Lee-flox (Levofloxacin): Uses, Formulations, and Safety Warnings

1. Disclaimer

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2. Summary

Lee-flox is a branded formulation of levofloxacin, a broad-spectrum fluoroquinolone antibacterial agent, available as oral tablets and 0.5% ophthalmic eye drops.

Oral levofloxacin is effective against a wide range of Gram-positive, Gram-negative, and atypical pathogens and is used in selected respiratory, urinary, skin, and prostate infections. However, due to serious and potentially irreversible adverse effects, systemic use is now restricted and reserved for situations where safer alternatives are unsuitable.

The ophthalmic formulation is used topically for bacterial conjunctivitis, with minimal systemic absorption.

3. Brand Name

Lee-flox® (also written as LEE-FLOX)

4. Category

• Antibacterial agent
• Fluoroquinolone (quinolone subclass)

5. Active Ingredient

Levofloxacin (the optically active L-isomer of ofloxacin)

6. Pharmaceutical Form & Strength

Oral (Systemic)

• Film-coated tablets: 250 mg, 500 mg, 750 mg

Ophthalmic

• Eye drops: 0.5% w/v (5 mg/mL), 5 mL bottle

7. Manufacturer & Marketing Authorization Holder

Pharaonia Pharmaceuticals New Borg El-Arab City, Alexandria, Arab Republic of Egypt

8. Mechanism of Action

Levofloxacin exerts concentration-dependent bactericidal activity by inhibiting:

• DNA gyrase (topoisomerase II)
• Topoisomerase IV

These enzymes are essential for bacterial DNA replication, transcription, repair, and recombination, leading to rapid bacterial cell death. Human topoisomerases are not affected at therapeutic concentrations.

9. Spectrum of Activity

Levofloxacin has in-vitro activity against susceptible strains of:

Gram-positive

• Streptococcus pneumoniae
• Streptococcus pyogenes
• Staphylococcus aureus (MSSA)
• Enterococcus faecalis

Gram-negative

• Haemophilus influenzae
• Haemophilus parainfluenzae
• Moraxella catarrhalis
• Escherichia coli
• Klebsiella pneumoniae
• Enterobacter cloacae
• Proteus mirabilis
• Pseudomonas aeruginosa

Atypical

• Chlamydia pneumoniae
• Mycoplasma pneumoniae
• Legionella pneumophila

Note: Resistance to fluoroquinolones is increasing globally; activity should be guided by local susceptibility data.

10. Pharmacokinetics

Oral Tablets

• Absorption: ~99% bioavailability; food has minimal clinical effect
• Distribution: Extensive tissue penetration (lungs, skin, prostate, urine)
• Protein binding: ~30–40%
• Metabolism: Minimal (<5%)
• Elimination: Primarily renal (≈87% unchanged)
• Half-life: ~6–8 hours (prolonged in renal impairment)

Eye Drops

• Systemic absorption: Negligible
• Ocular distribution: High local concentrations in conjunctiva and cornea

11. Indications

Systemic (Oral Tablets)

Reserved for use when alternative agents are inappropriate:

• Community-acquired pneumonia
• Nosocomial (hospital-acquired) pneumonia
• Complicated skin and skin-structure infections
• Complicated urinary tract infections, including pyelonephritis
• Chronic bacterial prostatitis

Ophthalmic

• Bacterial conjunctivitis caused by susceptible organisms

12. Administration

Tablets

• Once daily, with or without food
• Swallow whole with water
• Complete the full prescribed course

Eye Drops

• Instill into the conjunctival sac
• Avoid contact between dropper tip and eye or surfaces

13. Method of Preparation

• Tablets: No preparation required
• Eye drops: Ready to use

➡️ No additional preparation information of clinical relevance

14. Contraindications

• Hypersensitivity to levofloxacin or other fluoroquinolones
• History of fluoroquinolone-associated tendon disorders
• Myasthenia gravis
• Pregnancy and breastfeeding
• Children and adolescents (<18 years), except specific life-threatening indications

15. Warnings & Precautions

Boxed / Major Warnings (Systemic Use):

• Tendinitis and tendon rupture
• Peripheral neuropathy (may be irreversible)
• Central nervous system effects (seizures, psychosis, depression)
• Increased risk of aortic aneurysm and dissection
• QT interval prolongation
• Dysglycemia (hypo- or hyperglycemia)

Discontinue immediately at the first sign of tendon pain, neuropathy, or severe CNS effects.

16. Drug Interactions

• Antacids / iron / zinc / calcium: ↓ absorption (separate by ≥2 hours)
• NSAIDs: ↑ risk of CNS stimulation and seizures
• Warfarin: ↑ anticoagulant effect (monitor INR)
• Antidiabetic drugs: Risk of dysglycemia
• QT-prolonging drugs: Additive arrhythmia risk

17. Side Effects

Common

• Nausea, diarrhea
• Headache, dizziness
• Insomnia

Serious

• Tendon rupture
• Peripheral neuropathy
• CNS and psychiatric reactions
• Clostridioides difficile–associated diarrhea
• Cardiac arrhythmias

Ophthalmic

• Transient burning or stinging
• Mild blurred vision

18. Use in Special Populations

• Elderly: Increased risk of tendon injury and QT prolongation
• Renal impairment: Dose adjustment mandatory
• Hepatic impairment: No dose adjustment usually required
• Pregnancy/Lactation: Contraindicated
• Pediatrics: Systemic use generally contraindicated

19. Storage Conditions

• Store at 15–30°C
• Protect from light and moisture
• Keep out of reach of children
• Eye drops should be discarded after the recommended in-use period

20. Additional Sections

Antimicrobial Stewardship:

Systemic fluoroquinolones should be reserved for clearly indicated infections to minimize resistance development and serious adverse outcomes.

21. Frequently Asked Questions (FAQ)

Q: Can Lee-flox be used for viral infections? A: No. It is effective only against susceptible bacterial infections.

Q: Can dairy products be taken with tablets? A: Avoid taking large amounts simultaneously, as calcium may reduce absorption.

Q: Are eye drops associated with systemic side effects? A: Systemic effects are unlikely due to minimal absorption.

22. References

1. FDA Prescribing Information – Levofloxacin (Levaquin®)
2. European Medicines Agency (EMA) – Fluoroquinolone safety restrictions
3. StatPearls / NCBI: Levofloxacin Drug Monograph
4. British National Formulary (BNF)
5. Pharaonia Pharmaceuticals – Lee-flox product information