Sparfloxacin, Uses, Dosage, Side effects, Interactions, Pregnancy

Sparfloxacin, Uses, Dosage, Side effects, Interactions, Pregnancy

Sparfloxacin is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase, thereby inhibiting DNA replication and transcription. Sparfloxacin was withdrawn from the U.S. market due to a high incidence of phototoxicity.
Sparfloxacin is a fluoroquinolone antibiotic used in the treatment of bacterial infections. Sparfloxacin 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.

Mechanism of action of Sparfloxacin

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 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.

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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.

Indications of Sparfloxacin 

  • For the treatment of adults with the following infections caused by susceptible strains microorganisms: community-acquired pneumonia (caused by Chlamydia pneumoniaeHaemophilus influenzaeHaemophilus parainfluenzaeMoraxella catarrhalisMycoplasma pneumoniae, or Streptococcus pneumoniae) and acute bacterial exacerbations of chronic bronchitis (caused by Chlamydia pneumoniaeEnterobacter cloacaeHaemophilus influenzaeHaemophilus parainfluenzaeKlebsiella pneumoniaeMoraxella catarrhalisStaphylococcus aureus, or Streptococcus pneumoniae).
  • Treatment of radiologically confirmed community acquired pneumonia which has failed to respond to conventional therapy
  • Community-acquired pneumonia
  • Bacterial Infection
  • Bronchitis
  • Acute bacterial exacerbations of chronic bronchitis
  • Leprosy, Borderline
  • Leprosy, Lepromatous
  • Pneumonia
  • Acne,
  • Burns,
  • Conjunctivitis,
  • Cystitis,
  • Dysenteries,
  • Folliculitis,
  • Impetigo,
  • Otitis media,
  • Prostatitis,
  • Pyelonephritis,
  • Respiratory tract infections,
  • Sinusitis,
  • Superficial infections,
  • Surgical infections,
  • Tonsillitis,
  • Urethritis
  • Travelers’ Diarrhea
  • Ulcerative keratitis
  • Uncomplicated Cystitis
  • Bronchitis
  • Campylobacter Gastroenteritis
  • Cervicitis
  • Chancroid
  • Chlamydia Infection
  • Epididymitis, Non-Specific
  • Epididymitis, Sexually Transmitted
  • Joint Infection
  • Kidney Infections
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Contra-Indications of Sparfloxacin 

  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.
  • Allergy
  • Avoid taking this medicine if you have a known allergy to it or any other fluoroquinolones.
  • Tendinitis or tendon rupture
  • Avoid if you have a past history of tendinitis or tendon rupture after using this medicine.
  • Myasthenia Gravis
Avoid if you have a past history of myasthenia gravis or family history of myasthenia gravis.

Dosage of Sparfloxacin 

Strengths : 100 mg, 200 mg, 400 mg

Sparfloxacin’s dosage details are as follows

Dose
Single Dose
Frequency
Route
Instructions
Adult Dosage
100 to 200 mg
150 (150)
12 hourly
PO
Maintenance.
400 mg
400 (400)
24 hourly
PO
Initially.
Paedriatic Dosage (20kg)
Not recommended in this age group
Neonatal Dosage (3kg)
Not recommended in this age group

Bronchitis

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.

Pneumonia

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.

Side Effects of Sparfloxacin 

The most common 

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More common

Rare

Drug Interactions of Sparfloxacin 

Sparfloxacin may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Sparfloxacin 

FDA Pregnancy Category C 

Pregnancy

Sparfloxacin has been assigned to pregnancy category C by the FDA. High-dose animal studies revealed no evidence of teratogenicity. However, when studied in rats at maternally toxic doses (9.3 times the maximum human dose based on mg/m2) there was an increased incidence of fetuses with ventricular septal defects. This event was not observed in monkeys or rabbits at maternally toxic doses. There are no controlled data in human pregnancy.

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Lactation

Sparfloxacin is excreted into human milk. Cartilage erosion and arthropathy have been reported in immature animals giving rise to concern over toxic effects in the developing joints of nursing infants. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

  1. References
    1. https://www.drugs.com/mtm/sparfloxacin.html
    2. https://www.webmd.com/drugs/2/drug-36/sparfloxacin-oral/details
    3. https://pubchem.ncbi.nlm.nih.gov

    4. https://www.ncbi.nlm.nih.gov/projects/linkout

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