Beta lactamase inhibitors

What are beta lactamase inhibitors?

Beta-lactamase inhibitors are active ingredients that are used in combination with antibiotics to treat certain types of bacteria. Beta-lactamase inhibitors are drugs that target a defense mechanism of bacteria against conventional antibiotics such as penicillins and cephalosporins.

Bacterial types that defend themselves against penicillins and cephalosporins with a so-called beta-lactamase can also be treated with antibiotics. The beta-lactamase inhibitors prevent the bacteria from being able to inhibit the action of the antibiotics through their own enzyme called beta-lactamase.

Indications

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

If a bacterial infection is suspected, treatment of the disease with an antibiotic is often started. In addition, a so-called culture is created before antibiotic therapy. Material infected with the bacteria is collected, and the bacteria obtained from it are stimulated to grow. So you can determine the exact pathogen.
In addition, the bacterial colony obtained in this way can be tested for various antibiotics. A so-called antibiogram is obtained from this knowledge. This antibiogram describes which antibiotics are effective against the bacteria.

If the pathogens are resistant to normal penicillins and cephalosporins, they can be treated with a beta-lactamase inhibitor if necessary.
Typical infections for which this may be necessary are, for example, pneumonia or urinary tract infection.

In particular, people who have suffered from such infections several times and are being treated with antibiotics often get infections with resistant bacteria as a result. Therefore, they are often treated with antibiotics in combination with beta-lactamase inhibitors.

effect

Beta-lactamase inhibitors are active ingredients that work together with antibiotics against certain groups of bacteria. Many antibiotics contain what is known as a beta-lactam ring, a structure that is very important for the antibiotics to work against bacteria. These antibiotics are also called beta-lactam antibiotics. However, some types of bacteria have reacted to this beta-lactam ring in the antibiotic active ingredients and formed what is known as beta-lactamase. Beta-lactamase is an enzyme that can break down the beta-lactam ring in antibiotics.

This makes the bacteria that have a beta lactamase resistant to the antibiotics, so an infection can no longer be treated. In order to be able to treat these bacteria effectively, beta-lactamase inhibitors were developed. These can inhibit the enzyme beta-lactamase in the bacteria and thus ensure the effectiveness of the antibiotic again.

The following active ingredients are among the beta-lactamase inhibitors: Clavulanic acid, sulbactam and tazobactam are frequently used preparations, and avibactam is also one of the beta-lactamase inhibitors, but is less common. 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 ingredient piperacillin.

side effect

The side effects of beta-lactamase inhibitors are due to their antibacterial effects. Therefore, beta-lactamase inhibitors have the same side effects as the antibiotics they are co-administered with. In therapy with antibiotics and beta-lactam inhibitors, the bacteria that cause an infection are fought by the active ingredients. This is the desired effect.

However, not only the pathogenic bacteria are killed. The bacteria that naturally belong to the body, such as the bacteria in the digestive tract and on the skin, can also be affected by treatment with beta-lactamase inhibitors.

For this reason, treatments with beta-lactamase inhibitors and antibiotics often cause side effects in the digestive tract. This often leads to symptoms such as diarrhea and abdominal pain. Nausea and vomiting can also occur as side effects. The destruction of the natural intestinal flora also helps other bacteria that are resistant to the antibiotics and beta-lactamase inhibitors to spread in the digestive tract.

The side effects are noticeable on the skin in that instead of the natural bacterial skin flora, other germs such as fungi can now spread on the skin. Especially people with a weakened immune system cannot defend themselves adequately against these fungi and therefore suffer more frequently from fungal infections after therapy with beta-lactamase inhibitors and antibiotics.

• For more information on the side effects of the antibiotics given in combination, read our article: Side effects of antibiotics

interaction

Interactions of beta-lactamase inhibitors mainly take place in the metabolic process. The beta-lactamase inhibitors are mainly metabolized in the liver. They are also partly excreted via the liver and partly via the kidneys. All drugs that require the same metabolic enzymes in the liver can interact with the beta-lactamase inhibitors.

Since there are various beta-lactamase inhibitors, you can switch from one of the active ingredients to another if there is a risk of interactions.
Which beta-lactamase inhibitor interacts with which other drug cannot be answered across the board and can be better read on the basis of the specific question in the package insert or specialist information.

When should beta-lactamase inhibitors not be given?

Beta-lactamase inhibitors, like all medications, must not be given if the person to be treated with the active ingredient is allergic to one of the ingredients.
In addition, when treating with beta-lactamase inhibitors, it must always be ensured that the bacteria to be treated can actually be treated by the beta-lactamase inhibitors. Otherwise there will be unnecessary antibiotic therapy that is not effective and also promotes the development of resistance.

There are further contraindications in the case of severe liver or kidney dysfunction.
In this case, the dosage of the beta-lactamase inhibitors must be adapted to the restricted organ function; therapy with beta-lactamase inhibitors may also not be possible and more aggressive antibiotics must be used.

dosage

The dosage of beta-lactamase inhibitors depends on various factors. In children, for example, the dosage should be adapted to their body weight.
For adults there are standard dosages, which depend on which antibiotic the beta-lactamase inhibitors are combined with.

Clavulanic acid is often used in combination with amoxicillin at a dosage of 125 mg. Both 500 mg of amoxicillin and 875 mg of amoxicillin can be combined with 125 mg of clavulanic acid.
How many of the tablets with this combination of active ingredients should be taken daily also depends on the severity of the disease, the underlying bacterial species and the affected organ.

Tazobactam, on the other hand, is used in combination with piperacillin, for example in doses of 0.25 g (= 250 mg) or 0.5 g (= 500 mg).
In general, the dose of beta-lactamase inhibitors must be adjusted if people who are to be treated with beta-lactamase inhibitors suffer from impaired liver or kidney function. In this case, the excretion of the substances is slowed down, so the dosage should be reduced.

price

The price of beta-lactamase inhibitors is difficult to determine. The beta-lactamase inhibitors are usually offered in combination preparations with antibiotics.
The price of the combination of active ingredients depends on the dosage and the amount of tablets contained in a pack. Liquid solutions of the active ingredient combination, for example for intravenous therapy (therapy with the antibiotic and the beta-lactamase inhibitor directly via the vein) are also offered.

For the person being treated with the active ingredient, the price in the pharmacy is usually an additional payment of 5 €. Therapy with antibiotics may only be carried out if there is a medical indication. As soon as this is available, the cost of the medication will be covered by the health insurance company.

Beta lactamase inhibitors and alcohol - are they compatible?

In general, antibiotic therapy does not go well with alcohol. The same applies to treatment with antibiotics in combination with beta-lactamase inhibitors. The reason for the particularly poor tolerance is that both the active ingredients and the alcohol have to be metabolized and broken down in the liver.

This leads to competition between the substances in the liver when taking beta-lactamase inhibitors and consuming alcohol at the same time. This leads to a slower breakdown of both the alcohol and the beta-lactamase inhibitor. Both substances therefore remain in the body longer.

Alternatives to the beta-lactamase inhibitors

Alternatives to beta-lactamase inhibitors are usually other antibiotics. Often it is not possible to switch between different beta-lactamase inhibitors, as bacteria that are resistant to one beta-lactamase inhibitor usually cannot be treated by the others either.

However, antibiotics with no beta-lactam rings in their structure are often suitable for treating these infections. For example, antibiotics from the group of fluoroquinolones can be used.
But antibiotics such as carbapenems often get by without a beta-lactamase inhibitor despite their beta-lactam ring.

Can it be taken during pregnancy and breastfeeding?

As with many medications, taking beta-lactamase inhibitors during pregnancy and breastfeeding is not always safe. For the combination Unacid (ampicillin and sulbactam), for example, there is so far no evidence that taking it during pregnancy harms the child, but there are no large studies that can confirm this tendency. There is also insufficient data for Unacid for breastfeeding.

The same applies to the intake of clavulanic acid during pregnancy and breastfeeding. The effects on the unborn or breast-fed child in particular have not yet been adequately researched.

In contrast, with tazobactam in combination with piperacillin, it is known that the active ingredient can be passed on to the child via the placenta (placenta) during pregnancy as well as via breast milk during breastfeeding. How large the amounts are and whether they harm the child is also not known.

In general, treatment with beta-lactam inhibitors during pregnancy should be carefully considered and advice from a responsible doctor or pharmacist should be given.

Effectiveness of the pill when taking beta-lactam inhibitors

The effectiveness of the pill may be limited when treated with beta-lactamase inhibitors.

This is due to the fact that the active substances sometimes go through similar metabolic processes in the body and thus influence each other if they are to be found in the body at the same time.
For this reason, the effectiveness of the pill cannot be guaranteed when taking beta-lactamase inhibitors at the same time.

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Exclusion of liability / disclaimer

We would like to point out that medication must never be discontinued, applied or changed independently without consulting your doctor.
Please note that we cannot claim that our texts are complete or correct. The information may be out of date due to current developments.