Acespan Uses, Dosage, Side Effects and more

Acespan 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).

Acespan 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.

Acespan is a synthetic fluoroquinolone broad-spectrum antimicrobial agent in the same class as ofloxacin and norfloxacin. Acespan has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Acespan 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	Acespan
Availability	Discontinued
Generic	Sparfloxacin
Sparfloxacin Other Names	Sparfloxacin
Related Drugs	amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, rifampin
Type	Tablet
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Groups	Approved, Investigational, Withdrawn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	Lifespan Pharmaceuticals Pvt Ltd
Available Country	India
Last Updated:	January 7, 2025 at 1:49 am

Uses

Acespan 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.

Acespan is also used to associated treatment for these conditions: Acute Sinusitis, Chronic Obstructive Airways Disease Exacerbated, Community Acquired Pneumonia (CAP), Susceptible infections

How Acespan 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

In patients with normal renal function the recommended daily dose is two tablets of Acespan 200 mg on first day as a loading dose, thereafter take one tablet of Acespan 200 mg every 24 hours for a total of 10 days of therapy.

The recommended daily dose of Acespan 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.

Acespan 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 Acespan 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, Acespan 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 Acespan.

Acespan 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.

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

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. Acespan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Contraindication

Acespan 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. Acespan 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.

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