Levofloxacin 5 mg/mL

(Sterile, Pyrogen Free, Single Dose)

Indication

It is a fluoroquinolone antibiotic medicine used in adults, age 18 years or older to treat certain infections caused by certain bacteria.

It is indicated for the treatment of mild to moderate bacterial infections in adults when caused by levofloxacin sensitive bacteria: Acute sinusitis (inflammation of one or more paranasal sinuses), inflammation of the lower airways (acute exacerbation of chronic bronchitis, community acquired pneumo...read more

Dosage and Administration

This infusion should be given over a period of at least 60 minutes.

Adult:

Community acquired pneumonia: 500 mg once daily for 7 to 14 days 750 mg once daily for 5 days

Complicated urinary tract infections: 250 mg once daily for 10 days

Chronic prostatitis: 500 mg once daily for 28 days

Complicated skin and soft tissue infections: 750 mg once daily for 7 to 14 days

Inhalation of anthrax(treatment and post-exposure prophylaxis): 500 mg once daily.

Composition

Each 100 mL contains:

Levofloxacin Hemihydrate equivalent to Levofloxacin ... 500 mg

Water for Injection B.P ... q.s.

Description

Levofloxacin is a synthetic broad spectrum antimicrobial agent and optically active levo isomer of ofloxacin.

Chemically, Levofloxacin, a chiral fluorinated carboxyquinolone, is the pure (-)-(S)-9-fluoro-2,3-dihydro- 3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido [1,2,3-de]-1,4-benzoxazine-6-carboxylic acid hemihydrate. Its molecular formula is C18H20FN3O4 and molecular weight is 361.373.

Clinical Pharmacology

Mechanism of Action

The main mechanism of action of Levofloxacin is the inhibition of DNA gyrase. It is two fold stronger than that of ofloxacin. There is not much difference between the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The activity of Levofloxacin is bactericidal. In...read more

Pharmacological Action

Levofloxacin is active against Gram-positive and Gram-negative organisms. It is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. It has greater activity against Pneumococci than Ciprofloxacin. Levofloxacin is licensed for community acquired pneumonia ...read more

Antimicrobial Spectrum

Levofloxacin has been shown to be active against most strains of the following:

Aerobic Gram-positive Microorganisms: Enterococcus faecalis (many strains are only moderately susceptible), Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus pneumonia, Streptococcus pyogenes. With other drugs in this class, some strains of Pseudomonas ae...read more

Pharmacokinetics

Distribution: Vd- 1.25 L/Kg; CSF concentration - approximately 15% of serum levels; high concentrations are achieved in prostate and gynecological tissues, sinus, breast milk and saliva.

Protein binding: 50%

Metabolism: Minimally hepatic Bioavailability: 100%

Half-life elimination: 6 hours Time to peak: I hour

Excretion: primarily urine (as unchanged drug).

Contraindication

Hypersensitivity to levofloxacin, any component of the formulation or other quinolones. Patients who suffer from epilepsy, with a history of tendon disorders related to the treatment with an antibiotic of the fluoroquinolone class.

Warning and Precaution

Systemic: Not recommended in children under 18 years of age; CNS stimulation may occur (tremor, restlessness, confusion and very rarely hallucination or seizure); use with caution in patients with known or suspected CNS disorders or renal dysfunction; use caution to avoid possible photosensitivity r...read more

Use caution in patients with bradycardia, hypokalaemia, hypomagnesemia, or in those receiving concurrent therapy with Class Ia or Class Ill antiarrhythmias.

Prolonged use may result in superinfection, pseudomembranous colitis may occur and should be considered in all patients who present with diarrhea. Tendon inflammation and/or rupture has been reported; discontinue at first sign of tendon inflammation or pain.

Adverse Effects

Tendon effects, hypersensitivity reactions, other serious and sometimes fatal reactions, hepatotoxicity, CNS effect, Clostrium difficle associated diarrhoea, peripheral neuropathy, prolongation of QT interval, musculoskeletal disorders in pediatric patients, blood glucose disturbances, photosensitiv...read more

Overdose

Symptoms include acute renal failure and seizures. Treatment should include GI decontamination and supportive care. Not removed by peritoneal or hemodialysis.

Drug Interaction

Levofloxacin should not be co-administered with any solution containing multivalent cations, e.g. magnesium, through the same IV line.

The elimination of levofloxacin was slightly reduced by cimetidine and probenecid. However, these interactions are unlikely to be of clinical relevance.

Levofloxacin should be given carefully when it is co­ administered with drugs that affect a certain mode elimination (tubular secretion) e.g. probenecid and cimetidine.

This applies especially to patients with impaired renal function.

The half-life of cyclosporin was increased by 33% when co-administered with levofloxacin.

No pharmacokinetic interactions of levofloxacin were found with warfarin in a clinical study. However, levofloxacin is reported to enhance the effects of warfarin. Elevation of the prothrombin time and bleeding episodes have been reported with concurrent warfarin and levofloxacin.

Distrubances of blood glucose, including hyperglycemia and hypoglycemia have been reported in patients treated concomitantly with quinolones and antidiabetic agents. Therefore, careful monitoring of blood glucose is recommended when these agents are co-administered.

Antineoplastic agents may decrease the absorption of levofloxacin. Levofloxacin may cause increase levels of azlocillin, cyclosproin and caffeine. Azlocillin, cimetidine, loop diuretics (furosemide, torsemide) and probenecid increase quinolone levels (decreased renal secretion).

Concomitant administration of NSAID with a quinolone including levofloxacin may increase risk of CNS stimulation and convulsive seizures.

Theophylline levels should be closely monitored and appropriate dosage adjustments made when levofloxacin is co-administered. Adverse reactions including seizures, may occur with or without an elevation in serum theophylline level.

Storage

Should be stored in cool and dark place. Avoid freezing.

Do not remove inner container from carton box until ready for use.