Tazobactamisapenicillanicacidsulfonederivativeandbeta-lactamaseinhibitorwithantibacterialactivity.TazobactamwasdiscoveredbyDr.R.G.MicetechattheUniversityofAlbertain1982.Tazobactamcontainsabeta-lactamringandirreversIBLybindstobeta-lactamaseatornearitsactivesite.Thisprotectsotherbeta-lactamantibioticsfrombeta-lactamasecatalysis.Thisdrugisusedinconjunctionwithbeta-lactamasesusceptiblepenicillinstotreatinfectionscausedbybeta-lactamaseproducingorganisms.
TazobactamaloneshowedanMICof≤8mg/liter(range2to32mg/liter)againstseveralAcinetobacterbaumanniistrains.Tazobactamincombinationwithpiperacillin,successfullyrestoredtheactivityofpiperacillinagainstβ-lactamase-producingbacteria.TazobactamexhibitedinhibitoryactivityandprotectedpiperacillinagainstRichmondandSykestypesII,III,IVandVβ-lactamases,staphylococcalpenicillinaseandextended-spectrumβ-lactamases.Tazobactamshowedspecies-specificactivityagainstclassIchromosomally-mediatedenzymes.
TOKU-Eofferstwoformsoftazobactam:tazobactam(T001)andtazobactamsodium(T031).Tazobactamisslightlysolubleinaqueoussolution(9.59mg/mL).Tazobactamsodiumisfreelysolubleinaqueoussolution.
CASNumber
89786-04-9
MolecularFormula
C10H12N4O5S
MolecularWeight
300.29
MechanismofAction
Tazobactamcontainsabeta-lactamringthatbindsstronglytobeta-lactamaseatornearitsactivationsite,therebypermanentlyinhibitingenzymaticactivity.Thisactionprotectsotherbeta-lactamantibiotics(penicillins,cephalosporins,etc.)frombeta-lactamasecatalysis,therebyenhancingtheirantibacterialactivity.
StorageConditions
2-8°C
TariffCode
2941.10.5000
Spectrum
Tazobactamexhibitslittleusefulantimicrobialactivity,althoughweakactivityagainstAcinetobacterspp.andBorreliaburgdorferihasbeenreported. Tazobactaminhibitsawiderangeofβ-lactamases,includingthegroup2penicillinasesfromStaph.aureus,theTEM-1andSHV-1β-lactamases,manyextended-spectrumenzymes,andthecommongroup2ecephalosporinasesofB.fragilis.Againstthegroup1cephalosporinases,activityisstronglyinfluencedbytheamountofenzymeproduced.Theinhibitor-resistantgroup2brβ-lactamasesarepoorlyinhibitedandgroup3metallo-β-lactamasesarenotinhibitedatclinicallyusefullevels.Itisapoorinducerofβ-lactamasesofGram-positiveandGram-negativeorganisms.
