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Evaflox

( Ofloxacin Tablets )

COMPOSITION :

Evaflox 200 mg : Each film coated tablet contains : Ofloxacin USP 200 mg

Evaflox 400 mg : Each film coated tablet contains : Ofloxacin USP 400 mg

PROPERTIES :

Ofloxacin, the active ingredient of EVAFLOX is a bactericidal quinolone antibiotic.

Mechanism of action :

A primary bacterial target of ofloxacin, like other quinolones is the enzyme DNA gyrase. DNA gyrase contains four subunits: two 'A" and two 'B' subunits. Genetic and biochemical studies have identified the A subunit of DNA gyrase (type I) topoisomerase) as the target of quinolones. Quinolones inhibit all the enzymatic activities of DNA gyrase, including inhibition of negative supercoiling, the joining and separation of interlocked DNA circles. )n addition, ofloxacin has a second mechanism of action, independent of its effect on RNA synthesis. Rifampicin which exhibits RNA synthesis prevents bactericidal action of quinolones such as nalidixic acid but has much less effect on the action of ofloxacin. Ofloxacin has bactericidal activity against bacteria, in genera) the minimal bactericidal concentration (MBC) is the same as, or no more than, one fold concentration higher than the minima) concentration (MNC).

Antibacterial spectrum :

I Highly susceptible organisms

Enterobacteriaceae - Escherichia coli, Enterobacter, Klebsiella, Proteus, Salmonella, Shigella, Serratia, Citrobacter.

Staphylococci : Staphylococcus aureus (including methicillin-resistant Staph). Staphylococcus epidermidis.

Neisseriae : Neisseria gonorrhoeae (including ampicillin resistant strains), Neisseria meningitidis.

II Susceptible organisms

Campylobacter, Aeromonas, Vibrio cholerae, Yersinia enterocolitica, Helicobacter pylori, Gardnerella vaginalis.

III Organisms with variable susceptibility

Pseudomonas aeruginosa, Enterococci

Streptococci (Strept. pyogenes, Strept. pneumoniae, Strept. viridans)

Mycoplasma (Mycoplasma hominis, Mycoplasma pneumoniae)

Mycobacteria (Mycobacterium tuberculosis, Mycobacterium fortuitum)

IV Usually resistant organisms

Ureaplasma urealyticum, Nocardia asteroides, and anaerobes (e.g.: Bacteroides, Peptococcus, Peptostreptococcus, Fusobacterium, Clostridium difficile)

V Resistant organisms

Treponema pallidum.

PHARMACOKINETICS

Ofloxacin is essentially 100% absorbed following oral administration. Very high concentrations of the drug are achieved in serum and most body fluids and tissues. These levels are sufficient to inhibit most bacteria at the site of infection.

Ofloxacin is rapidly and uniformly absorbed after oral administration. There is negligible presystemic metabolism. Maximum serum concentration (T_max) are usually achieved in under 2h (0.5-1.6h). Following an oral dose of 100 mg ofloxacin, the peak serum concentration (C_max) is 1.3 mg.l^-1, which increase to 3.8 mg.l^-1 with 300 mg, 5.5 mg.l^-1 with 400 mg, and 7-10 mg.l^-1 with 600 mg respectively. The plasma elimination half-life is about 6-7h. The apparent volume of distribution is 1-2.5 l.kg^-1. More than 70% of the drug is recovered unchanged in the urine in 24h, and 80% in 48h. Renal clearance is 180-190 ml.min^-1. Less than 10% of the dose is received as metabolites. Ofloxacin exhibits low plasma protein binding (20-25%).

Ofloxacin penetrates well into many body fluids. Very high concentrations of the drug are found in saliva, nasal secretions, tears, blister fluid, bronchial secretions, and sputum. ofloxacin penetration into sputum and bronchial secretion is 70-115%. Bronchial secretion penetration studies suggest that ofloxacin, at a 400 mg oral dose, is likely to achieve therapeutic activity against respiratory pathogens. After oral administration of ofloxacin 200 mg, 42-71% penetration is found in the cerebrospinal fluid.

Ofloxacin penetration into lung tissue is quite high (with tissue/serum levels of 17.7/8.7 mg.l^-1, to give a ratio of 2). Ofloxacin penetration into bone has been studied. The ratio of the bone to serum levels was 0.61%. Penetration of up to 112% into prostatic tissue were reported.

Metabolism plays a very limited role in the elimination of ofloxacin. Three metabolites of ofloxacin have been found: ofloxacin-glucuronide, desmethyl-ofloxacin, and ofloxacin-N-oxide.

Ofloxacin is extensively excreted by the kidneys as the unchanged drug with up to 80% of an oral dose eliminated in the urine as the parent compound within 48h.

Urinary recovery of desmethyl and N-oxide ofloxacin accounts for less than 5% of an administered oral dose.

INDICATIONS :

For the treatment of infections caused by susceptible strains of micro-organisms in infections of the urinary tract, respiratory tract, ear, nose and throat, abdominal cavity and skin and soft tissues.

CONTRAINDICATIONS :

EVAFLOX must not be used in

1. Pregnancy and lactation

2. Children and adolescents in the growth phase

3. Epileptics as well as in patients with a lowered cerebral seizure threshold due to pre-existing central nervous system lesions

4. Patients hypersensitive to ofloxaoin, other quinolones or any of the excipients

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