Sparfloxacin is indicated for the treatment of adults 18 years of age and older with infections caused by susceptible microorganisms.Respiratory tract infections:

• Community-acquired pneumonia (CAP) caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae
• Acute bacterial exacerbation of chronic bronchitis (ABECB) caused by Chlamydia pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Staphylococcus aureus, or Streptococcus pneumoniae

Sparfloxacin is also indicated for the treatment of the following conditions:

• Chronic obstructive pulmonary disease (COPD)
• Acute maxillary sinusitis (AMS)
• Urinary tract infections, including gonococcal and nongonococcal urethritis, chancroid, and other sexually transmitted diseases
• Bacterial prostatitis
• Bacterial diarrhoea
• Osteomyelitis
• Other uses: Sparfloxacin may also be used in the treatment of tuberculosis in combination with rifampicin and isoniazid, and in the treatment of leprosy in combination with standard therapeutic agents.

Sparfloxacin is a broad-spectrum antibacterial agent that acts by inhibiting DNA gyrase and topoisomerase IV. It is active against many bacteria that infect the respiratory tract and lungs, and clinical studies have shown it to be effective in the treatment of various bacterial infections. In vitro, sparfloxacin has demonstrated greater activity than some other fluoroquinolones against certain Gram-positive organisms, including Streptococcus pneumoniae and Staphylococcus aureus, as well as against Mycobacteria and *Chlamydia species.

Absorption: Sparfloxacin is well absorbed after oral administration, with an absolute oral bioavailability of approximately 92%. Following a single 400 mg oral dose, the mean peak plasma concentration is about 1.3 ± 0.2 µg/mL, and the mean area under the curve (AUC) is approximately 34 ± 6.8 µg·hr/mL. Steady-state plasma concentrations can be achieved on the first day when a loading dose equal to twice the daily dose is given. After a 200 mg dose, peak plasma concentrations are generally reached within 3 to 6 hours, with an average of about 4 hours. Oral absorption of sparfloxacin is not affected by food or milk, including high-fat meals. However, concurrent use of antacids containing magnesium hydroxide or aluminium hydroxide may reduce its oral bioavailability by up to 50%.

Distribution: After entering the systemic circulation, sparfloxacin is widely distributed throughout the body, with a mean steady-state volume of distribution (Vdss) of approximately 3.9 ± 0.8 L/kg. Plasma protein binding is relatively low, at about 45%. Sparfloxacin penetrates well into body tissues and fluids. Studies have shown that concentrations in lower respiratory tract tissues and fluids generally exceed corresponding plasma levels. Concentrations in respiratory tissues such as the pulmonary parenchyma, bronchial wall, and bronchial mucosa are approximately 3 to 6 times higher than plasma concentrations within 2 to 6 hours after oral administration, and these levels may continue to increase for up to 24 hours. Sparfloxacin also accumulates significantly in alveolar macrophages. The mean pleural effusion-to-plasma concentration ratios are reported to be 0.34 at 4 hours and 0.69 at 20 hours after dosing.

Metabolism: Sparfloxacin is metabolized in the liver, mainly through phase II glucuronidation, forming a glucuronide conjugate. Its metabolism does not involve cytochrome P450-mediated oxidation.

Excretion: The total body clearance and renal clearance of sparfloxacin are approximately 11.4 ± 3.5 L/hr and 1.5 ± 0.5 L/hr, respectively. Sparfloxacin is eliminated through both the feces (50%) and urine (50%). In patients with normal renal function, approximately 10% of an oral dose is excreted unchanged in the urine.

In patients with normal renal function, the recommended dosage of sparfloxacin is two 200 mg tablets on the first day as a loading dose. Thereafter, one 200 mg tablet once every 24 hours should be taken to complete a total of 10 days of treatment (11 tablets in total). In patients with renal impairment (creatinine clearance <50 mL/min), the recommended dosage is two 200 mg tablets on the first day as a loading dose. Thereafter, one 200 mg tablet once every 48 hours should be taken for a total of 9 days of treatment (6 tablets in total).

Antacids and sucralfate containing aluminium or magnesium may form chelation complexes with sparfloxacin, thereby reducing its absorption. Concomitant use of sparfloxacin with medications known to prolong the QTc interval and/or cause Torsade de pointes (for example, terfenadine) should be avoided. Sparfloxacin does not significantly interact with theophylline, caffeine, warfarin, or cimetidine. In addition, probenecid does not significantly alter the pharmacokinetics of sparfloxacin.

• Sparfloxacin is contraindicated in patients with known hypersensitivity to sparfloxacin or any of its components.
• It is also contraindicated during pregnancy and lactation,
• in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency,
• in those with a history of Achilles tendinitis associated with fluoroquinolone use.

Most adverse effects of sparfloxacin are mild to moderate in severity and transient in nature. The most frequently reported side effects at the recommended dosage include photosensitivity reactions, diarrhoea, nausea, headache, dyspepsia, dizziness, insomnia, abdominal pain, pruritus, taste disturbance, QTc interval prolongation, vomiting, flatulence, and vasodilatation.

There are no adequate and well-controlled studies on the use of sparfloxacin in pregnant women. Therefore, sparfloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Special Warnings: Moderate to severe phototoxic reactions may occur in patients exposed to direct or indirect sunlight or to artificial ultraviolet light (such as sunlamps) during or after treatment with sparfloxacin. Patients should be advised to discontinue sparfloxacin immediately at the first signs or symptoms of phototoxicity, including:

• Burning sensation of the skin
• Swelling
• Rash
• Itching
• Dermatitis

Sparfloxacin may also cause prolongation of the QTc interval. The safety and efficacy of sparfloxacin have not been established in children and adolescents under 18 years of age, pregnant women, or lactating women.

Precautions: Adequate hydration should be maintained in patients receiving sparfloxacin to help prevent the formation of highly concentrated urine. Sparfloxacin should be used with caution in patients with renal insufficiency. Concomitant use with medications known to prolong the QTc interval (such as erythromycin and terfenadine) should be avoided. Patients should also avoid excessive exposure to sunlight during treatment.

Geriatric: The pharmacokinetics of sparfloxacin are not significantly altered in elderly patients with normal renal function.

Paediatric: The pharmacokinetics of sparfloxacin in paediatric patients have not been studied.

Gender: There are no significant gender-related differences in the pharmacokinetics of sparfloxacin.

Renal insufficiency: In patients with renal impairment (creatinine clearance <50 mL/min), the terminal elimination half-life of sparfloxacin is prolonged. Single or multiple doses in patients with varying degrees of renal impairment generally produce plasma concentrations about twice as high as those observed in individuals with normal renal function.

Hepatic impairment: The pharmacokinetics of sparfloxacin are not significantly affected in patients with mild to moderate hepatic impairment without cholestasis.

4-Quinolone preparations

Store below 30°C, away from heat and direct light. Keep out of the reach of children.