Voxatic

Voxatic

levofloxacin

Manufacturer:

Coronet
Full Prescribing Info
Contents
Levofloxacin.
Description
Levofloxacin hemihydrate equal to Levofloxacin 500 mg.
Levofloxacin is an optical isomer of S-(-) of ofloxacin. It has broad spectrum antibacterial effects. Levofloxacin is active against gram-positive and gram-negative bacteria including anaerobic bacteria.
Furthermore, levofloxacin exhibits antibacterial activity against Chlamydia pneumoniae and Mycoplasma pneumoniae. Levofloxacin is bactericidal at a concentration equal to or slightly greater than its inhibitory concentration.
Action
Pharmacology: The main mechanism of action of levofloxacin is through inhibition of DNA-gyrase, the type of topoisomerase. This results in inhibition of bacterial DNA replication and transcription processes.
Pharmacokinetics: Concomitant administration with food has little effect on levofloxacin absorption. Levofloxacin is widely distributed to all parts of the body with high concentrations. Levofloxacin is also well penetrated into lung tissue. The concentration in lung tissue is 2 to 5 times greater than the plasma concentration.
Levofloxacin is metabolized in a very small portion, metabolites turns into desmethyl-levofloxacin and levofloxacin N-oxide. The metabolite amounts to <5% of the dose excreted in the urine.
Primary excretion is done through the kidney canal (>85% of given dose). The clearance of levofloxacin is reduced and the plasma elimination half-life is extended in patients with impaired renal function (CrCl ≤80 mL/min), it is necessary to adjust the dose to these patients to avoid drug accumulation. Most of these drugs are not metabolized in the body. Approximately 85% of the doses administered excreted through urine without changes its form.
Indications/Uses
Levofloxacin is indicated as a treatment for adult (≥18 yo) with mild, moderate to severe infection caused by susceptible bacteria.
Acute bacterial sinusitis caused by Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis.
Acute exacerbation from chronic bronchitis caused by Streptococcus aureus, Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis.
Nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus, Pseudomonas aeruginosa, Serratia marcescens, Eschericia coli, Klebsiella pneumoniae, Haemophilus influenzae or Streptococcus pneumoniae. Additional therapy should be performed if there is clinical indication. Pseudomonas aeruginosa is considered as pathogenic bacteria, it is recommended to combine anti-pseudomonas therapy with beta-lactam groups.
Pneumonia community acquired caused by methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae, Legionella pneumophilla, or Mycoplasma pneumoniae.
Multi Drug Resistant (MDR) Streptococcus pneumoniae which is isolated from strains of bacteria resistant to 2 or more of the following antibiotics: penicillin, second generation of cephalosporins such as cefuroxime, tetracycline, macrolide, and trimethoprim/sulfamethoxazole.
Chronic bacterial prostatitis caused by Eschericia coli, Enterococcus faecalis, or Staphylococcus epidermidis.
Complicated skin infections; Complicated urinary tract infection; Acute pyelonephritis.
Dosage/Direction for Use
General dose of levofloxacin tablets: 250 mg or 500 mg every 24 hours orally, which is indicated for the infection mentioned in the following dosage table. The oral dose should be given at least 2 hours before or 2 hours after administration of antacids contains magnesium, aluminum, sucralfate, metal cations such as iron, and multivitamins with zinc or didanosine. (See Table 1 & 2.)


Click on icon to see table/diagram/image




Click on icon to see table/diagram/image

Overdosage
Symptoms: The most important symptoms of acute levofloxacin overdose are the occurrence of central nervous system disturbances such as confusion, dizziness, consciousness, and convulsions, QT interval elevation and gastrointestinal disturbances such as nausea and mucosal erosion.
Treatment: In case of overdose, symptomatic treatment should be performed. Perform ECG monitoring, because of the possibility of QT intervals prolongation. Antacids can be used to protect gastric mucosa. Hemodialysis including peritoneal dialysis and CAPD is not effective to remove levofloxacin. There is no specific antidote.
Contraindications
Intolerance to class of fluoroquinolones, QTc prolongation, pregnancy.
Patients with epilepsy.
Patients with medical history of tendon impairment due to fluoroquinolone usage.
Children and adolescents in their growth period (<18 yo).
Women in pregnancy and lactation.
Special Precautions
Methicillin Resistant Staphylococcus Aureus (MRSA): Levofloxacin is not effective against infection that caused by MRSA. In infections suspected of being caused by MRSA, levofloxacin should be combined with other drugs to treat the infection.
Tendinitis and tendon crack: Tendinitis may be rare. This most often involves Achilles tendon and may cause tendon cracking. The risk of tendinitis and tendon cracking is elevated in elderly patients and patients taking corticosteroids. Close monitoring for patients who are receiving levofloxacin should be performed. Patients should consult a physician if they have symptoms of tendinitis.
If tendinitis is suspected, discontinue levofloxacin therapy immediately, and do appropriate treatment (such as immobilization) especially in the affected tendon.
Clostridium difficile-related disease: Diarrhea, especially in severe, persistent and/or bleeding diarrhea, during or after treatment with levofloxacin, it may be the symptoms of Clostridium difficile-related disease, the most severe form of the disease is enterocolitis pseudomembrane. If enterocolitis pseudomembrane is suspected, discontinue levofloxacin therapy immediately, and patients should be treated with supportive measures and specific therapy immediately (eg. oral metronidazole or vancomycin). All products those are known as peristaltic inhibitor are contraindicated in clinical situations.
Pseudomembrane colitis has been reported in almost all antibacteries including levofloxacin with mild to life-threatening severity. Therefore, it is important to consider the diagnosis to provide other antibacterial in patients with diarrhea.
Treatment with antibacterial may alters the normal flora of the colon and causes excess growth of Clostridia. Studies show that toxins produced by Clostridium difficile are the main causes of antibiotics associated with colitis.
After diagnosis of pseudomembranous colitis, treatment steps should be initiated. Mild cases of colic pseudomembranes usually can be stopped by discontinuation of the drug alone. In moderate to severe cases, other considerations should be made to overcome it with the administration of electrolyte fluids, protein supplements and effective antibacterial treatment against colitis that caused by Clostridium difficile.
Patients who are prone to seizures/convulsion: Tablets of levofloxacin contraindicated in patients with a history of epilepsy such as other quinolones, should be used with extreme caution in patients with impaired central nervous system, treatment is administered in conjunction with the same non-steroidal fenbufen and anti-inflammatory drugs or medications that lower the brain seizure threshold, such as theophylline.
Patients with dehydrogenase G-6-phosphate deficiency: Patients with latent or actual defects in glucose-6-phosphate dehydrogenase may be susceptible to hemolytic reactions when receiving treatment with quinolone antibacterials, and levofloxacin should be used with full caution.
Patients with renal impairment: Levofloxacin administration in patients with renal impairment should be very careful. Clinical observations and appropriate laboratory studies should be performed before and during therapy since levofloxacin elimination can be reduced. In patients with renal impairment (CrCl <80 mL/min), dose adjustment should be done to avoid levofloxacin accumulation due to clearance reduction.
Hypersensitivity reaction: Levofloxacin may cause fatal hypersensitivity reactions (such as angioedema to anaphylactic shock), sometimes after an initial dose administration. The therapy should be discontinued and contact the doctor to provide medical treatment immediately.
Serious acute hypersensitivity reactions may require treatment with epinephrine and other resuscitation measures, including oxygen, intravenous fluids, antihistamines, corticosteroids, amines, and airways management if it is clinically indicated.
Hypoglycemia: Like the other quinolones, blood glucose disorders, including symptomatic hyper and hypoglycemia, have been reported after diabetic patients receive drug therapy in conjunction with oral anti-hypoglycemic drugs (such as gliburide/glibenclamide) or with insulin.
Prevention of photosensitization: The therapy should be discontinued in case of phototoxicity happen (such as skin eruption).
Patients treated with vitamin K antagonists: Monitor coagulation test for co-administration levofloxacin and vitamin K antagonists (such as warfarin).
Psychotic reaction: Psychotic reaction has been reported in patients who received quinolones, including levofloxacin. In a very rare case, self-harmed psychotic reaction including suicidal thoughts and action could be happened after single dose administration. Administration of levofloxacin in patients with a history of psychiatric illness should be highly regarded.
Cardiac disorder: Caution should be seriously taken when using fluoroquinolone, including levofloxacin, in patients with known risk factors for prolonged QT interval for example: Built-in prolonged QT syndrome; Concomitant use with drugs known to prolong QT interval (such as class IA and III of anti-arrhythmia drugs, tricyclic antidepressants, macrolides); Undetectable electrolytes imbalance (such as hypokalemia, hypomagnesemia); Elderly; Cardiac disease; Peripheral neuropathy; Opiates; Liver function failure: Cases of liver necrosis to life-threatening liver failure have been reported in the use of levofloxacin, especially in patients with severe disease, such as sepsis.
The side effects may impair the ability to drive or operate machine.
Use In Pregnancy & Lactation
Fluoroquinolones are contraindicated to women who are in pregnancy and lactation.
Adverse Reactions
Vomit, bloated, headache, dizziness, insomnia, shiver.
Rare: Tendon cracking, arthralgia (the symptoms can be cure), QT prolongation.
Heart disorders: Rare: Tachycardia; Unknown frequency: Arrhythmia ventricular and torsade de pointes (dominated by the patients with QT prolongation risk factor), electrocardiogram QT prolonged.
Lymphatic and blood system disorders: Uncommon: Leukopenia, eosinophilia; Rare: Thrombocytopenia, neutropenia; Very rare: Agranulocytosis; Unknown frequency: Pancytopenia, hemolytic anemia.
CNS disorders: Uncommon: Dizziness, headache, drowsiness; Rare: Convulsion, tremor, paresthesia; Very rare: Sensory or sensorimotor peripheral neuropathy, dysgeusia including agesia, parosmia including anosmia.
Eye disorders: Very rare: Vision disorder.
Hearing impairment and labyrinth disorder: Uncommon: Vertigo; Very rare: Hearing impairment; Unknown: Tinnitus.
Respiratory disorder: Rare: Bronchospasm, dyspnea; Very rare: Pneumonitis allergic.
Gastrointestinal tract disorder: Common: Diarrhea, nausea; Uncommon: Vomit, abdominal pain, dyspepsia, bloated, constipated; Rare: In a very rare case, hemorrhagic diarrhea may show an indication of enterocolitis including pseudomembrane colitis.
Renal function and urinary tract disorder: Uncommon: Blood creatinine elevation; Rare: Acute renal failure (due to interstitials nephritis).
Skin and subcutaneous tissue disorder: Uncommon: Rash, pruritus; Rare: Urticaria; Very rare: Angioneurotic edema, photosensitivity reaction; Unknown: Toxic epidermal necrolysis, Steven-Johnson syndrome, multiforme erythema, hyperhidrosis, sometimes Mucocutaneous reaction might happen even after first dose administration.
Musculoskeletal and connective tissue disorders: Rare: Tendon disorder including tendinitis (Achilles tendon), arthralgia, myalgia; Very rare: Tendon rupture. The side effects may be happened in 48 hours and act bilaterally, may cause muscle weakness, especially to the patient with myasthenia gravis; Unknown: Rhabdomyolysis.
Metabolism and nutrition disorder: Uncommon: Anorexia; Very rare: Hypoglycemia, especially to patient with diabetes.
Infection and infestation: Uncommon: Fungal infection.
Vascular disorder: Rare: Hypotension.
Common disorder: Uncommon: Asthenia; Very rare: Pyrexia; Unknown: Pain (including back pain, neck pain and extremities pain).
Immune system disorder: Very rare: Anaphylactic shock.
Anaphylactic reaction or anaphylactoid might be perform even after the first administration; Unknown: Hypersensitivity.
Liver function disorder: Common: Increased bilirubin; Very rare: Hepatitis; Unknown: Jaundice and severe liver injury, including acute liver failure, which can be happened by consuming levofloxacin especially in patient with severe illness.
Mental disorder: Uncommon: Insomnia, nervousness; Rare: Psychotic disorder, depression, confusion state, agitation, anxious; Very rare: Self-harmed psychotic reaction including suicidal thoughts and action, hallucination.
Another adverse reaction related with fluoroquinolone usage: Extrapyramidal symptoms and another muscle tissues disorder, hypersensitive vasculitis, Porphyria attacks in patients with porphyria.
Drug Interactions
Iron salt, antacids containing magnesium or aluminum: Levofloxacin has the potential to form stable co-ordinate compounds with some metals (Al, Cu, Zn, Mg, Ca). Antacids those are containing aluminum or magnesium and iron-containing drugs may reduce the absorption of levofloxacin. The administration of these drugs is recommended at least two hours before or after levofloxacin administration.
Sucralfate: Concomitant use with sucralfate may significantly reduce the bioavailability of levofloxacin. The administration of these drugs is recommended at least two hours after levofloxacin administration.
Theophylline, phenbufen, or NSAIDs: Pharmacokinetics interaction has not found between levofloxacin and theophylline. However, brain seizure threshold reduction may occur when quinolones is administered with theophylline, NSAIDs or other drugs that may reduce the seizure threshold.
The levels of levofloxacin will be approximately 13% higher in concomitant administration with phenbufen than its administration as a solo therapy.
Probenecid and cimetidine: Probenecid and cimetidine have statistically significant effects on levofloxacin elimination. The clearance of levofloxacin was reduced by cimetidine (24%) and probenecid (34%), because these drugs are able to hold levofloxacin secretion in renal tubular. Attention should be given when levofloxacin is used in conjunction with drugs that have a renal tubular secretory effect such as probenecid and cimetidine, especially in patients with renal function impairment.
Levofloxacin effect in other products: Cyclosporine: Concomitant use of levofloxacin and cyclosporine may elevate cyclosporine's half-time to 33%.
Vitamin K antagonists: Increased coagulation testing and/or bleeding has been reported in patients who treated with levofloxacin in combination with vitamin K antagonists (such as warfarin). Therefore, the coagulation tests need to be closely monitored in patients who also receive vitamin K antagonists therapy.
Drugs that known to cause QT interval prolongation.
Further attention is needed in levofloxacin administration to the patients who also received the drugs that known to cause QT interval prolongation (such as Class IA and III of anti-arrhythmia, anti-depressants tricyclic, macrolides, antipsychotic).
Interactions with food: There are no relevant interactions between levofloxacin and food.
The other relevant information: Levofloxacin is not affected to use concomitantly with: Calcium carbonate; Digoxin; Glibenclamide; Ranitidine.
Storage
Store below 30°C. Protected from light exposure and in a tight sealed container.
MIMS Class
ATC Classification
J01MA12 - levofloxacin ; Belongs to the class of fluoroquinolones. Used in the systemic treatment of infections.
Presentation/Packing
FC tab 500 mg x 1 x 10's.
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