KOBUNDO LEVOQUIN Levofloxacin Tablets 500 mg
Description, Composition, Action, Absorption, Distribution, Metabolism, Elimination, Adverse effects, Contraindications, Interactions, Indications, Dosage, Presentation, Manufacturer and Marketer of Levoquin Tablet Medicine for Infections.
LEVOQUIN (levofloxacin) is a synthetic broad spectrum antibacterial agent for oral and intravermus administration. Chemically, levofloxacin, a chiral fluorinated carboxyquinolone, is the pure (-)-(S)-enantiomer of the racemic drug substance ofloxacin.
Each film coated tablet contains:
Levofloxacin Hemihydrate equivalent to Levofloxacin 250/500 Mg
All Flouoroquinolones and Quinolones act by inhibiting bacterial DNA gyrase enzyme which is required for DNA replication and thus cause bacterial lysis.
Absorption: Levofloxacin is rapidly and essentially completely absorbed after oral administration. Peak plasma concentrations are usually attained one to two hours after oral dosing. The absolute bioavailability of levofloxacin tablet is approximately 99%, demonstrating complete oral absorption of levofloxacin. Oral administration of 500 mg LEVOQUIN with food prolongs the time to peak concentration by approximately 1 hour and decreases the peak concentration by approximately 14% following tablet.
Distribution: The mean volume of distribution of levofloxacin generally ranges from 74 to 112 L after single and multiple doses, indicating widespread distribution into body tissues. Levofloxacin reaches its peak levels in skin tissues and in blister fluid of healthy subjects at approximately 3 hours after dosing to healthy subjects. Levofloxacin also penetrates well into lung tissues. Lung tissue concentrations were generally 2- to 5-fold higher than plasma concentrations and ranged from approximately 2.4 to 11.3 µg/g over a 24-hour period after a single 500 mg oral dose.
Metabolism: Levofloxacin undergoes limited metabolism in humans and is primarily excreted as unchanged drug in the urine. Following oral administration, approximately 87% of an administered dose was recovered as unchanged drug in urine within 48 hours, whereas less than 4% of the dose was recovered in feces in 72 hours. Less than 5% of an administered dose was recovered in the urine as the desmethyl and N- oxide metabolites, the only metabolites identified in humans. These metabolites have little relevant pharmacological activity.
Elimination: Levofloxacin is excreted largely as unchanged drug in the urine. The mean terminal plasma elimination half-life of levofloxacin ranges from approximately 6 to 8 hours following single or multiple doses of levofloxacin given orally. The mean apparent total body clearance and renal clearance range from approximately 144 to 226 mL/min and 96 to 142 mL/min, respectively. No levofloxacin crystals were found in any of the urine samples freshly collected from subjects receiving levofloxacin.
1% to 10%:
Central nervous system: Dizziness, headache, insomnia
Gastrointestinal: Nausea, vomiting, diarrhea, constipation
Neuromuscular & skeletal: Tremor, arthralgia
<1% (Limited to important or life-threatening symptoms): Cardiac failure, hypertension, bradycardia, tachycardia, seizures, elevated transaminases, pseudomembraneous colitis, leukorrhea, granulocytopenia, leukopenia, leukocytosis, thrombocytopenia, jaundice, acute renal failure, arrhythmia (torsade de pointes).
Hypersensitivity to levofloxacin, any component, or other quinolones; pregnancy, lactation.
Severe pneumococcal pneumonia. Nosocomial infections with pseudomonas aeruginosa – consider combination therapy, tendinitis, Hypotension, Excessive sunlight.
Antacids, Sucralfate, Metal Cations, Multivitamins
LEVOQUIN Tablets: While the chelation by divalent cations is less marked than with other quinolones, concurrent administration of LEVOQUIN Tablets with antacids containing magnesium, or aluminum, as well as sucralfate, metal cations such as iron, and multivitamin preparations with zinc may interfere with the gastrointestinal absorption of levofloxacin, resulting in systemic levels considerably lower than desired. Tablets with antacids containing magnesium, aluminum, as well as sucralfate, metal cations such as iron, and multivitamins preparations with zinc or didanosine may, substantially interfere with the gastrointestinal absorption of levofloxacin, resulting in systemic levels considerably lower than desired. These agents should be taken at least two hours before or two hours after levofloxacin administration.
Theophylline, Warfarin, Cyclosporine, Digoxin, Probenecid and Cimetidine
No significant effect of levofloxacin on the plasma concentrations, AUC, and other disposition parameters for all above drugs were detected.
LEVOQUIN should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Acute maxillary sinusitis due to S. pneumoniae, H. influenzae, or M.catarrhalis; uncomplicated urinary tract infection due to E. coli, K. pneumoniae, or S. saprophyticus; also for acute bacterial exacerbation of chronic bronchitis and community-acquired pneumonia due to S. aureus, S. pneumoniae (including penicillin-resistant strains), H. influenzae, H. parainfluenzae, or M. catarrhalis, C. pneumoniae, L. pneumophila, or M. pneumoniae; may be used for uncomplicated.
Community acquired pneumonia: 5Oomg every 24 hours for 7 – 14 days.
Acute maxillary sinusitis: 500 mg every 24 hours for 10 – 14 days.
Uncomplicated skin infections: 500mg every 24 hours for 7 – 10 days.
Uncomplicated urinary tract infections: 250mg once daily for 3 days.
Complicated urinary tract infections include acute pyelonephritis: 250mg every 24 hours for 10 days.
2 x 7 TABLETS IN A ALU-ALU BLISTER PACK
Manufactured in India by
LABORATORIES PVT LTD.
C-1B, 305/2 & 3, G.I.D.C. Kerala (Bavla),
Dist.: Ahmedabad-382 220, Gujarat.
KOBUNDO PHARMACEUTICALS NIG.LTD.
330 Port Harcourt Rd., Aba, Abia State,