Veflox

500 mg: Pale yellowish-white, oblong, biconvex, one-side scored, with letter "VF" and "500" on the scored side and the letters "Rx" on the other.
1 film-coated tablet contains Levofloxacin 500 mg.
750 mg: Pinkish orange, oblong, biconvex film-coated tablet. One side has incision, letter "VF" and "750" on each side. Another side has the letter "Rx".
Each film-coated tablet contains Levofloxacin hemihydrate 768.96 mg equivalent to Levofloxacin 750.00 mg.

Pharmacology: Pharmacodynamics: Mechanism of action: Levofloxacin inhibits DNA-gyrase in susceptible organisms thereby inhibits relaxation of the supercoiled DNA and promotes breakage of DNA standards. DNA gyrase (topoisomerase II), is an essential bacterial enzyme that maintains the superhelical structure of DNA and is required for DNA replication and transcription, DNA repair, recombination, and transposition.
500 mg: Levofloxacin has been shown to be active against various strains of microorganisms in clinical infections as described in Indications/Uses.
Pharmacokinetics: Absorption: Levofloxacin is rapidly absorbed from the GI tract and absolute bioavailability is approximately 99%. Peak plasma concentrations are usually attained 1-2 hours after oral dose; steady state plasma concentrations are attained within 48 hours with once-daily regimens.
Distribution: Levofloxacin is approximately 24% to 38% bound to serum proteins primarily albumin.
500 mg: The mean volume of distribution of levofloxacin generally ranges from 74 to 112 L; CSF concentrations ~15% of serum levels; high concentrations are achieved in prostate, lung, and gynecological tissues, sinus, saliva.
750 mg: Levofloxacin is widely distributed into body tissues and fluids, including skin, blister fluid, and lungs. Levofloxacin is distributed into cerebrospinal fluid (CSF). The drug is distributed into milk following oral administration.
Metabolism: 500 mg: Levofloxacin is minimally metabolized by liver.
750 mg: Levofloxacin undergoes limited metabolism to inactive metabolites. The drug is not metabolized by cytochrome P-450 (CYP) isoenzymes.
Excretion: Levofloxacin is eliminated principally as unchanged drug in urine by glomerular filtration and active tubular secretion. The terminal elimination half-life of levofloxacin is approximately 6-8 hours after oral administration.
500 mg: Approximately 87% of an oral dose is eliminated in urine within 48 hours, whereas less than 4% of dose was recovered in feces in 72 hours. Less than 5% of an administered dose was recovered in urine as the metabolites.
750 mg: Approximately 87% of an oral dose is eliminated in urine and less than 4% is eliminated in feces.

Veflox is indicated for the treatment of adults with mild, moderate, and severe infections caused by susceptible strains of the designated microorganisms in the conditions listed as follows.
Acute sinusitis due to Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis.
Acute exacerbation of chronic bronchitis due to Staphylococus aureus, Streptococcus pneumoniae, Haemophilus influenzae, Haemophillus parainfluenzae or Moraxella catarrhalis.
Community-acquired pneumonia due to Staphylococcus aureus, Streptococcus pneumoniae (including penicillin-resistant strains), Haemophilus influenzae, Heamophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pheumoniae, Legionella pneumophila or Mycoplasma pneumoniae.
Nosocomial pneumonia due to methicillin-susceptible Staphylococcus aureus, Pseudomonas aeruginosa, Serratia marcescens, Escherichia coli, Klebsiella pneumoniae, Haemophilus influenzae, or Streptococcus pneumoniae. Adjunctive therapy should be used as clinically indicated. Where Pseudomonas aeruginosa is a documented or presumptive pathogen, combination therapy with an anti-pseudomonal β-lactam is recommended.
Uncomplicated skin and skin structure infections (mild to moderate) including abscesses, cellulitis, furuncles, impetigo, pyoderma, wound infections due to Staphylococcus aureus and Streptococcus pyogenes.
Complicated skin and skin structure infections due to methicillin-susceptible Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes or Proteus mirabilis.
Complicated urinary tract infections due to Enterococcus faecalis, Enterobacter cloacae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa or Staphylococcus saprophyticus.
Chronic bacterial prostatitis due to Escherichia coli, Enterococcus faecalis, or Staphylococcus epidermidis.
Acute pyelonephritis caused by Escherichia coli.
750 mg: Empirical treatment for community acquired pneumonia most likely caused by organisms susceptible to levofloxacin.
Third-line therapy for Helicobacter pylori Infection: Levofloxacin-based Triple Therapy: Levofloxacin, in combination with other antimicrobial agent and proton pump inhibitor as triple therapy, is indicated for the treatment of patients with gastric ulcer caused by Helicobacter pylori infection and duodenal ulcer disease.

Recommended Dose: 500 mg: See Table 1.

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750 mg: For empirical treatment for community-acquired pneumonia: 750 mg once daily. (See Table 2.)

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When only the serum creatinine is known, the following formula may be used to estimate creatinine clearance: see equation.

Click on icon to see table/diagram/image

The serum creatinine should represent a state of renal function.
Patients with impaired liver function: No adjustment of dosage is required since levofloxacin is not metabolized to any relevant extent by liver and is mainly excreted by kidneys.
Elderly patient: No adjustment of dosage is required in the elderly, other than that imposed by consideration of renal function.
Mode of Administration: Levofloxacin is administered orally without regard to meals. Patients receiving oral levofloxacin should be well hydrated and instructed to drink fluids liberally to prevent highly concentrated urine and formation of crystals in urine. Levofloxacin should be administered orally at least 2 hours before or 2 hours after antacids containing magnesium or aluminum, metal cations (e.g., iron), sucralfate, multivitamins or dietary supplements containing iron or zinc, or buffered didanosine (pediatric oral solution admixed with antacid). These drugs may interfere with oral absorption of levofloxacin, resulting in subtherapeutic systemic concentrations of the quinolone.

500 mg: Symptoms include acute renal failure and seizures. Treatment should include GI decontamination and supportive care. Levofloxacin cannot be removed by peritoneal or hemodialysis.
750 mg: Overdose and Treatment: According to toxicity studies in animals, the most important signs to be expected following acute overdosage of Levofloxacin 750 mg are central nervous system symptoms such as confusion, dizziness, impairment of consciousness, and convulsive seizures, as well as gastrointestinal reactions such as nausea and mucosal erosions.
In the event of an acute overdosage, the stomach should be emptied. Antacid may be used for protection of gastric mucosa. No specific antidote exists. The patient should be observed and appropriate hydration maintained. Levofloxacin is not efficiently removed by hemodialysis or peritoneal dialysis.

Levofloxacin is contraindicated in patients with known hypersensitivity to levofloxacin or other quinolones.

500 mg: Do not use in patients who are hypersensitive to levofloxacin or any other quinolone antimicrobial agents.
If skin rash, or muscle pain or tendon pain (e.g. at the wrist or ankle) occurs, discontinue levofloxacin and consult a physician immediately.
Levofloxacin could be harmful to the liver and kidneys.
Do not use, or if necessary, use with special precaution in patients with CNS disorder that predispose to seizures in a dose related manner.
Levofloxacin may prolong the QT interval therefore, use with caution in patients with a history of prolonged QT interval, patients at risk to develop prolongation of the QT interval such as elderly, patients with heart diseases, especially arrhythmia, patients with hypertension and patients with uncorrected electrolyte disorders (e.g., hypokalemia) etc.
Avoid coadministration with drugs that cause prolongation of the QT interval such as antiarrhythmic class IA (e.g. quinidine, procainamide), class III (e.g. amiodarone, sotalol), cisapride, erythromycin, antipsychotics drugs, tricyclic antidepressants, etc.
Levofloxacin may cause phototoxicity reaction or a severe rash, such as Toxic Epidermal Necrolysis, Stevens-Johnson syndrome, Erythema Multiforme, etc.
Levofloxacin may affect blood sugar levels. Carefully use in diabetic patients.
Coadministration of this drug with warfarin may increase the effect of warfarin.
Use in Pregnancy & Lactation: Avoid using levofloxacin in pregnant and breast-feeding women.
Use in Children: Levofloxacin may used be for inhalational anthrax (post exposure) in adolescents and children 6 months of age or older. Safety and efficacy do not established for any other indication in this age group. There is reported that levofloxacin causes arthropathy in juvenile animals use of so, fluoroquinolones may be justified in children younger than 18 years old.
750 mg: Levofloxacin should be avoided in patients who have a history of tendon disorders or have experienced tendinitis or tendon rupture.
Levofloxacin should be avoided in patients who have experienced peripheral neuropathy.
Levofloxacin should be used with caution in patients with known or suspected CNS disorders that predispose to seizures or lower the seizure threshold (e.g., severe cerebral arteriosclerosis, epilepsy) or with other risk factors that predispose to seizures or lower the seizure threshold (e.g., certain drugs, renal impairment).
Levofloxacin should be avoided in patients with a known history myasthenia gravis. Patients should be advised to immediately contact a clinician if they experience any symptoms of muscle weakness, including respiratory difficulties.
Levofloxacin should be avoided in patients with a history of prolonged QT interval, in those with uncorrected electrolyte disorders (e.g., hypokalemia), and in those receiving class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents.

Pregnancy: Category C. Avoid using levofloxacin in pregnant and breast-feeding women.
500 mg: Levofloxacin crosses the placenta. Quinolone exposure during human pregnancy has been reported with other agents. To date, no specific teratogenic effect or increased pregnancy risk has been identified; however, because of concerns of cartilage damage in immature animals exposed to quinolones and the limited levofloxacin specific data, levofloxacin should only be used during pregnancy if a safer option is not available.
750 mg: There are no adequate and well-controlled studies of levofloxacin in pregnant women, and the drug should be used during pregnancy only if the potential benefits justify the potential risk to the fetus.
Lactation: 500 mg: Enters breast milk, not recommended.
750 mg: Levofloxacin is distributed into milk following oral administration. Because of the potential for serious adverse reactions in the infant, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the mother.

500 mg: 1% to 10%: Cardiovascular: Chest pain (1%), edema (1%).
Central nervous system: Headache (6%), insomnia (4%), dizziness (3%), fatigue (1%), pain (1%).
Dermatologic: Rash (2%), pruritus (1%).
Gastrointestinal: Nausea (7%), diarrhea (5%), constipation (3%), abdominal pain (2%), dyspepsia (2%), vomiting (2%).
Genitourinary: Vaginitis (1%).
Local: Injection site reaction (1%).
Respiratory: Pharyngitis (4%), dyspnea (1%).
Miscellaneous: Monilias (1%).
<1%: Limited to important or life-threatening: Acute renal failure, agitation, agranulocytosis; allergenic reaction (including anaphylaxis, angioedema, pneumonitis rash, pneumonitis, and serum sickness); anaphylactoid reaction, arrhythmia (including atrial/ventricular tachycardia/fibrillation and torsade de pointes), aplastic anemia, arthralgia, ascites, bradycardia, bronchospasm, carcinoma, cardiac failure, cholecystitis, cholelithiasis, confusion, depression, EEG abnormalities, encephalopathy, eosinophilia, erythema multiforme, GI hemorrhage, granulocytopenia, hallucination, heart block, hemolytic anemia, hemoptysis, hepatic failure (some fatal), hepatitis, hyper-/hypoglycemia, hyperkalemia, hyperkinesias, hyper-/hypotension, infection, INR increased, intestinal obstruction, intracranial hypertension, involuntary muscle contractions, jaundice, leukocytosis, leukopenia, leucorrhea, lymphadenopathy, MI, migraine, multiple organ failure, myalgia, nephritis (interstitial), palpitation, pancreatitis, pancytopenia, paralysis, paresthesia, peripheral neuropathy, photosentivity (<0.1%), pleural effusion, pneumonititis, postural hypotension, prothrombin time increased/decreased, pseudomembraneous colitis, psychosis, pulmonary edema, pulmonary embolism, purpura, QT_c prolongation, respiratory depression, rhabdomyolysis, seizure, skin disorder, somnolence, speech disorder, Stevens-Johnson syndrome, stupor, suicide attempt/ideation, syncope, tendonitis, tendon rupture, tongue edema, toxic epidermal necrolysis, transaminases increased, thrombocythemia, thrombocytopenia, tremor, urticaria, WBC abnormality.
750 mg: Common: Gastrointestinal: Diarrhea (5%), nausea (7%).
Neurologic: Dizziness (3%), headache (6% to 10%), insomnia (4%).
Serious: Cardiovascular: Aortic aneurysm, or dissection, cardiac arrest (0.1% to 1%), prolonged QT interval, torsades de pointes, ventricular tachycardia (0.1% to 1%).
Dermatologic: Erythema multiforme, Stevens-Johnson syndrome.
Endocrine metabolic: Hypoglycemia (0.1% to 1%).
Hematologic: Aplastic anemia, pancytopenia, thrombocytopenia purpura.
Hepatic: Hepatitis, liver failure.
Immunologic: Anaphylactoid reaction, hypersensitivity reaction (0.1% to 1%).
Musculoskeletal: Exacerbation of myasthenia gravis, rupture of tendon, tendinitis (0.1% to 1%).
Neurologic: Disorientated, disturbance of attention, Guillain-Barré syndrome, memory impairment, peripheral neuropathy, pseudotumor cerebri, raised intracranial pressure, seizure (0.1% to 1%).
Ophthalmic: Retinal detachment.
Psychiatric: Delirium, depression (0.1% to 1%), hallucinations (0.1% to 1%), paranoid disorder, psychotic disorder, suicidal.
Renal: Renal failure (0.1% to 1%).

500 mg: Antacid, Sucralfate, Metal Cations, Multivitamins: While the chelation by divalent cations is less marked than with other quinolones, concurrent administration of Veflox 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. These agents should be taken least two hours before of two hours after levofloxacin administration.
Theophylline, Non-steroidal anti-inflammatory drugs: No pharmacokinetic interactions of levofloxacin were found with theophylline in a clinical study. However there are indications of a pronounced lowering of the cerebral seizure threshold when quinolones are given concurrently with other drugs that lower the seizure threshold (e.g. theophylline) or with fenbufen or similar non-steroidal anti-inflammatory drugs.
Antidiabetic agents: Disturbances of blood glucose, including hyperglycemia and hypoglycemia, have been reported in patients treated concomitantly with quinolones and an antidiabetic agent. Therefore, careful monitoring of blood glucose is recommended when this agents are co-administered.
Anticoagulant drug (warfarin): Coadministration with warfarin has been reported that the effect of warfarin was potentiated (hepatic metabolism of warfarin may be inhibited, or free warfarin may be increased by competitive displacement from the protein binding site) and therefore prothrombin time prolonged.
750 mg: Concomitant use of levofloxacin and class IA (e.g., quinidine, procainamide) or class III (e.g., amiodarone, sotalol) antiarrhythmic agents has resulted in prolong QT interval.
Concomitant administration of levofloxacin with aluminum- or magnesium-containing antacids has resulted in decreased absorption of oral levofloxacin.
Concomitant use of levofloxacin and procainamide has resulted in increased half-life and decreased clearance of procainamide.
Concomitant use of levofloxacin and antidiabetic agents (e.g., insulin, glyburide) has resulted in altered blood glucose concentrations and symptomatic hyperglycemia or hypoglycemia.
Concomitant use of levofloxacin and corticosteroids increases the risk of severe tendon disorders (e.g., tendinitis, tendon rupture), especially in geriatric patients older than 60 years of age.
Concomitant use of levofloxacin and iron or multivitamins or mineral supplements has resulted in decreased absorption of oral levofloxacin.
Concomitant use of levofloxacin and nonsteroidal anti-inflammatory agents (NSAIAs) may increase the risk of CNS stimulation and seizures.
Concomitant use of levofloxacin and warfarin has resulted in increased prothrombin time.

Store below 30°C (at room temperature for 500 mg).

Quinolones

J01MA12 - levofloxacin ; Belongs to the class of fluoroquinolones. Used in the systemic treatment of infections.

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