Levofloxacin - instructions for use, dosage, side effects, contraindications

Excipients: croscarmellose sodium (impellosis) - 7 mg and 14 mg, magnesium stearate - 3.2 mg and 6.4 mg, povidone medium molecular weight (polyvinylpyrrolidone medium molecular weight medical) - 14 mg and 28 mg, microcrystalline cellulose - 21.6 mg and 43.2 mg, silicon dioxide colloid (aerosil 380) 5 mg and 10 mg, talc 6.4 mg and 12.8 mg pregelatinized starch (Starch-1500) 12.8 mg and 25.6 mg.

The composition of the shell: Opadrai II (polyvinyl alcohol, partially hydrolyzed - 4 mg and 8 mg, macrogol (polyethylene glycol 3350) - 2.02 mg and 4.04 mg, talc - 1.48 mg and 2.96 mg, titanium dioxide - 1.459 mg and 2,918 mg, an aluminum lacquer based on yellow quinoline E 104 - 0.84 mg and 1.68 mg, iron oxide oxide (II) E 172 - 0.198 mg and 0.396 mg, an aluminum lacquer based on indigo carmine E 132 - 0.003 mg and 0.006 mg) to a film coated tablet weighing 330 mg and 660 mg, respectively.

Description:

The tablets covered with a film cover of yellow color, round, biconcave form. Tablets at the break of light yellow color.

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 bactericide from the group of fluoroquinolones. 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.

To the preparation in vitro sensitive (minimum inhibitory concentration less than 2 mg / l): Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (at m. h. Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing, coagulase-negative methicillin-sensitive / moderately sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive / moderately sensitive / resistant strains), Streptococcus pyogenes, Streptococcus spp. groups viridans (penicillin-sensitive / resistant strains).

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

Anaerobic microorganisms: 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 pneumophila, Mycobacterium spp. (at m. h. Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (minimum inhibitory concentration 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, Campylobacter jejuni, Campylobacter 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 Staphylococcus spp. (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 in the blood plasma (TCmah) - 1-2 hours; at reception of 250 and 500 mg the maximum concentration in a blood plasma (Withmax) is about 2.8 and 5.2 μg / ml, respectively. The connection with plasma proteins is 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated. Kidney clearance is 70 % of the total ground clearance. The half-life (T1 / 2) is 6-8 hours. It is excreted from the body mainly kidneys by glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form, 70% are excreted by the kidneys within 24 hours, and 87% in 48 hours; the intestine displays 4 % an internal dose of levofloxacin.

Indications:

Infectious-inflammatory diseases caused by susceptible to levofloxacin microorganisms:

- acute bacterial sinusitis;

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

- urinary tract and kidney (including acute pyelonephritis);

- chronic bacterial prostatitis;

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

- intra-abdominal infections in combination with drugs acting on anaerobic microflora;

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

Contraindications:

Hypersensitivity to levofloxacin and other fluoroquinolones, epilepsy, tendon damage with quinolones previously treated, pregnancy, breastfeeding, children and adolescence (up to 18 years).

Carefully:

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

Dosing and Administration:

The drug is taken orally once or twice a day. Tablets can not be chewed and washed down with a sufficient amount of liquid (0.5 to 1 cup), can be taken before meals or between meals. Doses are determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility.

Patients with normal or moderately reduced renal function (creatinine clearance> 50 mL / min) are recommended the following dosing regimen:

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

Exacerbation of chronic bronchitis: 250 mg or 500 mg once a day - 7-10 days. Community-acquired pneumonia: 500 mg 1-2 times a day - 7-14 days.

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

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

Complicated urinary tract infections, including pyelonephritis: 250 mg once a day-7-10 days.

Infections of the skin and soft tissues: 250-500 mg 1-2 times a day - 7-14 days. Intraabdominal infection: 500 mg once a day - 7-14 days (in combination with antibacterial drugs acting on anaerobic flora).

With tuberculosis (as part of complex therapy) - 500 mg 1-2 times a day, the course of treatment - up to 3 months.

Correction of the dose of levofloxacin in adult patients with impaired renal function

(creatinine clearance less than 50 ml / min)

Dose with normal kidney function every 24 hours	Creatinine clearance from 20 to 49 ml / min	Creatinine clearance from 10 to 19 ml / min	Creatinine clearance less than 10 ml / min, incl.with hemodialysis or chronic outpatient peritoneal dialysis
1000 mg	The initial dose of 500 mg every 12 hours, then 250 mg every 12 hours	The initial dose of 500 mg every 12 hours, then 125 mg every 12 hours	The initial dose of 500 mg every 12 hours, then 125 mg every 24 hours
500 mg	The initial dose is 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 of dose is not required	250 mg every 48 hours. In uncomplicated infections urinary tract dosage adjustment is not required	No information on dose adjustment

After hemodialysis or permanent ambulatory peritoneal dialysis (CAPD), no additional doses are required.

If the liver function is not required, a special dose selection is required, since levofloxacin is metabolized in the liver only to a very small extent.

For elderly patients, there is no need to change the dosage regimen, except for cases of low creatinine clearance

As with the use of other antimicrobials, treatment with levofloxacin is recommended to continue at least 48-72 hours after normalization of body temperature or after a reliable eradication of the pathogen.

If you missed taking the drug, you should take a pill as soon as possible until the time of the next appointment is near. Then continue taking the drug according to the scheme.

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 Q-T, atrial fibrillation.

From the side of metabolism: hypoglycemia (increased appetite, increased

sweating, trembling, nervousness), hyperglycemia.

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

From the urinary system: hypercreatininemia, interstitial nephritis, acute renal failure.

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

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

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

Overdose:

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

Treatment: gastric lavage, symptomatic therapy, dialysis is not effective.

Interaction:

Increases T1 / 2 cyclosporine.

The effect of the drug reduces drugs that depress intestinal motility, sucralfate, aluminum- and magnesium-containing antacid drugs and iron salts (a break between taking at least 2 hours is necessary).

Non-steroidal anti-inflammatory drugs, theophylline increase the risk of seizures, glucocorticosteroids increase the risk of rupture of tendons.

Cimetidine and drugs that block tubular secretion slow down excretion.

Hypoglycemic drugs: strict control over the concentration of glucose in the blood is necessary, since there is a possibility of hyper- and hypoglycemia with simultaneous use with levofloxacin.

Levofloxacin increases the anticoagulant effectiveness of warfarin.

Special instructions:

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 salts.

During treatment, sun and artificial UV irradiation should be avoided to avoid damage to the skin (photosensitivity).

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

It should be borne in mind that in patients with a history of brain damage (stroke, severe trauma), convulsions may develop, with insufficiency of glucose-6-phosphate dehydrogenase - the risk of hemolysis increases.

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 ratio or other anticoagulation tests, as well as monitoring of bleeding symptoms, is shown.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 250 mg and 500 mg.

Packaging:

For 5 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 5 or 10 tablets in a jar of light-protective glass or in a jar of polymeric, or in a vial of polymer.

Each jar or bottle or 1 circuit cell package, together with the instructions for use, is placed 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:

2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000327

Date of registration:22.02.2011

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp06.10.2015

Illustrated instructions

Instructions

Levofloxacin (Levofloxacin)