OD-Levox - instructions for use, dose, side effects, contraindications

crospovidone 22.00 mg, hypromellose 8.00 mg, microcrystalline cellulose 65.00 mg, silicon colloidal dioxide 5.00 mg, talc 3.00 mg, magnesium stearate 7.00 mg, water.

Sheath:

hypromellose 10.30 mg, macrogol 1.20 mg, titanium dioxide 6.00 mg, talc 1.20 mg, methyl parahydroxybenzoate 0.120 mg, propyl parahydroxybenzoate 0.060 mg, water.

* - Removed during production.

Description:

Capsule-coated tablets, white or almost white in color with a dividing risk on one side. Two layers are visible on the cross-section. At the break the core of the tablet is yellow.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Levofloxacin is a broad spectrum antimicrobial agent from the group of fluoroquinolones, containing as an active substance the levorotatory isofloxacin isomer.It blocks DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, suppresses DNA synthesis, causes profound morphological changes in the cytoplasm; cell wall and membranes.

Effective against most strains of microorganisms in vitro and in vivo. The action of the drug is sensitive:

aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (incl. Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive / moderately sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus spp., (leukotoxin-containing); Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive / moderately sensitive / resistant strains), Streptococcus pyogenes, Streptococcus group, viridans (penicillin-sensitive / resistant strains);

aerobic gram-negative microorganisms: Acinetobacter spp. (at t.h. Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (at t.h. Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive/resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (at t.h. Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (producing and non-reducing beta-lactamase strains), Morganella morganii, Neisseria gonorrhoeae (producing and non-reducing penicillinase strains), Neisseria meningitidis, Pasteurella spp., (at t.h. Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (at t.h. Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (at t.h. Pseudomonas aeruginosa), Serratia spp. (at t.h. Serratia marcescens), Salmonella spp .;

anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp .; Peptbstreptococcus.spp., Propionibacterium spp., Veilonella spp .;

other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella spp. (at t.h. Legionella pneumophila), Mycobacterium spp. (at t.h. Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (minimal suppressing concentrations of more than 4 mg / l):

aerobic Gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains);

aerobic gram-negative microorganisms: Burkholderia cepacia, Campilobacter jejuni; Campilobacter coli;

anaerobic microorganisms: Bacteroides thetaiotaomicronron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Sustainable microorganisms (minimal overwhelming concentration more 8 mg/l):

aerobic gram positive microorganisms; Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcusspp. (coagulase-negative methicillin-resistant strains);

aerobic gram-negative microorganisms; Alcaligenes xylosoxidans;

other: microorganisms: Mycobacterium avium.

Pharmacokinetics:

Ingestion levofloxacin quickly and almost completely absorbed (food intake has little effect on the speed and completeness of absorption). Bioavailability is 99%. Time to reach the maximum concentration (Tcmah) in the plasma -1-2 h.At reception of 500 mg the maximum concentration (Withmah) in the plasma is 5.2 μg / ml. Connectivity from plasma proteins about 30-40%.

Moderate cumulation of levofloxacin is observed already on the third day of taking the drug at a dose of 500 mg 2 times a day. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, urinary organs systems, polymorphonuclear leukocytes, alveolar macrophages. FROMmah in the bronchial mucosa and fluid / epithelial lining after oral administration of 500 mg of the drug - 8.3 μg / g and 10.8 μg / ml, respectively; FROMmlevofloxacin in the blister fluid - 4.0-6.7 μg / ml, Tcmah in this case - 2-4 hours. Withmah in the lung tissue after oral intake of 500 mg of the drug, 11.3 μg / g, and Tcmah - 4-6 hours. Levofloxacin penetrates into the cerebrospinal fluid in small amounts. With oral administration of 500 mg / day of levofloxacin on the third day of treatment Cmin the tissues of the prostate gland 2, 6 and 24 hours after taking the drug - 8.7 μg / g, 8.2 μg / g and 2.0 μg / g, respectively. Attitude Concentration of the prostate, iron / plasma on average - 1.84. The average value of Cmah in urine after taking 500 mg of the drug after 8-12 hours - 200 mg / l. In the liver, a small part of the preparation is oxidized and / or deacetylated.The half-life period (T1 / 2) is 6-8 hours. It is excreted mainly by the kidneys (about 85% of the dose) by glomerular filtration and tubular secretion. 4% of the ingested dose of levofloxacin is excreted by the intestine within 72 hours. With violations of kidney function and a decrease in renal clearance, T1 / 2 increases.

During clinical trials, there was no difference in the pharmacokinetics of the drug in men and women.

Indications:

A drug OD-Levox is used for infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin:

- lower respiratory tract (exacerbation of chronic bronchitis, community-acquired pneumonia);

- urinary tract and kidneys (including acute pyelonephritis);

- chronic bacterial prostatitis;

- skin and soft tissues (festering atheromas, abscess, boils);

- intra-abdominal infections;

- acute bacterial sinusitis;

- tuberculosis (complex therapy of drug-resistant forms).

Contraindications:

Hypersensitivity to levofloxacin or other fluoroquinolones, as well as to the auxiliary substances of the drug, epilepsy, tendon damage with quinolones previously treated, pregnancy, lactation, children and adolescence (up to 18 years).

Carefully:

Elderly age (due to high probability of concomitant decrease in kidney function), deficiency of glucose-6-phosphate dehydrogenase, predisposition to convulsive reactions (atherosclerosis of cerebral vessels, cerebral circulatory disorders (in anamnesis), organic diseases of the central nervous system), renal failure, congenital lengthening syndrome Q-T, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (eg, hypokalemia, hypomagnesemia), diabetes mellitus, myasthenia gravis gravis, psychoses and other mental disorders in the anamnesis, hepatic porphyria, simultaneous reception of drugs that extend the interval Q-T (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including. astemizole, terfenadine, ebastine) and lowering the threshold of convulsive readiness of the brain (fenbufen, theophylline).

Dosing and Administration:

OD-Levox should be administered orally during meals or during a break between meals food, without chewing, squeezed with enough liquid.

Doses of OD-Levox preparation are determined by the nature and severity of the infection, as well as by the suspected pathogen susceptibility.

The recommended dose of the drug for adults with normal renal function (creatinine clearance (CK)> 50 ml / min):

In acute bacterial sinusitis - 500 mg once a day for 10-14 days;

With an exacerbation of chronic bronchitis - 250-500 mg once a day for 7-10 days;

With community-acquired pneumonia - 500 mg 1 or 2 times a day for 7-14 days;

With uncomplicated infections of the urinary tract and kidneys - 250 mg (1/2 tablet) 1 time per day for 3 days;

With complicated infections of the urinary tract -250 mg (1/2 tablet) once a day in within 7-10 days;

With chronic bacterial prostatitis - 500 mg once a day for 28 days;

With infections of the skin and soft tissues - 250-500 mg 1-2 times a day for 7-14 days;

Intra-abdominal infections - 500 mg once a day - 7-14 days (in combination with antibacterial drugs acting on anaerobic flora);

Tuberculosis (complex therapy of drug-resistant forms) - 500 mg 1-2 times a day, treatment course up to 3 months.

For patients with impaired renal function (CK <50 mL / min):

Dosing regimen with normal kidney function, every 24 hours	Creatinine clearance, ml / min
	50-20		19-10		<10 (including hemodialysis and CAPD *)
	the first dose: 500 mg,		the first dose: 500 mg,		the first dose: 500 mg,
500 mg		then: 250 mg every 24 hours		then: 250 mg every 48 hours		then: 250 mg, every 48 hours
250 mg		adjustments dose is not required		250 mg every 48 hours, in the treatment of uncomplicated infections, urinary no dose adjustment is required		No data on the possibility of dose adjustment

* Permanent outpatient peritoneal dialysis.

After hemodialysis or permanent ambulatory peritoneal dialysis (CAPD) is not additional doses are required.

If the liver function is not required, a special dose selection is required, since levofloxacin It is only slightly metabolized in the liver and excreted mainly by the kidneys.

If you missed taking the drug you need to take a pill as soon as possible, until the time of the next admission is near. Continue to take levofloxacin according to the scheme.

The duration of therapy depends on the type of disease (see above). In all cases, treatment should continue from 48 to 72 hours after the disappearance of the symptoms of the disease.

Side effects:

From the digestive system: nausea, vomiting, diarrhea (including blood), digestive disorders, decreased appetite, abdominal pain, pseudomembranous colitis; increased activity of "hepatic" transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

From the cardiovascular system: decrease in arterial pressure, vascular collapse, tachycardia, lengthening of the interval QT, atrial fibrillation.

From the side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia (dry mouth, thirst, increased urination, fatigue, blurred vision, dry or itchy skin, arrhythmia).

From the nervous system: headache, dizziness, weakness, drowsiness, insomnia, tremor, anxiety, paresthesia, fear, hallucinations, confusion, depression, movement disorders, seizures, peripheral sensory neuropathy, peripheral, sensory-motor, neuropathy, extrapyramidal disorders, agitation, , nightmares, mental disorders with behavioral disorders with self-harm, including suicidal thoughts and suicidal attempts.

From the sense organs: impaired vision, hearing, smell, taste and tactile sensitivity, ringing in the ears.

From the musculoskeletal system: arthralgia, muscle weakness, myalgia, tendon rupture, tendonitis, rhabdomyolysis.

From the side urinary system: hypercreatininaemia, interstitial nephritis; acute renal failure.

From the hematopoiesis: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions: itching and hyperemia of the skin; edema of the skin, and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal, necrolysis (Lyell's syndrome), bronchospasm, choking, anaphylactic shock, allergic pneumonitis, vasculitis.

Other: photosensitivity, asthenia, exacerbation of porphyria, persistent, fever, development of superinfection.

Overdose:

Symptoms: confusion, dizziness, impaired consciousness, convulsions, nausea, vomiting and erosive lesions of the mucous membranes are possible. During the research it was shown that when levofloxacin is used in doses,exceeding the average therapeutic, it is possible to extend the interval QT.

Treatment: if necessary, conduct symptomatic therapy. Levofloxacin is not excreted in hemodialysis, peritoneal dialysis and peritoneal dialysis. There is no specific antidote.

Interaction:

Quinolones can enhance the ability of drugs, including theophylline, non-steroidal anti-inflammatory drugs lower threshold of convulsive readiness. If you simultaneously receive fenbufen higher concentrations of levofloxacin are observed than with monotherapy.

The effect of levofloxacin reduces medication drugs that depress intestinal motility, sucralfate magnesium- or aluminum-containing antacid agents, salts of iron and zinc.

Reception glucocorticosteroids increases the risk of rupture of tendons.

Levofloxacin increases anticoagulant activity warfarin.

Excretion (renal clearance), levofloxacin slightly slows down under the action of cimetidine and probenecid in view of the possible blocking of the tubular secretion of levofloxacin in the kidneys. It should be noted that this interaction is of clinical importance, first of all,for patients with impaired renal function.

Levofloxacin increases half-life cyclosporine.

Simultaneous use of levofloxacin and hypoglycemic agents leads to a change in the concentration of glucose in the blood plasma (hypoglycemia and hyperglycemia).

With simultaneous application with drugs that extend the interval Q-T (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including antihistamines. astemizole, terfenadine, ebastine) it is possible to extend the interval Q-T.

Special instructions:

OD-Levox should be used at least 2 hours before or 2 hours after taking iron, zinc, antacid and sucralfate salts.

During treatment with OD-Levox, avoid sunlight and artificial UV irradiation to avoid damage to the skin (photosensitivity).

When there are signs of tendinitis, pseudomembrane colitis, allergic reactions OD-Levox immediately canceled.

It should be borne in mind that the development of seizures is possible in patients with a history of brain damage (stroke, severe trauma), and the risk of hemolysis is a deficiency in glucose-6-phosphate dehydrogenase.

With the simultaneous use of OD-Levox and warfarin, careful monitoring of prothrombin time and other coagulation parameters is necessary. It is recommended to carefully monitor the concentration of glucose in the blood plasma, while using OD Levoksa with hypoglycemic drugs.

As levofloxacin excreted mainly by the kidneys, in patients with impaired kidney function requires mandatory monitoring of kidney function; as well as adjustment of the dosing regimen. Very rare cases of lengthening of the interval have been reported Q-T in patients who received fluoroquinolones, including levofloxacin. When using fluoroquinolones, including levofloxacin, caution should be exercised in patients with known risk factors for lengthening interval Q-T: elderly age; violation of electrolyte balance (hypokalemia, hypomagnesemia); congenital lengthening syndrome Q-T; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous reception of drugs that can lengthen the interval Q-T.

In patients receiving fluoroquinolones, including levofloxacin, sensory and sensory-motor peripheral neuropathy was noted, the onset of which can be rapid. If the patient has symptoms of neuropathy, the use of levofloxacin should be discontinued. This minimizes the possible risk of irreversible changes.

Effect on the ability to drive transp. cf. and fur:During the treatment with OD-Levox, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 500 mg.

Packaging:

5 tablets per blister of aluminum foil or aluminum foil and PVC film.

For 1 blister, along with instructions for medical use, put in a pack of cardboard.

Storage conditions:

In dry, the dark place at a temperature of no higher than 25 C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-000993

Date of registration:18.10.2011

The owner of the registration certificate:Edge Pharma Private LimitedEdge Pharma Private Limited India

Manufacturer: & nbsp

EDGE PHARMA PRIVATE, Limited India

Representation: & nbspEdge Pharma Private Limited Edge Pharma Private Limited India

Information update date: & nbsp30.09.2015

Illustrated instructions

Instructions

OD-Levox (OD-Levox)