Raspelocin Uses, Dosage, Side Effects and more

Raspelocin is a synthetic broad spectrum, flouroquinolone derivative antibacterial agent. Raspelocin has in vitro activity against a wide range of Gram-positive and Gram-negative microorganisms. The bactericidal action of Raspelocin results from inhibition of the topoisomerase II (DNA gyrase) and topoisomerase IV required for bacterial DNA replication, transcription, repair and recombination.

Raspelocin is a quinolone/fluoroquinolone antibiotic. Raspelocin can be used to treat infections caused by the following bacteria: Aerobic Gram-positive microorganisms: Corynebacterium species, Micrococcus luteus, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus warneri, Streptococcus pneumoniae, and Streptococcus viridans group. Aerobic Gram-negative microorganisms: Acinetobacter lwoffii, Haemophilus influenzae, and Haemophilus parainfluenzae. Other microorganisms: Chlamydia trachomatis.Raspelocin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Raspelocin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.

Trade Name	Raspelocin
Availability	Prescription only
Generic	Moxifloxacin
Moxifloxacin Other Names	Moxifloxacin, Moxifloxacino
Related Drugs	amoxicillin, prednisone, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin
Type
Formula	C21H24FN3O4
Weight	Average: 401.4314 Monoisotopic: 401.175084476
Protein binding	50% bound to serum proteins, independent of drug concentration.
Groups	Approved, Investigational
Therapeutic Class	4-Quinolone preparations
Manufacturer
Available Country	Egypt
Last Updated:	January 7, 2025 at 1:49 am

Uses

Raspelocin is used for the treatment of adults (>18 years of age) with infections caused by susceptible strains of the designated microorganisms in the conditions listed below-

• Acute Bacterial Sinusitis caused by Streptococcus pneumoniae, Haemophilus infuenzae or Moraxella catarrhalis.
• Acute Bacterial Exacerbation of Chronic Bronchitis caused by Streptococcus pneumoniae, Haemophilus infuenzae, Haemophilus parainfuenzae, Klebsiella pneumoniae, methicillin-susceptible Staphylococcus aureus or Moraxella catarrhalis
• Community Acquired Pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant strains), Haemophilus infuenzae, Moraxella catarrhalis, methicillin-susceptible Staphylococcus aureus, Klebsiella pneumoniae, Mycoplasma pneumoniae or Chlamydophilia pneumoniae.
• Uncomplicated Skin and Skin Structure Infections caused by methicillin-susceptible Staphylococcus aureus or Streptococcus pyogen.
• Complicated Skin and Skin Structure Infections caused by methicillin-susceptible Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae or Enterobacter cloacae.
• Complicated Intra-Abdominal Infections including polymicrobial infections such as abscess caused by Escherichia coli, Bacteroides fragilis, Streptococcus anginosus, Streptococcus constellatus, Enterococcus faecalis, Proteus mirabilis, Clostridium perfringens, Bacteroides thetaiotaomicron or Peptostreptococcus species.

Raspelocin is also used to associated treatment for these conditions: Acute Exacerbation of Chronic Bronchitis (AECB), Bacterial Conjunctivitis, Community Acquired Pneumonia (CAP), Plague, Postoperative Inflammatory Response, Sinusitis, Skin Infections, Ocular bacterial infections, Post-operative infection

How Raspelocin works

The bactericidal action of moxifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

Dosage

The dose of Raspelocin is 400 mg once every 24 hours. The duration of therapy depends on the type of infection as described bellow-

• In Acute Bacterial Sinusitis: Raspelocin 400 mg is given once daily for 10 days.
• In Acute Bacterial Exacerbation of Chronic Bronchitis: Raspelocin 400 mg is given once daily for 5 days.
• In Community Acquired Pneumonia: Raspelocin 400 mg is given once daily for 7-14 days.
• In Uncomplicated Skin & Skin Structure infections: Raspelocin 400 mg is given once daily for 7 days.
• In Complicated Skin & Skin Structure infections: Raspelocin 400 mg is given once daily for 7-21 days.
• In Complicated Intra-Abdominal infections: Raspelocin 400 mg is given once daily for 5-14 days.

Raspelocin 400 mg IV infusion can be administered intravenously for the entire treatment duration. Alternatively, therapy may be initial intravenous administration, followed by oral administration when clinically indicated. The recommended duration of treatment for the indication being treated should not be exceeded. The solution for infusion should be infused intravenously over 60 minutes.

Side Effects

The following one or more side effects may be observed: tendinopathy and tendon rupture, QT prolongation, hypersensitivity reactions, Clostridium difficile-associated diarrhea, peripheral neuropathy, photosensitivity, phototoxicity etc.

Toxicity

Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.

Precaution

Raspelocin should be discontinued at the first appearance of a skin rash or any other sign of hypersensitivity. Raspelocin should be discontinued if the patient experiences pain, swelling, inflammation or rupture of a tendon.

Interaction

No quinolone should be co-administered with any solution containing multivalent cations (e.g. magnesium) through the same intravenous line. Antacids, iron and adsorbents reduce absorption of Raspelocin. NSAID may increase the risk of CNS stimulation. Warfarin may increase the risk of bleeding.

Food Interaction

• Drink plenty of fluids.
• Take with or without food.

Raspelocin 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

Moderate: aspirin, aspirin, aspirin, celecoxib, albuterol / ipratropium, budesonide / formoterolUnknown: amoxicillin / clavulanate, diphenhydramine, ubiquinone, duloxetine, omega-3 polyunsaturated fatty acids, furosemide, atorvastatin, metoprolol, acetaminophen, acetaminophen, cyanocobalamin, pyridoxine, ascorbic acid, cholecalciferol

Disease Interaction

Major: colitis, liver disease, CNS disorders, myasthenia gravis, peripheral neuropathy, QT interval prolongation, tendonitisModerate: crystalluria, diabetes

Volume of Distribution

• 1.7 to 2.7 L/kg

Elimination Route

Well absorbed from the gastrointestinal tract. Absolute oral bioavailability is approximately 90%. Food has little effect on absorption.

Half Life

11.5-15.6 hours (single dose, oral)

Clearance

• 12 +/- 2 L/hr

Elimination Route

Approximately 45% of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~20% in urine and ~25% in feces).

Pregnancy & Breastfeeding use

Pregnancy Category C. Raspelocin is not recommended during pregnancy & lactation.

Contraindication

Raspelocin is contraindicated in persons with a history of hypersensitivity to Raspelocin or any member of the quinolone class of antimicrobial agents and any component of this formulation.

Special Warning

Elderly: No adjustment of dosage is required in the elderly.

Children: Efficacy and safety of Raspelocin IV infusion in children and adolescent have not been established.

Acute Overdose

In the events of an acute overdose, the stomach should be emptied. The patient should be kept under observation and appropriate hydration should be maintained.

Storage Condition

Store between 15 to 30° C. Protect from light and moisture. Keep away from reach of children.

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