Sparfloxacin
Sparfloxacin Uses, Dosage, Side Effects, Food Interaction and all others data.
Sparfloxacin is a synthetic, broad-spectrum antibacterial agent from the difluoroquinolone family. It has been reported to be more active in vitro than ciprofloxacin against some organisms, including staphylococci and Mycobacteria, and has a much longer plasma half-life (16 hours).
Sparfloxacin inhibits the supercoiling activity of DNA gyrase which is an enzyme essential for DNA replication thus promoting the breakage of DNA structures. It has activity against S. pneumoniae, S. aureus, H. influenzae, K. pneumoniae, M. catarrhalis and Mycobacterium spp.
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.
Trade Name | Sparfloxacin |
Availability | Discontinued |
Generic | Sparfloxacin |
Sparfloxacin Other Names | Sparfloxacin |
Related Drugs | amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, rifampin |
Type | Oral |
Formula | C19H22F2N4O3 |
Weight | Average: 392.3998 Monoisotopic: 392.165997 |
Protein binding | Low plasma protein binding in serum at about 45%. |
Groups | Approved, Investigational, Withdrawn |
Therapeutic Class | 4-Quinolone preparations |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Sparfloxacin is used for the treatment of the following infections due to susceptible microorganisms:
- Upper and lower respiratory tract infections including sinusitis, acute exacerbation of chronic bronchitis, community and hospital acquired pneumonia.
- Urinary tract infections including gonococcal and non-gonococcal urethritis, chancroid and other sexually transmitted diseases.
- Skin and soft tissue infections.
- Prophylactic use in different urological and ophthalmic operations.
Sparfloxacin is also used to associated treatment for these conditions: Acute Sinusitis, Chronic Obstructive Airways Disease Exacerbated, Community Acquired Pneumonia (CAP), Susceptible infections
How Sparfloxacin works
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.
Dosage
Sparfloxacin dosage
In patients with normal renal function the recommended daily dose is two tablets of Sparfloxacin 200 mg on first day as a loading dose, thereafter take one tablet of Sparfloxacin 200 mg every 24 hours for a total of 10 days of therapy.
The recommended daily dose of Sparfloxacin in patients with renal impairment (Creatinine clearance < 30 ml/min) is two tablets of 200 mg taken on the first day as a loading dose. Thereafter, should be taken one tablet of 200 mg every 48 hours for total of 9 days of therapy.
Sparfloxacin can be taken with or without food.
Side Effects
Most of the adverse events were mild to moderate in severity and transient in nature. The most frequently reported events among the Sparfloxacin treated patients with the recommended dosage are: diarrhea, nausea, headache, dyspepsia, dizziness, insomnia, abdominal pain and QTc interval prolongation.
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.
Precaution
It should be used with caution in renal diseases, gastric ulcers and with concomitant use of NSAIDs. In renal failure of third degree severity (creatinine clearance < 30 ml/min) dosage modification is recommended 400 mg on 1st day, 200 mg on 2nd and 3rd day followed by 200 mg every 48 hours. Because fluoroquinolones have been associated with tendon rupture, Sparfloxacin should be discontinued at the first sign of tendon pain. Exposure to UV radiation during treatment should be avoided.
Interaction
On concomitant use with Quinidine, Sotalol, Erythromycin, Astemizole, Terfenadine, vinca alkaloids there is increased risk of arrhythmia. Salts, oxides and hydroxides of Magnesium, Aluminium and Calcium decrease absorption of Sparfloxacin.
Sparfloxacin multivitamins interaction
[Moderate] ADJUST DOSING INTERVAL: Oral preparations that contain magnesium, aluminum, or calcium may significantly decrease the gastrointestinal absorption of quinolone antibiotics.
Absorption may also be reduced by sucralfate, which contains aluminum, as well as other polyvalent cations such as iron and zinc.
The mechanism is chelation of quinolones by polyvalent cations, forming a complex that is poorly absorbed from the gastrointestinal tract.
The bioavailability of ciprofloxacin has been reported to decrease by as much as 90% when administered with antacids containing aluminum or magnesium hydroxide.
When coadministration cannot be avoided, quinolone antibiotics should be dosed either 2 to 4 hours before or 4 to 6 hours after polyvalent cation-containing products to minimize the potential for interaction.
When coadministered with Suprep Bowel Prep (magnesium Please consult individual product labeling for specific recommendations.
Sparfloxacin Drug Interaction
Major: glyburide / metformin, dextromethorphan / promethazineModerate: aspirin, celecoxib, multivitamin with minerals, metronidazoleMinor: sulfamethoxazole / trimethoprimUnknown: amikacin, amoxicillin / clavulanate, amoxicillin, ciprofloxacin, clomiphene, lvp solution, omega-3 polyunsaturated fatty acids, amlodipine / valsartan, chondroitin / glucosamine / methylsulfonylmethane, nifedipine, acetaminophen, lvp solution with potassium, omeprazole
Sparfloxacin Disease Interaction
Major: colitis, CNS disorders, myasthenia gravis, peripheral neuropathy, tendonitis, QT interval prolongationModerate: crystalluria, diabetes, renal dysfunction
Elimination Route
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%.
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).
Pregnancy & Breastfeeding use
There are no adequate and well controlled studies in pregnant women. Sparfloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Contraindication
Sparfloxacin is contraindicated for individuals with a history of hypersensifivity and in achilles tend in its following the use of fluoroquinolone and in pregnancy and lactation. Sparfloxacin is contraindicated in patients with known QTc prolongation or in patients being treated concomitantly with medications known to produce an increase in the QTc interval and/or torsade depointes.
Special Warning
Use in children: Safety and effectiveness have not been established in patients below the age of 18 years.
Storage Condition
Store at temperature below 30° C.
Innovators Monograph
You find simplified version here Sparfloxacin
Sparfloxacin contains Sparfloxacin see full prescribing information from innovator Sparfloxacin Monograph, Sparfloxacin MSDS, Sparfloxacin FDA label
FAQ
What is Sparfloxacin used for?
Sparfloxacin is an antibiotic in a class of drugs called fluoroquinolones. It fights bacteria in the body. Sparfloxacin is used to treat various types of bacterial infections.
How safe is Sparfloxacin?
Sparfloxacin passes into breast milk and may harm a nursing infant. It may affect bone development. Do not take this medication without first talking to your doctor if you are breast-feeding a baby.
What are the common side effects of Sparfloxacin?
The common side effects of Sparfloxacin are include:
- nausea
- vomiting
- diarrhea
- constipation
- headache
- lightheadedness
- drowsiness
- ringing in the ears
- increased sensitivity of the skin to sunlight
- indigestion
- dizziness
- insomnia
- abdominal pain
- itching
- changes in taste
- gas
- elevated blood pressure, and
- heart rhythm disorders
Is Sparfloxacin safe during breastfeeding?
Sparfloxacin should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby. No studies have been done in animals, and no well-controlled studies have been done in pregnant women. Sparfloxacin should be given to a pregnant woman only if clearly needed.
Is Sparfloxacin safe during pregnancy?
Use of Sparfloxacin is acceptable in nursing mothers with monitoring of the infant for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis.
How should I take Sparfloxacin?
Take Sparfloxacin exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you.
Take each dose with a full glass of water (8 ounces). Drink several extra glasses of fluid each day to prevent the formation of Sparfloxacin crystals in your urine.
How do I take Sparfloxacin?
Take each dose with a full glass of water (8 ounces). Drink several extra glasses of fluid each day to prevent the formation of Sparfloxacin crystals in your urine.Sparfloxacin may be taken with or without food. Take Sparfloxacin at evenly spaced intervals.
How long does Sparfloxacin take to work?
You will start to feel better in 2 to 3 days after taking/using Sparfloxacin.
What happens if I miss a dose of Sparfloxacin?
Take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose of this medication unless otherwise directed by your doctor.
What happens if I overdose?
Seek emergency medical attention.
The most common symptom of a Sparfloxacin overdose is irregular or slow heartbeats.
Can I drive after taking Sparfloxacin?
Do not drive a car or work on dangerous machines until you know how Sparfloxacin will affect you. plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen.
Can Sparfloxacin treat staphylococcus?
In vitro tests show that the combination of Sparfloxacin and rifampin is antagonistic against Staphylococcus aureus.
Is Sparfloxacin an antibiotic?
Sparfloxacin is an antibiotic in a class of drugs called fluoroquinolones. It fights bacteria in the body. Sparfloxacin is used to treat various types of bacterial infections.