LEVOFLOX Tablet

Levoflox 250 tablets contains levofloxacin as the active ingredient. This belongs to a group of antibiotics called fluoroquinolones. Levofloxacin works by killing bacteria that cause infections, including the bacteria that cause tuberculosis (TB).

Levoflox 250 tablets is used to treat TB caused by Mycobacterium tuberculosis. It is always given together with other medicines for TB.

To help clear up your TB completely, you must keep taking this medicine for the full time of treatment even if you begin to feel better. This is very important. It is also important that you do not miss any doses.

 

Dosage

Adults and adolescents:

The recommended dose is 750-1000mg, given once daily.

Children:

The recommended dose is 20mg/kg/day, divided into two daily doses, up to a maximum of 1000mg/day.

Renal impairment:

For patients with an estimated creatinine clearance ≤30mL/min, with or without haemodialysis, the dose should be reduced to 750-1000mg given three times per week.

Hepatic impairment:

No adjustment of dosage is required.

Elderly:

No adjustment of dosage is required in the elderly, other than that imposed by consideration of renal function.

Method of administration

Levoflox 250 tablets should be swallowed whole with a sufficient amount of liquid. The tablets may be taken without regard to food.

- in patients with hypersensitivity to levofloxacin, other quinolones or to any of the excipients

- in patients with epilepsy

- in patients with history of tendon disorders related to fluoroquinolone administration

- in breast-feeding women

Infections and infestations

Uncommon: fungal infection (and proliferation of other resistant microorganisms of the normal flora)

Blood and lymphatic system disorders

Uncommon: leukopenia, eosinophilia

Rare: thrombocytopenia, neutropenia

Very rare: agranulocytosis

Not known: pancytopenia, haemolytic anaemia

Immune system disorders

Very rare: anaphylactic shock. Anaphylactic and anaphylactoid reactions may sometimes occur even after the first dose.

Not known: hypersensitivity

Metabolism and nutrition disorders

Uncommon: anorexia

Very rare: hypoglycaemia, particularly in diabetic patients

Psychiatric disorders

Uncommon: insomnia, nervousness

Rare: psychotic disorder, depression, confusional state, agitation, anxiety

Very rare: psychotic reactions with self-endangering behavior including suicidal ideation or acts, hallucination

Nervous system disorders

Uncommon: dizziness, headache, somnolence

Rare: convulsion, tremor, paraesthesia

Very rare: sensory or sensorimotor peripheral neuropathy, dysgeusia including ageusia, parosmia including anosmia

Eye disorders

Very rare: visual disturbance

Ear and Labyrinth disorders

Uncommon: vertigo

Very rare: hearing impaired

Not known: tinnitus

Cardiac disorders

Rare: tachycardia

Not known: electrocardiogram QT prolonged

Vascular disorders

Rare: hypotension

Respiratory, thoracic and mediastinal disorders

Rare: bronchospasm, dyspnoea

Very rare: allergic pneumonitis

Gastrointestinal disorders

Common: diarrhoea, nausea

Uncommon: vomiting, abdominal pain, dyspepsia, flatulence, constipation

Rare: haemorrhagic diarrhoea - which in very rare cases may be indicative of enterocolitis, including pseudomembranous colitis

Hepatobiliary disorders

Common: hepatic enzyme increased (ALT/AST, alkaline phosphatase, GCT)

Uncommon: blood bilirubin increased

Very rare: hepatitis

Not known: jaundice and severe liver injury, including cases with acute liver failure, primary in patients with severe underlying diseases

Skin and subcutaneous tissue disorders

Uncommon: rash, pruritus

Rare: urticaria

Very rare: angioneurotic oedema, photosensitivity reaction

Not known: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, hyperhidrosis, Mucocutaneous reactions may sometimes occur even after the first dose.

Musculoskeletal and Connective tissue disorders

Rare: tendon disorder including tendinitis (e.g. Achilles tendon), arthralgia, myalgia

Very rare: tendon rupture. This undesirable effect may occur within 48 hours of starting treatment and may be bilateral. Muscular weakness (which may be of special importance in patients with myasthenia gravis).

Not known: rhabdomyolysis

Renal and urinary disorders

Uncommon: blood creatinine increased

Very rare: acute renal failure (e.g. due to interstitial nephritis)

General disorders and administration site conditions

Uncommon: asthenia

Very rare: pyrexia

Not known: pain (including pain in back, chest, and extremities)

Other undesirable effects which have been associated with fluoroquinolone administration include:

- extrapyramidal symptoms and other disorders of muscular coordination

- hypersensitivity vasculitis

- attacks of porphyria in patients with porphyria

(See the package insert about the details.)

Iron salts, magnesium- or aluminium-containing antacids

Sucralfate

Theophylline

NSAIDs

Coadministration with NSAIDs

Probenecid and cimetidine

Vitamin K antagonists

Drugs known to prolong QT interval

Drugs undergoing renal tubular secretion

Women of childbearing potential

Pregnancy should be avoided in women treated with levofloxacin. Adequate contraceptive measure should be taken.

Pregnancy

There are limited data from the use of levofloxacin in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity.

However in the absence of human data and due to experimental data suggesting a risk of damage to the weight-bearing cartilage of the growing organism by fluoroquinolones, levofloxacin should only be used in pregnancy if the benefit is considered to outweigh the risks, and there are no available treatment alternatives.

Lactation

Levofloxacin is contraindicated in breast-feeding women. There is insufficient information on the excretion of levofloxacin in human milk; however other fluoroquinolones are excreted in breast milk.

In the absence of human data and due to experimental data suggesting a risk of damage to the weight-bearing cartilage of the growing organism by fluoroquinolones, Levoflox 250 tablets must not be used in breast-feeding women.

(See the package insert about the details.)

Tendinitis and tendon rupture

Clostridium difficile-associated disease

Patients predisposed to seizures

Patients with G-6-phosphate dehydrogenase deficiency

Patients with renal impairment

Hypersensitivity reactions

Hypoglycaemia

Prevention of photosensitization

Patients treated with Vitamin K antagonists

Psychotic reactions

QT interval prolongation

Peripheral neuropathy

Patients with myasthenia gravis

Opiates

Hepatobiliary disorders

Paediatric population

Pharmacotherapeutic group: Antibacterial for systemic use, fluoroquinolone

Levofloxacin is a synthetic antibacterial agent of the fluoroquinolone class and is the S(-) enantiomer of the racemic drug substance ofloxacin.

Mechanism action

Levofloxacin has in vitro activity against M-Tuberculosis, as well as against a wide range of Gram-positive and Gram-negative pathogens. The bactericidal action of levofloxacin against M-Tuberculosis results from the inhibition of the DNA gyrase, encoded by the gyrA and gyrB genes.

The wild-type levofloxacin MIC distribution for clinical isolates of M-Tuberculosis has been reported by different investigators to range between 0.125-0.5 mg/l. When resistance to fluoroquinolones arises, it is generally caused by mutations in gyrA. Cross-resistance within the fluoroquinolone drug class is extensive, though not universal.