TazobactamSodium(T031)isthesodiumsaltformoftazobactam,apenicillanicacidsulfonederivativeandbeta-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).Tazobactamsodiumissolubleinwaterandmethanol.
CASNumber
89785-84-2
MolecularFormula
C10H11N4NaO5S
MolecularWeight
322.27
MechanismofAction
Tazobactamsodiumcontainsabeta-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.
