PHARMACOLOGY

Pharmacotherapeutic Group: Fluoroquinolone Antibiotics

 Pharmacodynamic Properties:Levofloxacin is a fluoroquinolone which inhibits bacterial topoisomerase IV and DNA gyrase enzymes required for DNA replication, transcription, repair and recombination. It has activity against a wide range of gram-negative and gram-positive microorganisms.

 Pharmacokinetic Properties:

Absorption: Rapid and complete absorption from the GIT (oral); peak plasma concentrations within 1-2 hr.

 Distribution: Widely distributed in bronchial mucosa, lungs; CSF (relatively poor). Protein-binding: 30-40%.

Metabolism:  Levofloxacin undergoes limited metabolism in humans. 

Excretion: Mainly via urine (largely as unchanged drug); 6-8 hours (elimination half-life).

INDICATIONS

Nosocomial Pneumonia, Community Acquires pneumonia, Acute bacterial sinusitis, complicated and uncomplicated skin and skin structure infections, Chronic bacterial prostatitis, Complicated urinary tract infections, Acute pyelonephritis

 DOSAGE & ADMINISTRATION

Usual dose of levofloxacin Tablet is 250 mg, 500 mg, or 750 mg administered orally every 24 hours

 ADVERSE DRUG REACTIONS

Nausea, diarrhoea, constipation, headache, insomnia, tendon effects, hypersensitivity effects, hepatotoxicity, peripheral neuropathy

Potentially Fatal: Anaphylaxis.

 PRECAUTIONS

Tendonitis, known or suspected central nervous system (CNS) disorders (e.g. severe cerebral arteriosclerosis, epilepsy) or other risk factors that predispose to seizures. Avoid unnecessary exposure to sunlight or artificial UV light. History of prolonged QT interval, uncorrected electrolyte disturbances. Diabetes Mellitus (carefully monitor blood glucose levels). Periodically monitor renal, hepatic and haematopoietic functions during treatment. Pregnancy, lactation and elderly. May impair ability to drive or operate machinery.

 DRUG INTERACTIONS

Increased concentration of cyclosporin or tacrolimus. Reduced absorption with ferrous sulfate or dietary supplements containing zinc, calcium, magnesium or iron. May increase plasma levels of theophylline. Increased risk of tendon rupture with corticosteroids. Reduced absorption with sucralfate and antacids containing magnesium and aluminium; administer at least 2 hours before or 2 hours after antacids. Increased half-life and decreased clearance of procainamide. Altered glucose levels with antidiabetic agents (e.g. insulin, glyburide).
Potentially Fatal: Increased risks of ventricular arrhythmias with QT prolonging drugs e.g. class IA (quinidine, procainamide) or class III (amiodarone, sotalol) antiarrhythmics, fluoxetine, imipramine. Increased risk of CNS stimulation and seizures with NSAIDs. Increased prothrombin time with warfarin.

 CONTRAINDICATIONS

Contraindicated in persons with known hypersensitivity to levofloxacin, or other quinolone antibacterials.

 PRESENTATION

L-FROX: Each box contains 10 Blister of 10 tablets per strip