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Pharmacological particulars
Pharmacotherapeutic group: Quinolone and quinoxaline antibacterials, fluoroquinolones
ATCvet code: QJ01MA90
Pharmacodynamic properties
Enrofloxacin is a synthetic, broad spectrum antimicrobial, bactericidal in action and effective against a wide range of gram-positive and gram-negative bacteria as well as mycoplasmas. It inhibits the enzyme DNA-gyrase in the cell nuclei during replication of bacterial DNA. It also acts on bacterial cells during stationary phase by changing the permeability in the phospholipid cellular membranes.
Antibacterial spectrum: Enrofloxacin is active against many gram-negative bacteria, against gram-positive bacteria and Mycoplasma spp. In vitro susceptibility has been shown in strains of (i) gram-negative species such as Pasteurella multocida and Avibacterium (Haemophilus) paragallinarum and (ii) Mycoplasma gallisepticum and Mycoplasma synoviae. (See Special precautions for use in animals)
Types and mechanisms of resistance: Resistance to fluoroquinolones has been reported to arise from five sources, (i) point mutations in the genes encoding for DNA gyrase and/or topoisomerase IV leading to alterations of the respective enzyme, (ii) alterations of drug permeability in gram-negative bacteria, (iii) efflux mechanisms, (iv) plasmid mediated resistance and (v) gyrase protecting proteins. All mechanisms lead to a reduced susceptibility of the bacteria to fluoroquinolones. Cross-resistance within the fluoroquinolone class of antimicrobials is common.
Pharmacokinetic properties
The pharmacokinetics of enrofloxacin are such that both oral and parenteral administration lead to similar serum levels. Enrofloxacin possesses a high distribution volume. Tissue levels 2-3 times higher than that found in the serum have been demonstrated in laboratory animals and target species. Organs in which high levels can be expected are the lungs, liver, kidney, bone and lymphatic system.
Enrofloxacin also distributes into the cerebrospinal fluid, the aqueous humour.