Zagam
Zagam - General Information
Zagam is a fluoroquinolone antibiotic used in the treatment of bacterial infections. Zagam exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription.
Pharmacology of Zagam
Zagam is a synthetic fluoroquinolone broad-spectrum antimicrobial agent in the same class as ofloxacin and norfloxacin. Zagam has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Zagam exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription. Quinolones differ in chemical structure and mode of action from (beta)-lactam antibiotics. Quinolones may, therefore, be active against bacteria resistant to (beta)-lactam antibiotics. Although cross-resistance has been observed between sparfloxacin and other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to sparfloxacin. In vitro tests show that the combination of sparfloxacin and rifampin is antagonistic against Staphylococcus aureus.
Zagam for patients
Zagam Interactions
Digoxin: Sparfloxacin has no effect on the pharmacokinetics of digoxin.
Methylxanthines: Sparfloxacin does not increase plasma theophylline concentrations. Since there is no interaction with theophylline, interaction with other methylxanthines such as caffeine is unlikely.
Warfarin: Sparfloxacin does not increase the anti-coagulant effect of warfarin.
Cimetidine: Cimetidine does not affect the pharmacokinetics of sparfloxacin.
Antacids and Sucralfate: Aluminum and magnesium cations in antacids and sucralfate form chelation complexes with sparfloxacin. The oral bioavailability of sparfloxacin is reduced when an aluminum-magnesium suspension is administered between 2 hours before and 2 hours after sparfloxacin administration. The oral bioavailability of sparfloxacin is not reduced when the aluminum-magnesium suspension is administered 4 hours following sparfloxacin administration.
Zinc/iron salts: Absorption of quinolones is reduced significantly by these preparations. These products may be taken 4 hours after sparfloxacin administration.
Probenecid: Probenecid does not alter the pharmacokinetics of sparfloxacin.
Zagam 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 QT c -prolonging antiarrhythmic 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 contraindicated in patients with known QT c prolongation or in patients being treated concomitantly with medications known to produce an increase in the QT c interval and/or torsade de pointes (e.g., terfenadine).
It is essential to avoid exposure to the sun, bright natural light, and UV rays throughout the entire duration of treatment and for 5 days after treatment is stopped. Sparfloxacin is contraindicated in patients whose life-style or employment will not permit compliance with required safety precautions concerning phototoxicity.
Additional information about Zagam
Zagam Indication: For the treatment of adults with the following infections caused by susceptible strains microorganisms: community-acquired pneumonia (caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae) and 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).
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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Sparfloxacin
Synonyms: Not Available
Drug Category: Antitubercular Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Sparfloxacin: Zagam;
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%.
Toxicity (Overdose): 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.
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).
Dosage Forms of Zagam: Tablet, film coated Oral
Chemical IUPAC Name: 5-amino-1-cyclopropyl-7-[(3S,5R)-3,5-dimethylpiperazin-1-yl]-6,8-difluoro-4-oxoquinoline-3-carboxylic acid
Chemical Formula: C19H22F2N4O3
Sparfloxacin on Wikipedia: https://en.wikipedia.org/wiki/Sparfloxacin
Organisms Affected: Enteric bacteria and other eubacteria
