- Ofloxacin is a second-generation fluoroquinolone antibiotic used to treat bacterial infections by inhibiting DNA replication.
- It has broad-spectrum activity against both Gram-positive and Gram-negative bacteria and is commonly used for respiratory, urinary tract, and skin infections.
- Due to its strong bactericidal effects and good oral bioavailability, ofloxacin remains an important option in antimicrobial therapy.
- Ofloxacin consists of a quinolone core structure with a fluorine atom at the C-6 position, enhancing bacterial penetration and enzyme inhibition.
- Unlike some fluoroquinolones, ofloxacin is a racemic mixture, containing both levo- and dextro-isomers. The levo-isomer, known as levofloxacin, exhibits greater antibacterial activity, leading to its development as a separate drug with enhanced efficacy.
- Ofloxacin is available in multiple formulations, including oral tablets, intravenous solutions, and ophthalmic preparations, making it versatile for treating different types of bacterial infections.
- Ofloxacin inhibits bacterial DNA gyrase and topoisomerase IV, enzymes critical for DNA supercoiling, replication, and segregation. By stabilizing the DNA-enzyme complex after cleavage, it prevents the re-ligation of DNA strands, leading to lethal double-strand breaks and bacterial cell death.
- This bactericidal mechanism makes ofloxacin highly effective against actively dividing bacteria such as Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, and Pseudomonas aeruginosa.
- Ofloxacin is prescribed for various bacterial infections, including:
- Respiratory tract infections – such as pneumonia and bronchitis exacerbations.
- Urinary tract infections – including pyelonephritis and cystitis.
- Skin and soft tissue infections – used for cellulitis and wound infections.
- Prostatitis – effective in bacterial prostate infections.
- Bacterial conjunctivitis – available as ophthalmic drops.
- Despite its effectiveness, ofloxacin is associated with potential side effects such as QT interval prolongation, tendon rupture, and neurological disturbances. Due to safety concerns, its use is often restricted to cases where alternative antibiotics are unsuitable or ineffective.
- Resistance to ofloxacin has emerged due to mutations in bacterial DNA gyrase/topoisomerase IV genes and efflux pump mechanisms. Overuse of fluoroquinolones has contributed to rising resistance rates, prompting stricter regulations on their use.
- To combat resistance, researchers continue to explore modified fluoroquinolone derivatives with enhanced bacterial targeting and reduced resistance potential. As antimicrobial resistance remains a global challenge, ofloxacin still plays a role in bacterial infection management, though it is prescribed carefully.
