- Feb 13, 2018 -
Chloramphenicol is very widely used in livestock and poultry farms before florfenicol is developed. Because chloramphenicol has a unique antibacterial mechanism and advantages compared to penicillins, sulfonamides, aminoglycosides and other drugs. What’s more, chloramphenicol is not easy to cross-resistance with other types of antibiotics, and the effectiveness of clinical treatment has been relatively high. Moreover, the unique mechanism of action of chloramphenicol also makes it very difficult for it to produce resistance; in particular, it is drug resistance, which is also intermittent; that is, after a period of withdrawal, the sensitivity will be restored.
This is directly related to the unique role of chloramphenicol in binding to peptidyl transferases for inhibiting the binding of the enzyme to its substrate amino acids and blocking the formation of peptide bonds.
However, the chloramphenicol antibacterial activity inhibits the activity of peptidyl transferases on the 50s ribosomal subunit of bacteria when the bacterial protein is inhibited. The synthesis of the mitochondrial bone marrow ribosome (both 70s), which is very similar to the bacterial ribosomal structure, is also affected.
Therefore, prolonged administration of chloramphenicol to animals causes a dose-related side effect of myelosuppression and is most particularly susceptible to cats. This chloramphenicol-specific response to aplastic anemia, mainly para-nitro in chloramphenicol molecules.
The development of florfenicol, a new drug, is based on the group optimization of para-nitro in the side effects of chloramphenicol: the para-nitro group that causes chloramphenicol side effects is replaced by a sulfonic acid group that has no side effects
This is the advantage of florfenicol's usage in food animals (without para-nitro group in the molecule) and does not induce aplastic anemia in humans and animals.
Therefore, florfenicol residues in the food animal body will not cause great harm to the public health and safety of animals and people. So far, there have been no reports of routine doses of florfenicol applied to food animals, causing these adverse effects.
In the first three carbon atoms florfenicol molecules are more than a chloramphenicol fluorine atoms. This fluorine atom reduces the number of sites where bacteria acetylate chloramphenicol, thiamphenicol and other chloramphenicol drugs, thereby enhancing the "acetylation" of the drug against bacterial resistance.
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