and extended-spectrum β-lactamases. Tazobactam showed species-specific activity against class I chromosomally-mediated enzymes.
TOKU-E offers two forms of Tazobactam: Tazobactam (T001) and Tazobactam Sodium (T031). Tazobactam sodium is soluble in water and methanol.
|Mechanism of Action||Tazobactam sodium contains a beta-lactam ring that binds strongly to beta-lactamase at or near its activation site, thereby permanently inhibiting enzymatic activity. This action protects other beta-lactam antibiotics (penicillins, cephalosporins, etc.) from beta-lactamase catalysis, thereby enhancing their antibacterial activity.|
Tazobactam exhibits little useful antimicrobial activity, although weak activity against Acinetobacter spp. and Borrelia burgdorferi has been reported.
Tazobactam inhibits a wide range of β-lactamases, including the group 2 penicillinases from Staph. aureus, the TEM-1 and SHV-1 β-lactamases, many extended-spectrum enzymes, and the common group 2e cephalosporinases of B. fragilis. Against the group 1 cephalosporinases, activity is strongly influenced by the amount of enzyme produced. The inhibitor-resistant group 2br β-lactamases are poorly inhibited and group 3 metallo-β-lactamases are not inhibited at clinically useful levels. It is a poor inducer of β-lactamases of Gram-positive and Gram-negative organisms.
|Impurity Profile||Related Substances:|
Single Impurity: Not more than 2.0%
Total Impurities: Not more than 4.0%
|Microbiology Applications||Tazobactam is often combined with the extended-spectrum β-lactam antibiotic piperacillin in the drug zosyn or Tazocin (piperacillin/tazobactam), used in infections due Pseudomonas aeruginosa. Tazobactam broadens the spectrum of piperacillin by making it effective against organisms that express β-lactamase and would normally degrade piperacillin.|
|References||Wishart, David. "Tazobactam." DrugBank. The Metabolomics Innovation Center, 13 June 2005. Web. 23 Aug. 2012.|