Optilom

Approved Indications:

• Uncomplicated Urinary Tract Infections (UTIs):
  For the treatment of acute and chronic uncomplicated UTIs caused by susceptible Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Enterobacter cloacae.
• Complicated UTIs and Prostatitis:
  Effective for complicated urinary tract infections and chronic bacterial prostatitis caused by susceptible organisms.
• Acute Bacterial Exacerbation of Chronic Bronchitis (ABECB):
  Indicated for mild to moderate infections due to susceptible respiratory pathogens.
• Prophylaxis in Urological Procedures:
  Used to prevent infections following transurethral urological procedures or instrumentation.

Off-label and Clinically Accepted Uses:

• Traveler’s Diarrhea (Bacterial):
  Occasionally used for empiric treatment in select cases when fluoroquinolones are appropriate, although not preferred due to safety concerns.

Route of Administration: Oral
Available Strength: 400 mg film-coated tablets
Administration: Can be taken with or without food. Avoid antacids, dairy, or mineral supplements within 2 hours before or after dosing.

Adults:

• Uncomplicated UTI:
  400 mg once daily for 3 days.
• Complicated UTI or Prostatitis:
  400 mg once daily for 10 to 14 days.
• ABECB:
  400 mg once daily for 10 days.
• Prophylaxis for Urological Procedures:
  400 mg once, 2 to 6 hours prior to the procedure.

Elderly:
• No routine dose adjustment solely based on age.
• Assess renal function before dosing.

Renal Impairment:

• CrCl 30–49 mL/min:
  400 mg loading dose, then 200 mg once daily.
• CrCl <30 mL/min or Hemodialysis:
  400 mg loading dose, then 200 mg every 48 hours.

Hepatic Impairment:
• No dose adjustment required.

Pediatric Use:
• Not recommended in children or adolescents under 18 years of age due to risk of musculoskeletal toxicity.

Lomefloxacin is a broad-spectrum fluoroquinolone antibiotic that inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV—enzymes critical for DNA replication, transcription, repair, and recombination. By interfering with these processes, it prevents bacterial cell division and leads to cell death. Its primary action is bactericidal, especially against aerobic Gram-negative bacteria.

• Absorption: Rapid and complete oral absorption (bioavailability ~95%).
• Time to Peak Concentration: 1 to 2 hours post-dose.
• Distribution: Extensively distributed in body tissues, particularly in the urinary tract, lungs, and prostate.
• Protein Binding: ~10%.
• Metabolism: Minimal hepatic metabolism.
• Half-life: Approximately 8 hours.
• Elimination: Primarily excreted unchanged via the kidneys (60–80% within 24 hours).
• Dialysis: Partially removed by hemodialysis.

• Pregnancy:
  • FDA Category C
  • Animal studies have shown adverse fetal effects; human studies are lacking.
  • Use only when benefits clearly outweigh risks, particularly in the second and third trimesters.
• Lactation:
  • Lomefloxacin is excreted into human breast milk.
  • Due to potential cartilage toxicity in infants, breastfeeding is not recommended during treatment and for at least 24 hours after the last dose.

• Primary Class: Antibacterial
• Subclass: Fluoroquinolone Antibiotic (Second-generation)

• Hypersensitivity to lomefloxacin or other fluoroquinolones
• History of tendon disorders related to fluoroquinolone use
• Patients with known QT interval prolongation or electrolyte abnormalities
• Children and adolescents under 18 years
• Pregnancy and breastfeeding (unless clearly needed)

• Tendinitis and Tendon Rupture:
  Increased risk, especially in elderly patients and those on corticosteroids. Discontinue at first sign of tendon pain.
• QT Prolongation:
  May increase risk of ventricular arrhythmias. Use with caution in patients with known QT prolongation or those taking QT-prolonging drugs.
• Photosensitivity:
  Severe sunburn-like reactions reported. Avoid direct sunlight and artificial UV exposure during and for 48 hours after therapy.
• CNS Effects:
  May cause seizures, confusion, tremors, hallucinations—especially in elderly or renally impaired patients.
• Peripheral Neuropathy:
  May be irreversible. Discontinue immediately if symptoms develop.
• Glycemic Disturbances:
  Hypoglycemia or hyperglycemia may occur, particularly in diabetic patients.
• Superinfection:
  Prolonged use may result in fungal or resistant bacterial infections including Clostridioides difficile-associated diarrhea.

Common Side Effects:

• Gastrointestinal: Nausea, diarrhea, abdominal pain
• Neurologic: Headache, dizziness, insomnia
• Skin: Rash, pruritus, photosensitivity
• General: Fatigue, metallic taste

Serious or Rare Side Effects:

• Tendon rupture (especially Achilles tendon)
• QT interval prolongation, torsades de pointes
• Seizures, hallucinations
• Stevens-Johnson Syndrome
• Anaphylactic reactions
• Peripheral neuropathy
• Severe C. difficile-associated diarrhea

• Antacids, Iron, Zinc, Sucralfate, Multivitamins:
  • Reduce absorption of lomefloxacin. Take at least 2 hours before or 4 hours after these agents.
• Drugs That Prolong QT Interval (e.g., amiodarone, macrolides):
  • May increase risk of life-threatening arrhythmias.
• NSAIDs:
  • May increase CNS stimulation and risk of seizures.
• Warfarin:
  • Enhanced anticoagulant effect possible; monitor INR closely.
• Probenecid:
  • May reduce renal clearance of lomefloxacin.
• CYP450:
  • Lomefloxacin is not a significant substrate or inhibitor of CYP enzymes.

• Fluoroquinolone Class Warnings (FDA, EMA):
  • Reinforced safety alerts regarding risks of tendinopathy, aortic aneurysm, and irreversible peripheral neuropathy.
  • Use limited to cases where no safer alternatives exist.
• Clinical Guidelines (Infectious Disease Societies):
  • Lomefloxacin is no longer recommended as a first-line therapy for most indications. Reserved for specific, resistant infections.

• Temperature: Store at 20°C to 25°C (68°F to 77°F)
• Permitted Range: 15°C to 30°C
• Humidity: Store in a dry environment; avoid excessive moisture
• Light Protection: Keep in the original container; protect from light
• Handling: Keep tightly closed; avoid contamination
• Reconstitution/Refrigeration: Not applicable for tablet formulations