Parlox

Approved Indications:

• Community-Acquired Pneumonia (CAP): Mild to moderate severity caused by susceptible organisms including Streptococcus pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae, and Chlamydia pneumoniae.
• Acute Exacerbation of Chronic Bronchitis (AECB): Due to susceptible strains of H. influenzae, S. pneumoniae, and M. catarrhalis.

Clinically Accepted Off-label Uses (with caution):

• Uncomplicated urinary tract infections (UTIs): Caused by susceptible Gram-negative bacteria.
• Skin and soft tissue infections (SSTIs): Involving susceptible pathogens.
• Tuberculosis (adjunctive use): In multidrug regimens where first-line agents are not tolerated (not first choice).

Route of Administration: Oral

Adult Dose:

• Initial Dose: 400 mg orally on Day 1 (loading dose).
• Maintenance Dose: 200 mg orally once daily from Day 2 to Day 10.
• Duration: Typically 10 days depending on clinical response.

Pediatric Use:
Not recommended due to risk of arthropathy in developing cartilage.

Elderly:
No dosage adjustment required solely based on age. Monitor renal function.

Renal Impairment:

• Creatinine Clearance 21–50 mL/min: 400 mg Day 1, then 200 mg every 48 hours.
• Creatinine Clearance ≤20 mL/min or Hemodialysis: 400 mg Day 1, then 200 mg every 72 hours.

Hepatic Impairment:
No specific dose adjustment; use with caution in severe hepatic dysfunction.

Administration Instructions:

• Take with water, with or without food.
• Avoid concurrent intake of antacids or supplements containing magnesium, aluminum, calcium, or iron within 2–4 hours of dosing.

Sparfloxacin is a third-generation fluoroquinolone antibiotic that inhibits bacterial DNA replication. It specifically targets and inhibits two essential bacterial enzymes—DNA gyrase (topoisomerase II) and topoisomerase IV. These enzymes are critical for DNA supercoiling, repair, and separation during cell division. Inhibition leads to irreversible DNA damage, halting bacterial replication and resulting in bacterial cell death. Sparfloxacin exhibits concentration-dependent bactericidal activity, with enhanced efficacy against Gram-positive pathogens compared to earlier fluoroquinolones.

• Absorption: Rapid oral absorption; bioavailability ~92%.
• Peak Plasma Time: 3–5 hours after administration.
• Distribution: Widely distributed; high tissue penetration. Volume of distribution ~3.9–5.8 L/kg.
• Protein Binding: ~45%.
• Metabolism: Partially metabolized in the liver via oxidation.
• Elimination Half-life: Approximately 16–20 hours, allowing once-daily dosing.
• Excretion: 50% via urine (unchanged), ~20% via feces.

• Pregnancy: FDA Category C. Animal studies have shown adverse effects on the fetus; there are no adequate and well-controlled studies in pregnant women. Should be used during pregnancy only if the potential benefit justifies the risk.
• Lactation: Excreted in breast milk. Due to potential for serious adverse effects in nursing infants (e.g., cartilage toxicity), breastfeeding is not recommended during treatment.

• Primary Class: Antibacterial
• Subclass: Fluoroquinolone Antibiotic (Third Generation)

• Known hypersensitivity to sparfloxacin, other fluoroquinolones, or any formulation component.
• History of QT interval prolongation or concurrent use of QT-prolonging drugs.
• Patients with uncorrected hypokalemia or hypomagnesemia.
• Significant bradycardia or cardiac arrhythmias.
• Use in pediatric patients, pregnant or lactating women (due to safety concerns).

• QT Prolongation: Sparfloxacin has a higher risk of QT interval prolongation and torsades de pointes. Avoid in patients with cardiac arrhythmias or those taking QT-prolonging drugs.
• Photosensitivity: Increased risk of phototoxic reactions; avoid sunlight and use sunscreen during and for 5 days after therapy.
• Tendinitis and Tendon Rupture: Risk especially in elderly and those on corticosteroids.
• CNS Effects: May cause dizziness, confusion, hallucinations, or seizures—caution in patients with CNS disorders.
• Hepatotoxicity: Monitor liver enzymes in prolonged therapy.
• Clostridioides difficile-associated diarrhea (CDAD): May occur; consider in patients with persistent diarrhea.

Common Side Effects:

• Gastrointestinal: Nausea, diarrhea, abdominal pain
• Central Nervous System: Headache, dizziness, insomnia
• Dermatologic: Rash, photosensitivity reactions

Serious/Rare Side Effects:

• QT interval prolongation and torsades de pointes
• Tendon rupture (e.g., Achilles tendon)
• Hepatotoxicity (elevated liver enzymes, hepatitis)
• Peripheral neuropathy (rare, may be irreversible)
• Hypoglycemia or hyperglycemia
• Seizures or psychosis (especially in predisposed individuals)

Onset: Side effects may occur within the first few days of therapy; QT prolongation risk persists throughout treatment.

• QT-Prolonging Agents: Additive effects with antiarrhythmics (e.g., amiodarone), antipsychotics (e.g., haloperidol), and certain macrolides.
• Antacids, Sucralfate, Iron, Zinc, Calcium Supplements: Reduce absorption; separate dosing by 2–4 hours.
• NSAIDs: May increase CNS stimulation or seizure risk.
• Warfarin: May increase anticoagulant effect; monitor INR closely.
• CYP450 Enzymes: Limited interaction with CYP isoforms; however, monitor if used with drugs affecting QT.

• Market Status: Sparfloxacin has been withdrawn or restricted in several countries due to its high QT prolongation risk.
• Guideline Revisions: Not recommended as first-line therapy in current pneumonia or bronchitis guidelines due to safety concerns.
• Regulatory Notes: Safety warnings updated to emphasize phototoxicity and cardiac risks. FDA alerts advise considering alternatives when possible.

• Temperature: Store below 30°C (86°F).
• Humidity/Light: Protect from moisture and direct sunlight.
• Handling: Store in tightly closed containers. Avoid exposure to heat.
• Stability: No reconstitution required; oral tablets stable under standard conditions.