Sparfloxacin is indicated for the treatment of the following infections due to susceptible microorganisms: Upper and lower respiratory tract infections including sinusitis, acute exacerbation of chronic bronchitis, community and hospital acquired pneumonia. Urinary tract infections including gonococcal and non-gonococcal urethritis, chancroid and other sexually transmitted diseases. Skin and soft tissue infections. Prophylactic use in different urological and ophthalmic operations.
Sparfloxacin is a broad-spectrum antibacterial agent that inhibit DNA gyrase and topoisomerase IV and kills many of the types of bacteria that can infect the breathing airways and lungs and has been shown in a large number of clinical trials to be safe and effective for the treatment of bacterial infections. It is found to be more effective in vitro than other fluoroquinolones against some gram positive organisms (Streptococcus pneumoniae, Staphylococcus aureous), Mycobacteria and Chlamydia spp.
Absorption: Quinoflox‚ is well absorbed following oral administration with an absolute oral bioavailability of 92%. The mean maximum plasma sparfloxacin concentration following a single 400-mg oral dose was approximately 1.3 (±0.2) µg/mL. The area under the curve following a single 400-mg oral dose was approximately 34 (±6.8) µg·hr/mL. Steady-state plasma concentration was achieved on the first day by giving a loading dose that was double the daily dose. Maximum plasma concentrations for a 200 mg dose were also achieved between 3 to 6 hours after administration with a mean of about 4 hours. Oral absorption of sparfloxacin is unaffected by administration with milk or food, including high fat meals. Concurrent administration of antacids containing magnesium hydroxide and aluminium hydroxide reduces the oral bioavailability of sparfloxacin by as much as 50%.
Distribution: Upon reaching general circulation, Quinoflox‚ distributes well into the body, as reflected by the large mean steady-state volume of distribution (Vdss ) of 3.9 (±0.8) L/kg. Sparfloxacin exhibits low plasma protein binding in serum at about 45%. Sparfloxacin penetrates well into body fluids and tissues. Results of tissue and body fluid distribution studies demonstrated that oral administration of sparfloxacin produces sustained concentrations and that sparfloxacin concentrations in lower respiratory tract tissues and fluids generally exceed the corresponding plasma concentrations. The concentration of sparfloxacin in respiratory tissues (pulmonary parenchyma, bronchial wall, and bronchial mucosa) at 2 to 6 hours following standard oral dosing was approximately 3 to 6 times greater than the corresponding concentration in plasma. Concentrations in these respiratory tissues increase at up to 24 hours following dosing. Sparfloxacin is also highly concentrated into alveolar macrophages compared to plasma. Mean pleural effusion to plasma concentration ratios were 0.34 and 0.69 at 4 and 20 hours postdose, respectively.
Metabolism: Quinoflox‚ is metabolised by the liver, primarily by phase II glucuronidation, to form a glucuronide conjugate. Its metabolism does not utilize or interfere with cytochrome-mediated oxidation, in particular cytochrome P450.
Excretion: The total body clearance and renal clearance of Quinoflox‚ were 11.4 (±3.5) and 1.5 (±0.5) L/hr, respectively. Sparfloxacin is excreted in both the feces (50%) and urine (50%). Approximately 10% of an orally administered dose is excreted in the urine as unchanged drug in patients with normal renal function.
In patients with normal renal function the recommended daily dose is two tablets of Sparfloxacin 200 mg on first day as a loading dose, thereafter take one tablet of Sparfloxacin 200 mg every 24 hours for a total of 10 days of therapy. The recommended daily dose of Sparfloxacin in patients with renal impairment (Creatinine clearance < 30 ml/min) is two tablets of 200 mg taken on the first day as a loading dose. Thereafter, should be taken one tablet of 200 mg every 48 hours for total of 9 days of therapy. Sparfloxacin can be taken with or without food.
Aluminium and Magnesium cations in antacids and sucralfate form chelation complexes with sparfloxacin. Concomitant use with medications known to produce an increase in the QTc interval and/or Torsade de pointes (e.g., terfenadine). Sparfloxacin does not interact with theophylline or caffeine, nor with warfarin or cimetidine. Probenecid does not alter the pharmacokinetics of sparfloxacin.
Sparfloxacin is contraindicated for individuals with a history of hypersensifivity and in achilles tend in its following the use of fluoroquinolone and in pregnancy and lactation. Sparfloxacin is contraindicated in patients with known QTc prolongation or in patients being treated concomitantly with medications known to produce an increase in the QTc interval and/or torsade depointes. It should be used with caution in renal diseases, gastric ulcers and with concomitant use of NSAIDs. In renal failure of third degree severity (creatinine clearance < 30 ml/min) dosage modification is recommended 400 mg on 1st day, 200 mg on 2nd and 3rd day followed by 200 mg every 48 hours. Because fluoroquinolones have been associated with tendon rupture, Sparfloxacin should be discontinued at the first sign of tendon pain. Exposure to UV radiation during treatment should be avoided.
Most of the adverse events were mild to moderate in severity and transient in nature. The most frequently reported events among the Sparfloxacin treated patients with the recommended dosage are: diarrhea, nausea, headache, dyspepsia, dizziness, insomnia, abdominal pain and QTc interval prolongation.
There are no adequate and well controlled studies in pregnant women. Sparfloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
To store this medicine it should be kept out of the reach of children. Stored away from heat and direct light. Stored below 30ºC.
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