MOA: Fluoroquinolones act by inhibiting two enzymes involved in bacterial DNA synthesis, both of which are DNA topoisomerases that human cells lack and that are essential for bacterial DNA replication, thereby enabling these agents to be both specific and bactericidal
Drug Label Information | Brands:
Brands of Sparfloxacin in Kenya:
Community-acquired pneumonia caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae
Acute bacterial exacerbations of chronic bronchitis caused by Chlamydia pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Staphylococcus aureus, or Streptococcus pneumoniae
Sparfloxacin is contraindicated for individuals with a history of hypersensitivity or photosensitivity reactions.
Torsade de pointes has been reported in patients receiving sparfloxacin concomitantly with disopyramide and amiodarone.Consequently, sparfloxacin is contraindicated for individuals receiving these drugs as well as other QTc-prolongingantiarrhythmic drugs reported to cause torsade de pointes, such as class Ia antiarrhythmic agents (e.g., quinidine, procainamide), class III antiarrhythmic agents(e.g., sotalol), and bepridil.
Sparfloxacin is well absorbed following oral administration with an absolute oral bioavailability of 92%.
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, sparfloxacin distributes well into the body, as reflected by the large mean steady-state volume of distribution (Vdss) of3.9 (±0.8) L/kg. Sparfloxacin exhibits low plasma protein binding in serum at about45%. 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
Metabolism: Sparfloxacin is metabolized 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
Sparfloxacin is excreted in both the faeces (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.
Serious and occasionally fatal hypersensitivity (including anaphylactoid or anaphylactic) reactions, some following the first dose, have been reported in patients receiving quinolones. Some reactions were accompanied by cardiovascular collapse, hypotension/shock, seizure, loss of consciousness, tingling, angioedema (including the tongue, laryngeal, throat, or facial oedema), airway obstruction (including bronchospasm, shortness of breath, and acute respiratory distress), dyspnea, urticaria, and/or itching. Only a few patients had a history of previous hypersensitivity reactions. If an allergic reaction to sparfloxacin occurs, the drug should be discontinued immediately. Serious acute hypersensitivity reactions may require immediate treatment with epinephrine, and other resuscitative measures including oxygen, intravenous fluids, antihistamines, corticosteroids, pressor amines, and airway management, including intubation, as clinically indicated.