Sparfloxacin

Brand Names of Sparfloxacin in Kenya:

Sparbact®, IPCA
Sparflo®, Dr.Reddy
Sparta®,Alembic
Sparx®, Wockhardt Ltd.

SPARFLOXACIN MODE OF ACTION

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

INDICATIONS:

  • 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
  • Leprosy ( Borderline and Lepromatous

DOSAGE AND ADMINISTRATION

Acute bacterial exacerbations of chronic bronchitis:
400 mg orally once as a loading dose, followed by 200 mg orally once a day thereafter for a total of 10 days.

Leprosy – Borderline

200 mg orally daily.
Therapy may be required for several months to 1 year, depending on clinical and histopathological response.
Sparfloxacin has been used successfully in a limited number of patients either alone, or followed by the WHO recommended regimen of rifampin, dapsone, and clofazimine.

Leprosy – Lepromatous

200 mg orally daily.
Therapy may be required for several months to 1 year, depending on clinical and histopathological response.
Sparfloxacin has been used successfully in a limited number of patients either alone, or followed by the WHO recommended regimen of rifampin, dapsone, and clofazimine.

Community-acquired pneumonia:
400 mg orally once as a loading dose, followed by 200 mg orally once a day thereafter for a total of 10 days.

CONTRAINDICATIONS

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.

Absorption:
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

Excretion:
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.

DRUG INTERACTIONS

Coadministration with nonsteroidal anti-inflammatory drugs (NSAIDs) may potentiate the risk of central nervous system toxicity sometimes associated with fluoroquinolone use. The interaction has been reported most often with enoxacin. It may occur with other fluoroquinolones as well, but is poorly documented. The exact mechanism of interaction is unknown. Some investigators suggest that the piperazine ring of fluoroquinolones may inhibit the binding of gamma-aminobutyric acid (GABA) to brain receptors and that NSAIDs may synergistically add to this effect. Patients with a history of seizures may be at greater risk.

Limited data suggest that sulfamethoxazole-trimethoprim (SMX-TMP) may rarely prolong the QT interval of the electrocardiogram. Theoretically, coadministration with other agents that can prolong the QT interval may result in additive effects and increased risk of ventricular arrhythmias including torsade de pointes and sudden death.

Quinolone antibiotics may interfere with the therapeutic effects of insulin and other antidiabetic agents. The use of quinolones has been associated with disturbances in blood glucose homeostasis possibly stemming from effects on pancreatic beta cell ATP-sensitive potassium channels that regulate insulin secretion.

There have been isolated reports of QT prolongation and ventricular arrhythmias occurring in patients treated with metronidazole. However, a causal relationship has not been established, as nearly all published reports have involved underlying conditions and/or concomitant medications that predispose to QT prolongation.

ADVERSE REACTIONS

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.

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Sparfloxacin