Ofloxacin

Ofloxacin is a broad-spectrum fluoroquinolone antibiotic used to treat infections caused by susceptible bacteria. Approved indications include:

• Urinary tract infections (UTIs): Including acute and chronic pyelonephritis, cystitis, and complicated UTIs.
• Respiratory tract infections: Such as community-acquired pneumonia, acute exacerbations of chronic bronchitis, and sinusitis.
• Skin and soft tissue infections: Including cellulitis and wound infections.
• Sexually transmitted infections: Such as uncomplicated gonorrhea and nongonococcal urethritis/cervicitis.
• Prostatitis: Acute and chronic bacterial prostatitis.
• Bone and joint infections: Osteomyelitis and septic arthritis caused by susceptible organisms.
• Infectious diarrhea: Caused by susceptible bacteria.
• Intra-abdominal infections: Such as peritonitis and intra-abdominal abscess when used with metronidazole.
• Otitis externa and otitis media: Topical formulations used in infections caused by susceptible organisms.

Off-label (clinically accepted) uses:

• Multidrug-resistant tuberculosis adjunct therapy (in selected cases).
• Prevention and treatment of infections in neutropenic patients.
• Other infections caused by susceptible organisms where alternative therapies are unsuitable.

• Route: Oral and intravenous formulations available; topical formulations for ear and eye infections.

Oral and IV dosing (adults):

• Uncomplicated UTIs: 200 mg every 12 hours for 7 days.
• Complicated UTIs and pyelonephritis: 400 mg every 12 hours for 10–14 days.
• Respiratory tract infections: 400 mg every 12 hours for 7–14 days.
• Prostatitis: 200–400 mg every 12 hours for 28 days.
• Skin and soft tissue infections: 400 mg every 12 hours for 7–14 days.
• Gonorrhea: Single 400 mg dose orally.
• Infectious diarrhea: 200 mg every 12 hours for 5 days.
• Bone and joint infections: 400 mg every 12 hours for 4–6 weeks or more.

Pediatrics:

• Use is generally not recommended except in serious infections; dosing based on body weight (typically 10 mg/kg every 12 hours), under specialist supervision.

Elderly:

• No routine dose adjustment required; monitor renal function.

Renal impairment:

• Adjust dose based on creatinine clearance (CrCl):
• CrCl 20–50 mL/min: 200 mg every 12 hours or 400 mg every 24 hours.
• CrCl <20 mL/min: 200 mg every 24 hours or extend dosing interval.

Hepatic impairment:

• No dose adjustment necessary.

Topical formulations:

• Administer as per specific product instructions (e.g., ear drops: 3–4 drops 2–3 times daily).

Duration: Varies by infection type and severity; follow clinical response and guidelines.

Ofloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, enzymes essential for bacterial DNA replication, transcription, repair, and recombination. By preventing the supercoiling and relaxation of bacterial DNA, ofloxacin disrupts bacterial cell division and leads to bacterial cell death. This action is bactericidal and effective against a wide range of Gram-positive and Gram-negative bacteria.

• Absorption: Rapid and almost complete oral absorption with bioavailability of approximately 98%.
• Distribution: Widely distributed in body tissues and fluids, including lungs, prostate, skin, and urine; crosses the blood-brain barrier in small amounts.
• Metabolism: Minimally metabolized in the liver; mostly excreted unchanged.
• Elimination: Primarily renal; about 65–80% excreted unchanged in urine via glomerular filtration and tubular secretion.
• Half-life: Approximately 4–5 hours in healthy adults; may be prolonged in renal impairment.
• Onset of action: Rapid absorption; peak plasma concentration achieved within 1–2 hours after oral administration.

• Pregnancy: Classified as FDA Pregnancy Category C. Animal studies have shown adverse effects on cartilage development; human data are limited. Use only if potential benefits justify potential risks.
• Lactation: Ofloxacin is excreted in breast milk in small amounts. Caution is advised when administering to breastfeeding women; monitor infants for adverse effects.

• Primary class: Fluoroquinolone antibiotic.
• Subclass: Second-generation fluoroquinolone.

• Known hypersensitivity to ofloxacin, other fluoroquinolones, or any formulation excipients.
• History of tendon disorders related to fluoroquinolone use.
• Concurrent use with tizanidine (due to significant interaction).

• Risk of tendinitis and tendon rupture, especially in elderly patients and those on corticosteroids.
• May cause QT interval prolongation; caution in patients with cardiac arrhythmias or electrolyte abnormalities.
• Avoid use in patients with epilepsy or CNS disorders unless benefit outweighs risk.
• Use with caution in renal impairment; adjust dose accordingly.
• Possible photosensitivity reactions; avoid excessive sunlight or UV exposure during therapy.
• May cause peripheral neuropathy; discontinue if symptoms occur.
• Not recommended for use in children unless no alternatives are available due to potential effects on cartilage development.
• Monitor for signs of hypersensitivity reactions, including anaphylaxis.

• Common:
• Gastrointestinal: nausea, vomiting, diarrhea, abdominal pain.
• Central nervous system: headache, dizziness, insomnia.
• Skin: rash, pruritus.
• Serious/Rare:
• Tendon rupture or tendinitis.
• QT prolongation and cardiac arrhythmias.
• Peripheral neuropathy.
• Hypersensitivity reactions including Stevens-Johnson syndrome.
• Hepatotoxicity (rare).
• Onset: Usually within days of starting therapy; some adverse effects may occur after prolonged use.

• Major interactions:
• Antacids, sucralfate, iron salts, and multivitamins reduce oral absorption; administer ofloxacin at least 2 hours before or 4–6 hours after these agents.
• Probenecid and NSAIDs may increase risk of CNS toxicity.
• Concurrent use with corticosteroids increases risk of tendon rupture.
• Tizanidine co-administration contraindicated (marked hypotension and sedation).
• Drugs that prolong QT interval may have additive effects (e.g., amiodarone, quinidine).
• Metabolism: Minimal CYP450 involvement; interaction potential low.

• Fluoroquinolones including ofloxacin are recommended with caution due to increasing resistance and safety concerns.
• Regulatory agencies recommend restricting use to infections where alternatives are not suitable.
• Updated warnings highlight risks of tendinopathy, neuropathy, and CNS effects.
• No recent major changes in dosing guidelines, but emphasis on risk-benefit assessment before prescribing.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from light and moisture.
• Keep container tightly closed.
• Do not freeze.
• Keep out of reach of children.