beta-Lactamase Inhibitors

Endogenous substances and drugs that inhibit or block the activity of BETA-LACTAMASES.
DrugDrug NameDrug Indication
DB01606TazobactamTazobactam is used in combination with piperacillin or ceftolozane to broaden the spectrum of piperacillin antibacterial action, treating susceptible infections. As with any other antibiotic, tazobactam should only be used for infections that are either proven or strongly suspected to be susceptible to the tazobactam containing drug. **Tazobactam-piperacillin** When combined with piperacillin, it is used to treat a variety of infections, including those caused by aerobic and facultative gram-positive and gram-negative bacteria, in addition to gram-positive and gram-negative anaerobes. Some examples of infections treated with piperacillin-tazobactam include cellulitis, diabetic foot infections, appendicitis, and postpartum endometritis infections.[L4417] Certain gram-negative bacilli infections with beta-lactamase producing organisms cannot be treated with piperacillin-tazobactam, due to a gene mutation conferring antibiotic resistance.[A179266] **Tazobactam-ceftolozane** Tazobactam-ceftolozane combined with metronidazole is used to treat complicated urinary tract infections (UTI) and complicated intra-abdominal infections, as well as ventilator-associated bacterial pneumonia and hospital-acquired bacterial pneumonia.[FDA label]. This combination increases efficacy against infections with gram-negative bacilli.[A7657]
DB09324SulbactamSulbactam is currently available in combination products with ampicillin. Within this formulation it is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below. Skin and Skin Structure Infections caused by beta-lactamase producing strains of Staphylococcus aureus, Escherichia coli, Klebsiella spp. (including K. pneumoniae), Proteus mirabilis, Bacteroides fragilis, Enterobacter spp., and Acinetobacter calcoaceticus. Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli, Klebsiella spp. (including K. pneumoniae), Bacteroides spp. (including B. fragilis), and Enterobacter spp. Gynecological Infections caused by beta-lactamase producing strains of Escherichia coli, and Bacteroides spp. (including B. fragilis).
DB00766Clavulanic acidClavulanic acid combined with other antibiotics is indicated to prevent the development of drug-resistant strains of bacteria and promotes their therapeutic antibacterial effects.[L7880,L7904] The following conditions, when they produced beta-lactamases, have been treated with a combination of amoxicillin and clavulanic acid or ticarcillin and clavulanic acid[L7880,L7904]: Acute otitis media caused by H. influenzae and M. catarrhalis Sinusitis due to H. influenzae and M. catarrhalis Lower respiratory tract infections due to Haemophilus influenzae, S.aureus, Klebsiella species, and Moraxella catarrhalis Skin and skin structure infections caused by Staphylococcus aureus, Escherichia coli, and Klebsiella species Urinary Tract Infections due to E. coli, Klebsiella species of bacteria, and Enterobacter species of bacteria, S.marcescens, or S.aureus Gynecologic infections due to a variety of bacteria, including P.melaninogenicus, Enterobacter species, E.Coli species, Klebsiella species, S. aureus, S.epidermidis Septicemia due to a variety of bacteria, including Klebsiella species, E.Coli species, S.aureus, or Pseudomonas species Bone and joint infections due to S.aureus Intraabdominal infections due to E.Coli, K.pnemoniae, or B.fragilis group **A note on susceptibility** It should be noted that it is only to be administered in infections that are confirmed or highly likely to be caused by susceptible bacteria. Culture and susceptibility tests should be performed if possible and used in selecting whether this antibiotic is prescribed. When beta-lactamase enzyme production is not detected during microbiological testing, clavulanic acid should not be used. When these tests are not available patterns of local infection and susceptibility may be used to determine the appropriateness of using clavulanic acid.[L7880] Ticarcillin with clavulanate has shown particular efficacy in mixed infections in addition to empiric therapy before determining the susceptibility of causative organisms. The ticarcillin-clavulanic acid combination may prove to be an effective single-agent antibiotic therapy to treat infections where a regimen of several drugs may normally be used.[L7904]
DB09060AvibactamAVYCAZ (ceftazidime-avibactam), in combination with metronidazole, is indicated for the treatment of complicated intra-abdominal infections caused by the following susceptible microorganisms: Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Providencia stuartii, Enterobacter cloacae, Klebsiella oxytoca, and Pseudomonas aeruginosa in patients 18 years or older. AVYCAZ is also indicated for the treatment of complicated urinary tract infections including pyelonephritis caused by the following susceptible microorganisms: Escherichia coli, Klebsiella pneumoniae, Citrobacter koseri, Enterobacter aerogenes, Enterobacter cloacae, Citrobacter freundii, Proteus spp., and Pseudomonas aeruginosa in patients 18 years or older.
DB11593Isatoic anhydrideNot Available
DB12377RelebactamRelebactam is indicated in combination with [imipenem] and [cilastatin] for the treatment of complicated urinary tract infections, including pyelonephritis, and complicated intra-abdominal infections caused by susceptible organisms in adults.[label]
DB12107VaborbactamIndicated in combination with meropenem for the treatment of patients 18 years of age and older with complicated urinary tract infections (cUTI) including pyelonephritis caused by the following susceptible microorganisms: _Escherichia coli_, _Klebsiella pneumoniae_, and _Enterobacter cloacae_ species complex.[FDA Label]
DrugDrug NameTargetType
DB01606TazobactamBeta-lactamase TEMtarget
DB01606TazobactamSolute carrier family 22 member 6transporter
DB01606TazobactamSolute carrier family 22 member 8transporter
DB01606TazobactamBeta-lactamase Ohio-1target
DB01606TazobactamBeta-lactamase SHV-1target
DB09324SulbactamBeta-lactamasetarget
DB00766Clavulanic acidBacterial beta-lactamase enzymesenzyme
DB00766Clavulanic acidBacterial beta-lactamase enzymestarget
DB00766Clavulanic acidSodium/glucose cotransporter 1transporter
DB09060AvibactamCanalicular multispecific organic anion transporter 1transporter
DB09060AvibactamSolute carrier family 22 member 8transporter
DB09060AvibactamBeta-lactamase TEMtarget
DB09060AvibactamBeta-lactamase CTX-Mtarget
DB09060AvibactamBeta-lactamasetarget
DB09060AvibactamBeta-lactamase SHV-1target
DB09060AvibactamBeta-lactamase SHV-2target
DB09060AvibactamBeta-lactamase SHV-1target
DB09060AvibactamClass D OXA-48 carbapenemasetarget
DB09060AvibactamCarbapenem-hydrolyzing beta-lactamase KPCtarget
DB09060AvibactamBeta-lactamase CTX-M-15target
DB09060AvibactamExtended-spectrum beta-lactamase PER-1target
DB12377RelebactamSolute carrier family 22 member 8transporter
DB12377RelebactamSolute carrier family 22 member 11transporter
DB12377RelebactamMultidrug and toxin extrusion protein 1transporter
DB12377RelebactamMultidrug and toxin extrusion protein 2transporter
DB12377RelebactamBeta-lactamase TEMtarget
DB12377RelebactamBeta-lactamase SHV-1target
DB12377RelebactamBeta-lactamase CTX-Mtarget
DB12377RelebactamBeta-lactamase (KPC-2)target
DB12377RelebactamBeta-lactamasetarget
DB12107VaborbactamBeta-lactamasetarget
DB12107VaborbactamCarbapenem-hydrolyzing beta-lactamase KPCtarget
DB12107VaborbactamBeta-lactamase (KPC-2)target
DB12107VaborbactamBeta-lactamase CTX-Mtarget
DB12107VaborbactamBeta-lactamase (blaSHV)target
DB12107VaborbactamBeta-lactamase SHV-1target
DB12107VaborbactamBeta-lactamase TEMtarget
DB12107VaborbactamBeta-lactamase (MIR-1)target
DB12107VaborbactamBeta-lactamasetarget