This document discusses beta-lactamase inhibitors which are used to combat bacteria that have developed resistance to beta-lactam antibiotics like penicillins and cephalosporins. It explains that beta-lactamase enzymes produced by bacteria inactivate beta-lactam antibiotics by breaking the beta-lactam ring. The three main inhibitors discussed are clavulanic acid, sulbactam, and tazobactam, which are commonly used in combination with other antibiotics. Clavulanic acid is well-absorbed orally and re-establishes activity against common resistant bacteria. Sulbactam has less potency than clavulanic acid and is preferably given parenter

1. BETA-LACTAMASE
INHIBITORS
DR RAVI KUMAR S
PEDIATRIC RESIDENT
MGMCRI

2. BETA-LACTAM
Antibiotics which contain beta lactam ringsin theirmolecular
structuresare :
• Penicillin
• Cephalosporins
• Monobactum
• Carbapenem

3. MOA
• It interfereswith bacterial cell wall synthesis
• It inhibitsthe transpeptidases so that cross linkingdoes not take place
• Cross linkages between peptide chains of the neighbouringstrands
provides stabilityand rigiditytothe cell wall.

4. BETA-LACTAM INHIBITORS
• β-lactamasesare afamilyof enzymesproduced bymanygram-positive andgram-
negative bacteria thatinactivate β-lactamantibioticsbyopening the β-lactam
ring.
• Different β-lactamasesdiffer in their substrate affinities.
• Three inhibitors of this enzymeare Clavulanicacid,Sulbactamand Tazobactam
areavailablefor clinical use.

5. CLAVULANIC ACID
• Hasarapid oral absorption
• Additionof clavulanicacidre-establishes theactivityof amoxicillinagainst β-
lactamaseproducing resistant Staph.aureus (butnot MRSA), H. influenzae, N.
gonorrhoeae, E.coli,Proteus, Klebsiella, Salmonella and Shigella.
• Indicatedfor Respiratory tract,Skin& Softtissue, intra abdominalinfections.
• Dosage: 100mg/kg/dayin4 divided doses

6. SULBACTUM
• 2–3timesless potent thanclavulanicacid
• Oral absorptionofsulbactamis inconsistent.Therefore, it is preferably given
parenterally
• Ithasbeencombinedwith ampicillinfor useagainst β-lactamaseproducing
resistant strains
• UsedcommonlyinSurgicalInfections& Gonorrhea.
• DosageAmpicillinwithSulbactum: 200mg/kg/dayin4 divided doses

7. TAZOBACTUM
• Itis similar to sulbactam.
• Itspharmacokineticsmatcheswith piperacillin with whichit hasbeen combined
for use insevere infectionslike peritonitis, pelvic/urinary/respiratory infections
causedby β-lactamaseproducing bacilli.
• Dosage: Piperacillin+Tazobactum: 200-300mg/kg/dayin3 divided doses

8. THANKYOU