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 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).
- 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
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
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
- Abdominal or stomach cramps and pain (severe)
- diarrhea (watery and severe), which may also be bloody
- pain, inflammation, or swelling in calves, shoulders, or hands
- allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
- pain, swelling, irritation where injected
- sweating
- skin color change, mild diarrhea
- mild nausea
- loss of appetite
- swelling of feet or legs
- chest pain
- constipation
- cough
- difficulty with breathing
- dizziness
- heartburn
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- decreased amount of urine
Rare
- Anxiety
- change in vision
- seizures
- tremors
- weight loss
- chest pain or tightness
- confusion
- cough
- Agitation
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
Drug Interactions of Sparfloxacin
Sparfloxacin may interact with following drugs, supplements, & may change the efficacy of drugs
- antacids that contain aluminum, calcium, or magnesium
- birth control medications
- bismuth subsalicylate
- calcium supplements
- digoxin
- Rosuvastatin
- Duloxetine
- Albuterol
- Topiramate
- Carbamazepine
- Vitamin D3 (cholecalciferol)
- Alprazolam
- Cetirizine
- insulin
- iron supplements
- penicillin
- vitamin A derivatives (e.g. isotretinoin)
- warfarin
- zinc sulfate or gluconate
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.
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.
