- Lomefloxacin is a third-generation fluoroquinolone antibiotic with a molecular formula of C17H19F2N3O3 and a molecular mass of 351.35 g/mol. Its structure features a fluorine atom at the 6-position and a methylpiperazine ring at the 7-position, which enhance its antibacterial activity and spectrum of coverage. Additionally, it has a unique 8-methoxy group, which improves its activity against anaerobic bacteria and reduces the risk of phototoxicity compared to earlier fluoroquinolones. These structural modifications classify it as a member of the fluoroquinolone family.
- The antibiotic exerts its bactericidal action by inhibiting bacterial DNA synthesis. It specifically targets bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, enzymes essential for DNA replication, transcription, and repair. By binding to these enzymes, lomefloxacin induces double-stranded DNA breaks, leading to rapid bacterial cell death. This mechanism is particularly effective against actively dividing bacteria.
- Lomefloxacin demonstrates broad-spectrum activity against a wide range of gram-negative and gram-positive bacteria, with particularly potent activity against Enterobacteriaceae (e.g., Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis), Pseudomonas aeruginosa, and Haemophilus influenzae. It is also effective against some atypical pathogens, such as Legionella pneumophila and Mycoplasma pneumoniae. However, its activity against gram-positive organisms, such as Streptococcus pneumoniae, is generally less robust compared to newer fluoroquinolones.
- The pharmacokinetic profile of lomefloxacin includes excellent oral bioavailability (approximately 95-98%), rapid absorption, and widespread tissue distribution. It achieves high concentrations in the kidneys, prostate, lungs, and urinary tract, making it particularly effective for treating urinary tract infections, respiratory infections, and prostatitis. Lomefloxacin undergoes minimal hepatic metabolism and is excreted primarily unchanged in the urine, with a half-life of 6 to 8 hours, allowing for once-daily dosing.
- Despite its efficacy, lomefloxacin is associated with potential adverse effects, including gastrointestinal disturbances (e.g., nausea, diarrhea), central nervous system effects (e.g., headache, dizziness), and, rarely, phototoxicity or tendonitis. Its use is also limited by increasing bacterial resistance, particularly among gram-negative organisms.
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