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QuickView for Sparfloxacin (compound)

Name: sparfloxacin
PubChem Compound ID: 11618070
Molecular formula: C19H22F2N4O3
Molecular weight: 391.402 g/mol
Name: sparfloxacin
Name (isomeric): DB01208
Drug Type: small molecule
Brand: Zagam
Category: Antitubercular Agents
CAS number: 110871-86-8
Indication: For the treatment of adults with the following infections caused by susceptible strains microorganisms: community-acquired pneumonia (caused by <i>Chlamydia pneumoniae</i>, <i>Haemophilus influenzae</i>, <i>Haemophilus parainfluenzae</i>, <i>Moraxella catarrhalis</i>, <i>Mycoplasma pneumoniae</i>, or <i>Streptococcus pneumoniae</i>) and acute bacterial exacerbations of chronic bronchitis (caused by <i>Chlamydia pneumoniae</i>, <i>Enterobacter cloacae</i>, <i>Haemophilus influenzae</i>, <i>Haemophilus parainfluenzae</i>, <i>Klebsiella pneumoniae</i>, <i>Moraxella catarrhalis</i>, <i>Staphylococcus aureus</i>, or <i>Streptococcus pneumoniae</i>).
Sparfloxacin is a synthetic fluoroquinolone broad-spectrum antimicrobial agent in the same class as ofloxacin and norfloxacin. Sparfloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an...
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Mechanism of Action: The bactericidal action of sparfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.
Absorption: Well absorbed following oral administration with an absolute oral bioavailability of 92%. Unaffected by administration with milk or food, however concurrent administration of antacids containing magnesium hydroxide and aluminum hydroxide reduces the oral bioavailability of sparfloxacin by as much as 50%.
Protein binding: Low plasma protein binding in serum at about 45%.
Biotransformation: Hepatic. Metabolized primarily by phase II glucuronidation to form a glucuronide conjugate. Metabolism does not utilize or interfere with the cytochrome P450 enzyme system.
Half Life: Mean terminal elimination half-life of 20 hours (range 16-30 hours). Prolonged in patients with renal impairment (creatinine clearance <50 mL/min).
Toxicity: Single doses of sparfloxacin were relatively non-toxic via the oral route of administration in mice, rats, and dogs. No deaths occurred within a 14-day post-treatment observation period at the highest oral doses tested, up to 5000 mg/kg in either rodent species, or up to 600 mg/kg in the dog. Clinical signs observed included inactivity in mice and dogs, diarrhea in both rodent species, and vomiting, salivation, and tremors in dogs.
Affected organisms: Enteric bacteria and other eubacteria
Drug interaction:
ErythromycinIncreased risk of cardiotoxicity and arrhythmias
DisopyramideIncreased risk of cardiotoxicity and arrhythmias
ChlorpromazineIncreased risk of cardiotoxicity and arrhythmias
ImipramineIncreased risk of cardiotoxicity and arrhythmias
NortriptylineIncreased risk of cardiotoxicity and arrhythmias
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