The drug tazobactam is a beta-lactamase inhibitor and supports and enhances the antibacterial effect of the beta-lactam antibiotic piperacillin without being antibiotically active itself. Tazobactam irreversibly binds to the enzyme beta-lactamase, which is produced by some pathogenic bacteria and can inactivate beta-lactamase antibiotics. Because of its binding properties, tazobactam is used exclusively in combination with piperacillin.
What is tazobactam?
The drug substance tazobactam supports and enhances the antibacterial effect of the beta-lactam antibiotic piperacillin without being antibiotically active itself. Tazobactam is a drug classified as a beta-lactamase inhibitor or inhibitor. The active ingredient has a similar structure to beta-lactam antibiotics without being antibiotically active itself. Like other beta-lactamase inhibitors, tazobactam has the typical beta-lactam ring. It is a heterocyclic 4-membered ring containing 3 carbon atoms and one nitrogen atom. Drug-effective is the water-soluble sodium salt of tazobactam with the chemical molecular formula C10H11N4NaO5S. The physiological effect of tazobactam is its ability to bind to the enzyme beta-lactamase, which is secreted by some pathogenic bacteria. The enzyme leads to cleavage of the beta-lactam ring in beta-lactam antibiotics, which include penicillins. This cancels the antibiotic effect of the specific antibiotics. To prevent the cancellation of the antibiotic effect, beta-lactamase inhibitors are combined with beta-lactam antibiotics. The inhibitors bind to beta-lactamase and thus abolish the physiological effect against lactam antibiotics. Tazobactam is administered exclusively in combination with the beta-lactam antibiotic piperacillin. Because the combination drug is not absorbed in the digestive tract (it is not acid stable), only parenteral administration can be considered for the drug, i.e., intravenously by infusion solution or intramuscularly by injection.
Pharmacologic action
The isolated pharmacologic effect of tazobactam on the body and organs is not known because the drug is used exclusively in combination with piperacillin. The main active ingredient of piperacillin, as in other antibiotics from the penicillin group, is an acylaminopenicillin. The active ingredient inhibits the construction of their cell walls in various types of bacteria, so that they are no longer able to divide and are killed. Due to the less specific action of acylaminopenicillins, a good broad-spectrum effect is produced against many different pathogenic bacterial species, but vital and useful bacteria are also affected. Side effects may develop as a result, which may require discontinuation of treatment. Mainly white blood cells (leukocytes) may be affected, platelets (thrombocytes), veins and kidneys. In addition, there may be changes in electrolyte balance. For example, decreased potassium levels may develop, which can lead to heart rhythm problems, among other things.
Medical use and application
Drugs composed of a combination of tazobactam and piperacillin are classified as broad-spectrum antibiotics or broad-spectrum penicillins. The parenterally administered combination preparations are effective against a wide range of different Gram-positive and Gram-negative germs. Piperacillin in combination with tazobactam is also effective against anaerobic bacteria such as Haemophilus and others. In some cases, the combination of the two active ingredients can also successfully combat multi-resistant germs. Because of their broad and, in some cases, specific antibacterial properties, combination preparations such as Pipitaz, Tazobac, Tazonam, and others are used primarily against severe internal abdominal infections, infections of the urogenital tract, and biliary tract infections. Tazobactam and piperacillin play an equally important role in the use against the opportunistic pathogen Pseudomonas. Pseudomonas are rod-shaped, flagellated, gram-negative germs that are ubiquitous and prove pathogenic only in the case of a weakened immune system or an immune system artificially suppressed with drugs.However, they are difficult to combat because they have often developed multiresistance to the most common antibiotics. Severe general and mixed infections are also part of the preferred treatment spectrum of tazobactam, which is combined with piperacillin. In certain cases of severe sepsis caused by bacterial pathogens, treatment with tazobactam and piperacillin can be goal-directed and life-saving. Preventive treatment to prevent infection is not advisable because potential harmful side effects may outweigh long-term treatment, which could breed further resistance in the germs.
Risks and side effects
Before parenteral administration of tazobactam, ensure that there is no known allergy to penicillins, cephalosporins, or to other beta-lactamase inhibitors. The use of the drug should also be carefully weighed in terms of benefit and potential hazard in the presence of known liver or kidney disease and low blood potassium levels. It is equally important to inform the attending physician about the possible use of coagulation inhibitors such as aspirin, Marcumar or one of the modern “blood thinners”, for example apixabam, as the effects of these drugs may be weakened or intensified. Taking other medications at the same time can also alter the effect of tazobactam. In the course of an interaction, for example, taking the gout medication probenecid prolongs the residence time of the combination preparation in the body, so that a dose reduction is advisable. Other risks and harmful side effects are comparable to those that must be considered when treating with penicillin. Specifically, transient digestive disturbances, skin rashes (exanthema), a decrease in neutrophil granulocytes (neutropenia), and an increase in liver enzyme levels and a decrease in potassium concentrations may occur. In very rare cases, phlebitis and cardiovascular problems have also been observed.
