Levoflox - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 10.0 mg or 20.0 mg; corn starch 30.0 mg or 45.0 mg; lactose monohydrate 10.0 mg or 20.0 mg; silicon colloid dioxide 7.0 mg or 14.0 mg; povidone 16.0 mg or 32.0 mg. Fade orange (polyvinyl alcohol partially hydrolyzed, talc, titanium dioxide [E-171], macrogol, soy lecithin, sunscreen sunset yellow aluminum lacquer [E-110]) 3.0 mg or 6.0 mg; Opaprai pink (polyvinyl alcohol partially hydrolyzed, talc, titanium dioxide [E-171], macrogol, soy lecithin, iron oxide red oxide [E-172], dye iron oxide yellow [E 172]) 7.0 mg or 14.0 mg.

Description:

Dosage of 250 mg

Biconvex tablets are brown, film-coated.

Dosage 500 mg

Oval biconvex tablets are pinkish-orange in color, covered with a film membrane.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Levofloxacin is a fluoroquinolone, a broad-spectrum antimicrobial bactericide. It blocks DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and bacterial membranes.

Activity in vitro for the following microorganisms

Sensitive microorganisms - minimum inhibitory concentration less than 2 mg / l)

Gram-positive aerobes: 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 groups viridans (penicillin-sensitive / resistant strains).

Gram-negative aerobes: 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 (producethe 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.

Anaerobes: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus 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 (the minimum suppressive concentration is more than 4-8 mg / l):

Gram-positive aerobes: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains).

Gram-negative aerobes: Burkholderia cepacia, Campylobacter jejuni, Campylobacter coli.

Anaerobes: Bacteroides thetaiotaomicronron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Stable microorganisms (minimum inhibitory concentration more than 8 mg / l):

Gram-positive aerobes: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), others Staphylococcus spp. (coagulase-negative methicillin-resistant strains).

Gram-negative aerobes: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

Absorption: After oral administration levofloxacin quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is 99%. Food intake has little effect on the speed and completeness of absorption.The maximum concentration (Cmah) in blood plasma with the intake of 250 mg and 500 mg is achieved after 1-2 hours and is 2.8 μg / ml and 5.2 μg / ml, respectively.

Distribution: After taking a single or multiple dose, the amount of absorbed drug is directly proportional to the dose taken. The equilibrium concentration in plasma is reached after 48 hours. The connection with plasma proteins is φ 30-40%. The average volume of distribution is from 89 to 112 liters. Good penetrates into the organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages.

Metabolism: In the liver, a small part of levofloxacin is oxidized and / or deacetylated.

Excretion: Half-life (T_1/2) 6-8 hours. About 70% of levofloxacin is excreted by the kidneys for 24 hours unchanged (about 87% - for 48 hours) and less than 5% in the form of metabolites for 48 hours. Intestine excretes less than 4% of the dose taken for 72 hours. Kidney clearance is 70% of the total ground clearance. It is not excreted from the body by hemodialysis or chronic outpatient peritoneal dialysis.

Indications:

Infectious-inflammatory diseases caused by susceptible to levofloxacin microorganisms: infections of the lower respiratory tract (pneumonia,exacerbation of chronic bronchitis); acute bacterial sinusitis; urinary tract infection and kidney infection (including acute pyelonephritis); infections of the skin and soft tissues (festering atheromas, abscess, boils); chronic bacterial prostatitis; intra-abdominal infection (in combination with antibacterial drugs acting on anaerobic microflora); tuberculosis (as part of complex therapy of drug-resistant forms).

Contraindications:

Hypersensitivity to levofloxacin, other fluoroquinolones, or other components of the drug in the anamnesis; epilepsy; the defeat of tendons associated with taking quinolones in an anamnesis; children and adolescents under 18; pregnancy; lactation period; lactose intolerance, lactase deficiency, glucose-galactose malabsorption (due to the presence of lactose in the formulation).

Carefully:

Elderly age (high probability of concomitant decrease in kidney function); deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

Inside, before meals or at a break between meals, without chewing, squeezed enough water.

Adult patients with normal renal function (creatinine clearance greater than 50 ml / min) should be used according to the following schemes:

- Acute bacterial sinusitis - 500 mg once a day, for 10-14 days.

- Infectious exacerbation of chronic bronchitis - 250-500 mg once a day, for 7-10 days.

- For pneumonia, 250-500 mg 1-2 times a day (0.5-1 g / day) for 7-14 days.

- Uncomplicated urinary tract infections - 250 mg once a day for 3 days.

- Complicated urinary tract infections, incl. Acute pyelonephritis - 250 mg once a day for 7-10 days.

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

- Chronic bacterial prostatitis - 500 mg once a day for 28 days.

- Intra-abdominal infection (in combination with antibacterial drugs acting on anaerobic flora) is 500 mg once a day for 7-14 days.

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

Correction of the dose of levofloxacin in adult patients with impaired kidney function (creatinine clearance less than 50 ml / min)

Dose with normal kidney function every 24 hours

Creatinine clearance from 20 to 49 ml / min

Creatine clearance from 10 to 19 ml / min

Creatinine clearance less than 19 ml / min, incl. with hemodialysis or chronic outpatient peritoneal dialysis

500 mg

The initial dose of 500 mg.

Then 250 mg every 24 hours

The initial dose of 500 mg.

Then 250 mg every 48 hours

The initial dose of 500 mg.

Then 250 mg every 48 hours

250 mg

Correction is not required

250 mg every 48 hours.

With uncomplicated urinary tract infections, dose adjustment is not required

There is no information on dose adjustment

If the liver function is not corrected, dose adjustment is not required, because the volume of metabolism of levofloxacin in the liver is limited.

Side effects:

From the nervous system: headache, dizziness, weakness, drowsiness, insomnia, tremor, anxiety, paresthesia, fear, hallucinations, confusion, depression, movement disorders, convulsions.

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

From the side of the cardiovascular system: lowering of arterial pressure, vascular collapse, tachycardia, lengthening of the interval Q-T, atrial fibrillation.

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

From the side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia.

From the musculoskeletal system: arthralgia, muscular weakness, miagia, rhabdomyolysis, tendon rupture, tendonitis.

From the 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, swelling of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, suffocation, anaphylactic shock, allergic pneumonitis, vasculitis.

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

Overdose:

Symptoms: nausea, erosive lesions of the mucous membrane of the gastrointestinal tract, lengthening of the interval Q-T, confusion, dizziness, convulsions.

Treatment: gastric lavage, if necessary - symptomatic therapy. There is no specific antidote, dialysis is ineffective.

Interaction:

Levofloxacin increases the half-life of cyclosporine.

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

Non-steroidal anti-inflammatory drugs and theophylline while simultaneous use with levofloxacin increases the risk of seizures in predisposed patients, and glucocorticosteroids increase the risk of rupture of tendons.

With simultaneous administration of levofloxacin with hypoglycemic drugs, changes in blood glucose concentration, including hyperglycaemia and hypoglycemia, are possible.

Levofloxacin increases the anticoagulant effect of warfarin.

Cimetidine and drugs that block tubular secretion slow the withdrawal of levofloxacin.

Special instructions:

After normalization of body temperature, it is recommended to continue treatment for at least 48-72 hours.

Levofloxacin is taken at least 2 hours before or 2 hours after ingestion of aluminum-or magnesium-containing antacids, or sucralfate, or other preparations containing calcium, iron or zinc.

Due to possible photosensitization during the treatment period and within 5 days after the end of levofloxacin treatment, sunlight and artificial ultraviolet irradiation should be avoided. With the development of phototoxicity, drug treatment should be discontinued.

When there are signs of tendinitis, pseudomembranous colitis and allergic reactions levofloxacin immediately cancel.

It should be borne in mind that in patients with a history of brain damage (stroke, severe trauma) may develop seizures.

With insufficiency of glucose-6-phosphate dehydrogenase, the risk of hemolytic reactions is possible.

Patients with diabetes mellitus during treatment with levofloxacin should carefully monitor the concentration of glucose in the blood.

With the simultaneous use of levofloxacin and warfarin, monitoring of prothrombin time,international normalized relationship or other anticoagulation tests, and monitoring of bleeding symptoms.

Effect on the ability to drive transp. cf. and fur:

On the background of taking levofloxacin, the patient's ability to concentrate and speed of psychomotor reactions may be impaired. In this regard, care must be taken when driving vehicles and engaging in other potentially hazardous activities.

Form release / dosage:Film-coated tablets, 250 mg, 500 mg.

Packaging:For 5 or 10 tablets in a contour mesh package made of polyvinyl chloride film and aluminum foil.

1 contour pack together with instructions for use in a cardboard box.

Storage conditions:

In a 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 time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000049

Date of registration:23.11.2010

The owner of the registration certificate:Rowecq LimitedRowecq Limited United Kingdom

Manufacturer: & nbsp

BELCO PHARMA India

Representation: & nbspROUTEC LIMITEDROUTEC LIMITEDUnited Kingdom

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Levoflox (Levoflox)