• Tazobactam sodium packaged and labeled.

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SKU: T031

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Description

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.

    CAS Number

    89785-84-2

    Molecular Formula

    C10H11N4NaO5S

    Molecular Weight

    322.27

    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.

    Storage Conditions

    2-8°C

    Tariff Code

    2941.10.5000

    Spectrum

    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.

Applications

    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.

Specifications

    Form

    Powder

    Appearance

    White or off-white crystalline powder

    Impurity Profile

    Related Substances:
    Single Impurity: Not more than 2.0%
    Total Impurities: Not more than 4.0%

    Water Content (Karl Fischer)

    Not more than 4.0%

    pH

    5.0-7.0

    Assay

    (Anhydrous, Tazobactam): Not less than 87.5%

    Heavy Metals

    Not more than 20 ppm

References

    References

    Wishart, David. "Tazobactam." DrugBank. The Metabolomics Innovation Center, 13 June 2005. Web. 23 Aug. 2012.

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