Universal reference book for medicines
Product name: LEVOLET® P (LEVOLET R)

Active substance: levofloxacin

Type: Antibacterial drug of the group of fluoroquinolones

Manufacturer: DR.
REDDY`S LABORATORIES (India)
Composition, form of production and packaging
Solution for infusions is
transparent or slightly opalescent pale yellow.

1 ml of 1 fl.

levofloxacin hemihydrate 5.12 mg 512 mg,

which corresponds to the content of levofloxacin 5 mg 500 mg

Excipients: dextrose, hydrochloric acid, sodium hydroxide, water d / u.

100 ml - bottles of low density polyethylene (1) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2012.

PHARMACHOLOGIC EFFECT

Antibacterial preparation of a group of fluoroquinolones of a wide spectrum of action.
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.
Levofloxacin is active against the following strains of microorganisms, both in vitro and in vivo.

Sensitive microorganisms (MIC of less than 2 mg / ml)

Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp.
(including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive / moderately sensitive strains, leukotoxin-containing 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 group of viridans (penicillin-sensitive / resistant strains).
Aerobic Gram-negative microorganisms: Acinetobacter spp.
(including Acinetobacter baumannil), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (including Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive / resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (producing and non-producing β-lactamase strains), Morganella morganii, Neisseria gonorrhoeae (producing and non-producing penicillinase strains), Neisseria meningitidis, Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp. (including Serratia marcescens), Salmonella spp.
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, Legionella spp., Mycobacterium spp.
(including Mycobacterium leprae, Mycobacterium tuberculosis, Mycoplasma hominis), Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.
Moderately sensitive microorganisms (MIC 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, Campylobacter jejuni, Campylobacter coli.

Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Stable microorganisms (MIC of more than 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

The pharmacokinetics of levofloxacin with a single and repeated administration of the drug is linear.
The plasma profile of the concentrations of levofloxacin after intravenous administration is similar to that of tablets. Therefore, oral and / or administration routes can be considered interchangeable.
Suction

After IV infusion of levofloxacin at a dose of 500 mg for 1 h to healthy volunteers, the mean C max in plasma was 6.2 ± 1.0 μg / ml, T max - 1.0 ± 0.1 h.

Distribution

Binding to plasma proteins - 30-40%.

After a single and multiple IV injection at a dose of 500 mg, the average Vd of levofloxacin is 89-112 liters.

It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, organs of the genitourinary system, polymorphonuclear leukocytes, alveolar macrophages.

Metabolism

In the liver, a small portion of levofloxacin is oxidized and / or deacetylated.

Excretion

When ingested, T 1/2 is 6-8 hours. After a single IV administration, a dose of 500 mg T 1/2 is 6.4 ± 0.7 hours. It is excreted mainly by the kidneys by glomerular filtration and tubular secretion.
Kidney clearance is 70% of the total clearance. Less than 5% of levofloxacin is excreted as metabolites. In the urine, for a period of 24 hours, 70% is detected unchanged, and in 87 hours 87% of the dose taken orally or injected. In stool for a period of 72 hours, 4% of the dose taken orally administered orally is detected.
Pharmacokinetics in special clinical cases

With renal failure, the decrease in clearance of the drug and its excretion by the kidneys depends on the degree of decrease in QC.

INDICATIONS

Infectious-inflammatory diseases of mild and moderate severity caused by drug-susceptible pathogens:

- community-acquired pneumonia (for solution for infusion);

- as part of complex therapy of drug-resistant forms of tuberculosis;

- Complicated infections of the kidneys and urinary tract, including pyelonephritis;

uncomplicated urinary tract infections;

- prostatitis;

- septicemia / bacteremia associated with the above indications;

- intra-abdominal infections.

DOSING MODE

The drug is administered iv.

The dose is determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility.

With community-acquired pneumonia , 500 mg 1-2 times / day.
The course of treatment is 7-14 days.
In uncomplicated infections of the urinary tract - 250 mg 1 time / day.
The course of treatment is 3 days.
With complicated infections of the urinary tract (including pyelonephritis) - 250 mg 1 time / day.
In severe infections, the dose may be increased. The course of treatment is 7-10 days.
With bacterial prostatitis - 500 mg 1 time / day.
The course of treatment is 28 days.
With septicemia / bacteremia - 500 mg 1-2 times / day.
The course of treatment is 10-14 days.
With intra-abdominal infections - 500 mg 1 time / day.
The course of treatment is 7-14 days, in combination with antibacterial drugs acting on anaerobic flora.
In the complex therapy of drug-resistant forms of tuberculosis - 500 mg 1-2 times / day (500-1000 mg levofloxacin per day), depending on the severity of the disease and the treatment scheme used.
The course of treatment is up to 3 months.
Patients with slightly impaired renal function (CK> 50 ml / min) do not need dose adjustment.

Patients with impaired renal function require a correction of the dosing regimen, depending on the magnitude of the CK.

Creatinine clearance Intravenous doses

250 mg / 24 h 500 mg / 24 h 500 mg / 12 h

first dose 250 mg first dose 500 mg first dose 500 mg

50-20 ml / min then 125 mg / 24 hours then 250 mg / 24 hours then 250 mg / 12 h

19-10 ml / min then 125 mg / 48 h then 125 mg / 24 h then 125 mg / 12 h

<10 ml / min (including hemodialysis and continuous ambulatory peritoneal dialysis) then 125 mg / 48 h then 125 mg / 24 h then 125 mg / 24 h

After hemodialysis or permanent ambulatory peritoneal dialysis, 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 to a very small extent.

Levolete ® P, in the form of a solution for infusions, is injected intravenously drip slowly.
The duration of administration of the drug at a dose of 500 mg (100 ml infusion solution / 500 mg levofloxacin) should be at least 60 minutes.
Levoleth ® P solution is compatible with the following infusion solutions: 0.9% sodium chloride solution, 5% dextrose (glucose) solution, 2.5% Ringer's dextrose solution, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).
The solution of the drug can not be mixed with heparin or solutions with an alkaline reaction (for example, with sodium bicarbonate solution).
With a positive dynamics of the clinical state of the patient after a few days of treatment, it is possible to switch from an intravenous drip to an oral intake of the drug at the same dose.

The duration of treatment, depending on the course of the disease, is no more than 14 days (with the exception of bacterial prostatitis).
As with the use of other antibiotics, treatment with Levoleth ® P is recommended to continue for at least 48-72 hours after the normalization of body temperature or after a reliable eradication of the pathogen.
SIDE EFFECT

The frequency of side effects is classified according to the incidence of the event: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports.

From the hemopoietic system: sometimes - eosinophilia, leukopenia;
rarely - neutropenia, thrombocytopenia; very rarely - pronounced agranulocytosis; in some cases - hemolytic anemia, pancytopenia.
On the part of the digestive system: often - nausea, diarrhea, increased activity of ALT, ACT, dysbacteriosis;
sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders, hyperbilirubinemia; rarely - diarrhea with blood (in very rare cases it can be a sign of inflammation of the intestine or pseudomembranous colitis);very rarely - hepatitis.
From the cardiovascular system: rarely - tachycardia, lowering blood pressure;
very rarely - vascular collapse; in some cases - the extension of the QT interval.
From the central and peripheral nervous system: sometimes - headache, dizziness, drowsiness, sleep disturbances;
rarely - paresthesia in the hands, trembling, anxiety, states of fear, seizures and confusion; very rarely - psychotic reactions such as hallucinations and depressions, movement disorders.
From the senses: very rarely - visual and hearing impairments, smell, taste and tactile sensitivity.

From the side of metabolism: very rarely - hypoglycemia (manifested by a sharp increase in appetite, nervousness, perspiration, tremor);
in some cases - exacerbation of existing porphyria.
From the side of the urinary system: rarely - hypercreatininaemia;
very rarely - deterioration of kidney function up to acute renal failure (for example, due to allergic reactions - interstitial nephritis).
From the musculoskeletal system: rarely - tendon lesions (including tendonitis), joint and muscle pain;
very rarely - a rupture of the tendon (including the rupture of the Achilles tendon, which can be bilateral and manifest within 48 hours after the start of treatment), muscle weakness (is of particular importance for myasthenia patients); in some cases - rhabdomyolysis.
Allergic reactions: sometimes - itching and redness of the skin;
Rarely - anaphylactic and anaphylactoid reactions (manifested by such symptoms as hives, bronchospasm and possible severe suffocation, and - in rare cases - swelling of the face, larynx); very rarely - a sharp decrease in blood pressure, anaphylactic shock;in some cases - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) and exudative erythema multiforme, allergic pneumonitis, vasculitis.
Dermatological reactions: very rarely photosensitization.

Other: sometimes - asthenia;
very rarely - persistent fever, development of superinfection.
Local reactions: often with iv introduction - pain, redness, phlebitis.

CONTRAINDICATIONS

- epilepsy;

- tendon lesions associated with taking quinolones in an anamnesis;

- children and adolescence under 18;

- Pregnancy;

- lactation period (breastfeeding);

- hypersensitivity to levofloxacin or other quinolones;

- Hypersensitivity to the auxiliary components of the drug.

With caution should prescribe the drug in the presence of glucose-6-phosphate dehydrogenase deficiency, in elderly patients (high probability of concomitant decline in kidney function).

PREGNANCY AND LACTATION

The drug is contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with slightly impaired renal function (CK> 50 ml / min) do not need dose adjustment.

Patients with impaired renal function require a correction of the dosing regimen, in accordance with the amount of creatinine clearance.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

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

APPLICATION FOR CHILDREN

Contraindicated: children and adolescence under 18 years.

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients (high probability of concomitant decrease in kidney function).

SPECIAL INSTRUCTIONS

In severe pneumonia caused by Streptococcus pneumoniae, levofloxacin may not be effective.

The introduction should be carried out for at least 60 minutes, during the introduction, palpitations and transient decreases in blood pressure may occur, and there may rarely be a collapse.

With a marked decrease in blood pressure, the administration of levofloxacin is stopped.

If there is a suspected development of pseudomembranous colitis due to Clostridium difficile, treatment with levofloxacin is canceled and appropriate therapy is prescribed.

During treatment, sunlight and artificial ultraviolet irradiation should be avoided to avoid damage to the skin (photosensitization).

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

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 increases with insufficiency of glucose-6-phosphate dehydrogenase.

Impact on the ability to drive vehicles and manage mechanisms

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

OVERDOSE

Symptoms: nausea, erosive lesions of the mucous membranes of the gastrointestinal tract, prolongation of the QT interval, confusion, dizziness, convulsions.

Treatment: symptomatic, dialysis is ineffective.

DRUG INTERACTION

Increases T 1/2 cyclosporine.

The degree of absorption of levofloxacin reduces drugs that depress intestinal motility, sucralfate, antacid drugs containing salts of aluminum and magnesium, as well as preparations containing iron salts (a break between intake of at least 2 hours is necessary).

NSAIDs, theophylline increase convulsive readiness.

GCS increases the risk of rupture of tendons.

Cimetidine and drugs that block tubular secretion slow down excretion.

When used simultaneously with indirect anticoagulants (including warfarin), coagulability should be monitored.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 ° C;
Do not freeze. Shelf life - 2 years.
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