SulbactamsodiumisanirreversIBLeinhibitorofseveralbacterialpenicillinasesandcephalosporinases.Inthepresenceoflowconcentrationsofsulbactam,ampicillinandotherbeta-lactamsreADIlyinhibitthegrowthofavarietyofresistantbacteriathatcontainbeta-lactamases.SulbactamwasfirstdevelopedbythecentralresearchdivisionofPfizer,Inc.andwasfirstdescribedin1978.Sulbactamsodiumusedalonedisplaysonlyweakantibacterialactivity,withthenotableexceptionofitspotenteffectsonsusceptibleandresistantstrainsofNeisseriagonorrhoeae.Sulbactamsodiumappearstobesomewhatlesspotentbutmarkedlymorestable(inaqueoussolution)thanthebeta-lactamaseinhibitorclavulanicacid.

SulbactamSodiumisabletoinhibitthemostcommonformsofβ-lactamasebutisnotabletointeractwiththeAmpCcephalosporinase.Thus,itconferslittleprotectionagainstbacteriasuchasPseudomonasaeruginosa,Citrobacter,Enterobacter,andSerratia,whichoftenexpressthisgene.

Sulbactamiscommonlycombinedtoformampicillin/sulbactam(2:1).ItdoespossesssomeantibacterialactivitywhenadmiNISTeredalone,butitistooweaktohaveanyclinicalimportance.

Recently,sulbactamhasbeenusedintreatingAcinetobactersepticemiaandisreceivingrenewedinterest.Synonyms:(2S,5R)-3,3-dimethyl-7-oxo-4-thia-1-azABIcyclo[3.2.0]heptane-2-carboxylicacid4,4-dioxidesodium,Betamaze,CP45899,CP-45,899,Penicillanicacid1,1-dioxidesodium,PenicillanicacidS,S-dioxidesodium,Penicillanicaciddioxidesodium,Penicillanicacidsulfonesodium

CASNumber

69388-84-7

MolecularFormula

C₈H₁₀NNaO₅S

MolecularWeight

255.22

MechanismofAction

Sulbactamsodiumcontainsabeta-lactamringthatbindsstronglytobeta-lactamaseatornearitsactivationsite,therebypermanentlyinhibitingenzymaticactivity.Thisactionprotectsotherbeta-lactamantibiotics(penicillins,cephalosporins,etc.)frombeta-lactamasecatalysis,therebyenhancingtheirantibacterialactivity.Sulbactamalsoshowsantibacterialactivityagainstvariousstrains,sulbactamabletobindtoandinhibitpenicillinbindingproteinsPBP1andPBP3.Thisantibacterialactivityvariesdependingonspecies.

StorageConditions

2-8°C

TariffCode

2941.10.5000

Spectrum

AntimicrobialactivitySulbactamsodiumhasveryweakantimicrobialactivityagainstmostbacteria.ItsonlynotableactivityisagainstN.gonorrhoeae,N.meningitidisAcinetobacterbaumannii.Beta-Lactamaseactivity

Sulbactamsodiuminhibitsawiderangeofgroup2β-lactamases,includingthosefromStaph.aureus,K.pneumoniaeandB.fragilis.Itisagood-to-moderateinhibitoroftheTEMenzymesofgroups2band2bebuthaslittleeffectongroup1,group2brorgroup3β-lactamases.ItdoesnotinducetheactivityofcephalosporinasesfromGram-negativebacteriabutisaweakinducerofpenicillinasesfromStaph.aureus.

Aconcentrationof4–8mg/Lrestorestheactivityofampicillinformanyβ-lactamase-producingstrainsofStaph.aureus,H.influenzae,Mor.catarrhalis,enterobacteriaandB.fragilis,butthereisalargeinoculumeffect.

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