Betalactamase inhibitors

What are betalactamase inhibitors?

Betalactamase inhibitors are active ingredients used in combination with antibiotics to treat certain types of bacteria. Betalactamase inhibitors are drugs that are directed against a defence mechanism of bacteria against the traditional antibiotics such as penicillins and cephalosporins. Thus, antibiotic therapy can also be used to treat bacterial species that defend themselves against penicillins and cephalosporins with a so-called betalactamase. The betalactamase inhibitors prevent the bacteria from inhibiting the effect of the antibiotics through their bacteria’s own enzyme called betalactamase.

Indications

For the indication of a therapy with betalactamase inhibitors, a bacterial infection must first be present. Betalactamase inhibitors are given in combination with antibiotics such as penicillins and cephalosporins. The combination of antibiotic and betalactamase inhibitor can also be used to treat partially resistant bacterial infections with antibiotics.

Frequently, if a bacterial infection is suspected, treatment of the disease with an antibiotic is started. In addition, a so-called culture is made before antibiotic therapy. In this culture, material infected with the bacteria is collected and the bacteria obtained from it are then stimulated to grow.

In this way the exact pathogen can be determined. In addition, the bacterial colony thus obtained can be tested for various antibiotics. From this knowledge, a so-called antibiogram is obtained.

This antibiogram describes which antibiotics are effective against the bacteria. If the bacteria are pathogens that are resistant to normal penicillins and cephalosporins, they can also be treated with a beta-lactamase inhibitor. Typical infections where this may be necessary are, for example, pneumonia or urinary tract infections. Particularly people who have already had several cases of such infections and are treated with antibiotics often develop infections with resistant bacteria. Therefore, they are often treated with antibiotics in combination with beta-lactamase inhibitors.

Effect

Betalactamase inhibitors are active ingredients that act together with antibiotics against certain groups of bacteria. Many antibiotics contain a so-called betalactam ring, a structure that is very important for the antibiotics’ ability to fight bacteria. These antibiotics are also called beta-lactam antibiotics.

However, some types of bacteria have reacted to this beta-lactam ring in the antibiotic agents and formed a substance called beta-lactamase. Betalactamase is an enzyme that can split the betalactam ring in antibiotics. As a result, the bacteria that possess beta-lactamase become resistant to the antibiotics and an infection can no longer be treated.

To be able to treat these bacteria effectively, beta-lactamase inhibitors have been developed. These can inhibit the enzyme betalactamase of the bacteria and thus ensure the effectiveness of the antibiotic again. The following active ingredients are among the betalactamase inhibitors: clavulanic acid, sulbactam and tazobactam are frequently used preparations, avibactam is also among the betalactamase inhibitors, but is less commonly used. Clavulanic acid is usually used together with the antibiotic amoxicillin (amoxiclav), sulbactam is used in combination with ampicillin. Tazobactam is typically administered together with the active substance piperacillin.