Beta-lactamase inhibitors

Beta-lactamase inhibitors - substances that inhibit beta-lactamases - a group of bacterial enzymes that destroy beta-lactam antibiotics .

Content

History

In 1940, an enzyme that breaks down penicillin was found in Escherichia coli . Since then, a rather large number of enzymes have been described that in one place or another destroy the beta-lactam ring of penicillin and cephalosporins ^[1] .

The mechanism of development of bacterial resistance to beta-lactam antibiotics

The main mechanism for the development of bacterial resistance to beta-lactam antibiotics is the production of beta-lactamase enzymes that destroy the beta-lactam ring of these drugs. This mechanism is one of the leading ones for clinically significant pathogens such as Staphylococcus aureus , Haemophilus influenzae , Moraxella catarrhalis , Escherichia coli , Klebsiella pneumoniae , Bacteroides fragilis ^[2] . In order to overcome it, compounds that inactivate beta-lactamases were obtained.
The addition of beta-lactamase inhibitors ( clavulanic acid , sulbactam , tazobactam ) to ampicillin , amoxicillin , ticarcillin or piperacillin makes them active against many types of bacteria that form beta-lactamases ^[3] .

Beta-Lactamase Products

Beta-lactamase production is controlled by chromosomal or plasmid genes and their production can be induced by antibiotics or mediated by constitutional factors in the growth and distribution of bacterial resistance, with which plasmids carry genetic material. That is, plasmid-associated enzymes are among the main factors determining bacterial resistance.

Antibacterial activity

Significantly less known is the fact that beta-lactamase inhibitors have their own antibacterial activity. But it has been shown that clavulanic acid exhibits minimal, medium and high activity against several bacteria (see clavulanic acid ).

Beta-lactamase inhibitors
Clavulanic acid
Sulbactam
Tazobactam
Avibactam
Vaborbactam
Relebactam

Notes

↑ Antibiotic Resistance Archived January 16, 2012 on Wayback Machine , Beta-Lactamase Inhibitors
↑ Clavulanic acid: familiar and previously unknown properties , Abstract based on Finlay J. A review of the antimicrobial activity of clavulanate (Eng.) // Journal of Antimicrobial Chemotherapy. - 2003 .-- 12 June ( vol. 52 , no. 1 ). - P. 18-23 . - ISSN 1460-2091 . - DOI : 10.1093 / jac / dkg286 . - PMID 12775671 .
↑ Beta-lactamase inhibitors

Links

Clavulanic acid
Beta-lactam antibiotics
Beta-lactamases
Beta lactams
Amoxicillin / clavulanic acid

[1] Antibiotic Resistance Archived January 16, 2012 on Wayback Machine , Beta-Lactamase Inhibitors

[2] Clavulanic acid: familiar and previously unknown properties , Abstract based on Finlay J. A review of the antimicrobial activity of clavulanate (Eng.) // Journal of Antimicrobial Chemotherapy. - 2003 .-- 12 June ( vol. 52 , no. 1 ). - P. 18-23 . - ISSN 1460-2091 . - DOI : 10.1093 / jac / dkg286 . - PMID 12775671 .

[3] Beta-lactamase inhibitors