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Article about Zyvox
Linezolid is an antibiotic in the class of the active substances oxazolidinones. The drug is used as a reserve antibiotic.
What is Zyvox?
Linezolid is currently the only active antibiotic for MRSA available both orally and intravenously.
Zyvox belongs to the brand new group of oxazolidinones. Oxazolidinones have saturated heterocyclic compounds. They inhibit the biosynthesis of proteins in bacteria. Unlike other antibiotics such as tetracyclines, macrolides and lincosamides, they already inhibit the start of synthesis.
Linezolid is an antibiotic primarily used for infections with vancomycin-resistant pathogens. Zyvox is particularly effective for infections with gram-positive bacteria. It is currently the only antibiotic active against MRSA available both orally and intravenously. MRSA refers to strains of the Staphylococcus aureus bacteria that are resistant to all β-lactam antibiotics, such as penicillin. Typically, these pathogens are multi-resistant and also have resistance to antibiotics such as quinolones, tetracyclines, erythromycin, sulfonamide and vancomycin.
Linezolid is approved for the treatment of nosocomial pneumonia and serious skin and soft tissue infections.
Pharmacological effects
The Zyvox antibiotic inhibits the protein synthesis of bacteria. In protein biosynthesis, living things produce proteins by translation. Protein biosynthesis is essential for the new formation of proteins in cells. No gene expression is possible without the production of proteins. It also means that cells cannot proliferate without protein biosynthesis. You can't grow anymore.
Linezolid inhibits the biosynthesis of bacteria proteins from the start. For this, the drug binds to the 50S subunits of the ribosomes. Protein biosynthesis takes place in ribosomes. Zyvox, however, prevents protein synthesis by forming a so-called initiation complex.
However, only Gram positive pathogens are affected by this bacteriostatic effect. Gram-negative pathogens are resistant to linezolid.
Medical application and use
Zyvox, based on gram-positive bacteria, became an important reserve antibiotic soon after its development. Reserve antibiotics can only be administered with restrictions. There are strict indications. One of the reasons for this limitation is the serious side effects of the agents. In addition, additional resistance should be avoided through the targeted use of reserve antibiotics.
Usually vancomycin is the standard MRSA antibiotic. However, there are now more and more germs that are also resistant to vancomycin. Linezolid is used in these cases. It is particularly important in the treatment of severe MRSA infections in hospitals and in the treatment of multidrug-resistant tuberculosis. Staphylococci, including methicillin resistant strains (MRSA), enterococci, including vancomycin resistant strains (VRE) and streptococci, including penicillin resistant strains, are sensitive to Zyvox.
The drug is approved for the treatment of nosocomial or community-acquired pneumonia. Linezolid is also used for serious infections of the skin or soft tissue. Before treatment, however, a microbiological test should be performed to determine if the infection was caused by gram-positive bacteria sensitive to Zyvox.
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Risks and side effects
A serious side effect of linezolid is the suppression of bone marrow. Since blood formation takes place in the bone marrow, there are changes in the blood count. With pancytopenia, all the blood cells in the blood are greatly reduced, which simultaneously leads to anemia, leukopenia and thrombocytopenia. However, neutropenia and thrombocytopenia can also occur in solitary conditions. In neutropenia, neutrophilic granulocytes are reduced. As the immune system is directly affected, serious bacterial infections with fever and chills can develop. Affected people feel very sick and suffer from mucous membrane necrosis in the area of the mouth, throat, throat and genitals. Blood clotting is impaired in thrombocytopenia. Patients develop hematomas more quickly or have increased bleeding from the nose and / or gums.
Another side effect of Linezelid is high blood pressure (hypertension). In addition, monoamine oxidase-A and monoamine oxidase-B can be inhibited. This can have a negative impact on the nervous system. Patients also report headache and gastrointestinal irritation while taking Zyvox.
Linezolid should not be used in cases of known intolerance. Pregnancy and breastfeeding are also contraindications due to the serious side effects. Zyvox should also not be used while taking MAOIs. MAOIs are drugs from the group of antidepressants. They are prescribed, among other things, for Parkinson's disease and depression.
It should also be noted that linezolid also affects serotonin levels in the central nervous system (CNS) by inhibiting monoamine oxidase. If the drug is taken with other drugs that increase serotonin levels in the blood, a life-threatening serotonin syndrome may develop. Neuromotor and cognitive symptoms are characteristic of the disorder caused by an accumulation of the neurotransmitter serotonin. Affected people suffer from restlessness, involuntary muscle contractions, chills, tremors, sweating, and increased willingness to think.
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