Levofloxacin hemihydrate.
Each film-coated tablet contains: Levofloxacin (as hemihydrate) 512.45 mg.
(Equivalent to Levofloxacin 500 mg).
Levofloxacin (Winaflox) 500 mg Film-Coated Tablet is a white to off-white, oval, bisected, film-coated tablet.
Pharmacology: Pharmacodynamics and Pharmacokinetics: Levofloxacin is the L-isomer of the racemate, ofloxacin, a quinolone antibacterial agent. The mechanism of action of levofloxacin and other quinolones involves inhibition of bacterial topoisomerase II (DNA gyrase) and topoisomerase IV enzymes which are essential for DNA replication, transcription, repair, and recombination.
Levofloxacin is rapidly and almost completely absorbed following oral administration with peak plasma concentration achieved within an hour of a dose. It is distributed into body tissues including the bronchial mucosa and lungs, but penetration into CSF is relatively poor. Levofloxacin is approximately 30% to 40% bound to plasma proteins. It is only metabolized to a small degree to inactive metabolites. The elimination half-life of levofloxacin is 6 to 8 hours, although this may be prolonged in patients with renal impairment.
Levofloxacin is excreted largely unchanged, primarily in the urine. It is not removed by hemodialysis or peritoneal dialysis.
Levofloxacin is a fluoroquinolone antibacterial with a wider spectrum of activity. It has been used in the treatment of a wide range of infections including lower respiratory tract infections, skin infections, typhoid and paratyphoid fever and urinary tract infections. Levofloxacin is also used in the prophylaxis of meningococcal meningitis and for surgical infections.
Usual adult dose: 250 mg to 500 mg once or twice daily for 7 to 14 days.
Doses should be reduced in patients with renal impairment. Or as prescribed by the physician.
Clinical features of acute overdosage of levofloxacin may include CNS symptoms such as confusion, dizziness, impairment of consciousness, and convulsive seizures, as well as GI reactions such as nausea and mucosal erosions.
In the event of overdose, symptomatic treatment should be implemented. The patient should be observed and proper hydration maintained. ECG monitoring should be undertaken, because of the possibility of QT interval prolongation.
The administration of activated charcoal as soon as possible after oral overdose may prevent excessive increase of systemic levofloxacin exposure. Antacids may be used for protection of the gastric mucosa.
Hemodialysis, including peritoneal dialysis and CAPD, are not effective in removing levofloxacin from the body. No specific antidote exists.
Levofloxacin should not be used in children, adolescents, pregnant women, or breastfeeding mothers.
Levofloxacin should be used with caution in patients with epilepsy or history of CNS disorders.
Care is necessary in patients with impaired hepatic or renal function, glucose-6-phosphate dehydrogenase deficiency, or myasthenia gravis. An adequate fluid intake should be maintained during treatment to avoid excessive alkalinity of urine because of the risk of crystalluria. Exposure to strong sunlight should also be avoided. The ability to drive or operate machinery may be impaired especially when alcohol is also taken.
Tendon damage may occur and treatment should be discontinued if patients experience tendon pain, inflammation or rupture.
Levofloxacin should also be avoided in methicillin-resistant Staphylococcus aureus infection because of high level of resistance.
Levofloxacin should not be used in patients at increased risk unless there are no other treatment available. Patient at increased risk include those with a history of blockages or aneurysm (abnormal bulges) of the aorta or other blood vessels, high blood pressure, certain genetic disorders involving blood vessels (i.e. Marfan syndrome and Ehlers-Danlos syndrome), and the elderly. Fluoroquinolones can increase the occurrence of serious aortic ruptures which may result to hemorrhage or death. Patients should seek immediate medical treatment for any symptoms associated with aortic aneurysm i.e. throbbing pain in the stomach area, deep pain in back or side of the stomach, pain in the jaw, neck, back or chest, coughing or hoarseness and shortness of breath, trouble breathing or swallowing. Stop fluoroquinolone treatment immediately if a patient reports side effects suggestive of aortic aneurysm or dissection.
Pregnancy: (Pregnancy Category C). There are no adequate and well-controlled studies using levofloxacin in pregnant women. Since levofloxacin, as with most other fluoroquinolones, causes arthropathy in immature animals, the drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Levofloxacin has not been measured in human milk. However, based on the ofloxacin data, it can be presumed that levofloxacin will be excreted in human milk. Therefore, a decision should be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the drug to the mother as well as possible serious adverse effect to the infant.
Adverse effects are usually mild and transient. Gastrointestinal disturbances include nausea, vomiting, diarrhea, abdominal pain and dyspepsia are the most frequent adverse effects.
Headache, dizziness, and restlessness are among the most common effects on the CNS.
In addition to rash and pruritus, hypersensitivity-type reactions affecting the skin have included, rarely, vasculitis, erythema multiforme, Stevens-Johnson Syndrome, and toxic epidermal necrolysis.
Fluoroquinolone use has been reported to cause visual disturbance associated with bilateral uveitis.
Chelation Agents: Antacids, Sucralfate, Didanosine, Metal Cations, Multivitamins: Concomitant administration of levofloxacin tablets with antacids containing calcium, magnesium, or aluminum, as well as sucralfate, didanosine, metal cations such as iron, and multivitamin preparations with zinc, or any products containing any of these components may interfere with the GI 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 therapy.
Anti-arrhythmic Agents: Levofloxacin should be avoided in patients receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents because of potential pharmacologic interaction (additive effect on QT interval prolongation).
Antidepressants: Potential pharmacologic interaction with fluoxetine or imipramine (additive effect on QT interval prolongation).
Antidiabetic Agents: Disturbances of blood glucose, including hyperglycemia and hypoglycemia, have been reported in patients treated concomitantly with quinolones and antidiabetic agent. Careful monitoring of blood glucose is recommended when these agents are co-administered.
Ciclosporin and Tacrolimus: Possible pharmacokinetic interactions with ciclosporin or tacrolimus (increased AUC of the immunosuppressive agent). Although no dosage adjustment is necessary, monitoring of plasma concentrations of the immunosuppressive agent is recommended during concomitant therapy.
Corticosteroids: Risk of tendon rupture during treatment with levofloxacin may be increased in patients receiving corticosteroids, particularly in elderly patients.
Digoxin: There are no significant effects noted during concomitant therapy therefore, no dosage adjustment is required.
Fluconazole: Both levofloxacin and fluconazole can prolong the QT interval. The simultaneous use of IV levofloxacin and fluconazole resulted in an episode of torsades de pointes in patient on hemodialysis.
Non-steroidal anti-inflammatory drugs (NSAIDs): Concomitant administration of an NSAID with a quinolone including levofloxacin, may increase the risk of CNS stimulation and convulsive seizures.
Probenecid and Cimetidine: Potential pharmacokinetic interaction (increased levofloxacin AUC and t1/2) - not considered clinically important; dosage adjustments are not required.
Theophylline: Concomitant administration of other quinolones with theophylline has resulted in prolonged elimination t1/2 elevated serum theophylline levels, and a subsequent increase in the risk of theophylline-related adverse reactions. Closely monitor serum theophylline levels and adjust theophylline dosage accordingly; consider that adverse theophylline effects (e.g., seizures) may occur with or without elevated theophylline concentrations.
Warfarin: There have been reports of enhanced effects of warfarin when co-administered with levofloxacin. Therefore, prothrombin time, International Normalized Ratio (INR), or other suitable anticoagulation tests should be closely monitored if levofloxacin is administered concomitantly. Patient should also be monitored for evidence of bleeding.
Zidovudine: Levofloxacin absorption and disposition in HIV-infected subjects, with or without concomitant zidovudine treatment, were similar. The effect of levofloxacin on zidovudine pharmacokinetics has not been studied. No dosage adjustment for levofloxacin appears to be required when co-administered with zidovudine.
Store at temperatures not exceeding 30°C.
J01MA12 - levofloxacin ; Belongs to the class of fluoroquinolones. Used in the systemic treatment of infections.
Winaflox FC tab 500 mg
30's
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