Levot P - instructions for use, dose, side effects, contraindications

Excipients: microcrystalline cellulose (Avicel PH 101), corn starch, silicon dioxide colloid, crospovidone, hypromellose (15 cps), microcrystalline cellulose (Avicel PH 102), magnesium stearate.

Sheath: dyeing powder Opadrai white OY 58900 (hypromellose 5 cP, titanium dioxide, macrogol 400).

Description:

Tablets 250 mg - white or almost white capsular biconvex tablets coated with a film sheath, embossed "RDY"on one side, on the other -" 279 ".

Tablets 500 mg - white or almost white capsular biconvex tablets covered with a film sheath, embossed "RDY" on one side, on the other side - "280".

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Fluoroquinolone, a broad-spectrum antimicrobial bactericide. 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, as in conditions in vitro, and in vivo.

Sensitive microorganisms (MPK≤2 mg / ml).

Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp., Listeria monocytogenes, Staphylococcus coagulase-negative methi-S(I) (methicillin-sensitive / moderately sensitive strains), Staphylococcus aureus methi-S (methicillin-sensitive strains), Staphylococcus epidermidis methi-S (methicillin-sensitive strains), Staphylococcus spp. (CNs - leukotoxin-containing). Streptococci groups FROM and G (including, Streptococcus agalactiae, Streptococcus pneumoniae peni-S/1/R (penicillin-sensitive / moderately sensitive / resistant strains)), Streptococcus pyogenes, Viridans streptococci peni-S/R (penicillin-sensitive / resistant strains).

Aerobic Gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp., Actinobacillus actinomycetemcomitcms, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (including, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampi-S/R (ampicillin-sensitive / resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including, Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis β+β- (producing and non-β-lactamase-producing strains), Morganella morganii, Neisseria gonorrhoeae non-PPNG/PPNG (penicillinase-producing and non-producing penicillinase strains), Neisseria meningitidis, Pasteurella spp. (at Tom number of, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (at Tom number of, Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (at Tom number of, Pseudomonas aeruginosa), Serratia spp. (at Tom number of, Salmonella spp., 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, Legionella spp., Mycobacterium spp. (at Tom number of, Mycobacterium leprae, Mycobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae), Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive microorganisms (MPK≥4 mg / l):

Aerobic Gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis methi-R (methicillin-resistant strains), Staphylococcus haemolyticus methi-R (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.

Stable microorganisms (IPC≥8 mg / l):

Aerobic Gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus methi-R (methicillin-resistant strains), Staphylococcus coagulase-negative methi-R (coagulase-negative methicillin-resistant strains).

Aerobic Gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

When ingested quickly and almost completely absorbed (eating little influence on speed and completeness of absorption).

Bioavailability is 99%. The time to reach the maximum concentration (T_m_Oh) - 1-2 hours; at reception 250 and 500 mg the average size of the maximum concentration (With_m_Oh) is 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.

It is excreted from the body mainly by the kidneys through glomerular filtration and tubular secretion. The half-life (T1/2) - 6-8 hours. Kidney clearance is 70% of the total clearance. Less than 5% of levofloxacin is excreted as metabolites. AT urine, for a period of 24 hours, is unchanged 70%, and for 48 hours - 87% of the dose taken internally. In stool, for a period of 72 hours, 4% of the dose taken internally is detected.

In renal failure, the decrease in clearance of the drug and its excretion by the kidneys depends on the degree of decrease in the clearance of creatinine (CC).

Indications:

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

- infection of the ENT organs (acute sinusitis);

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

- infections of the skin and soft tissues;

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

- complicated kidney and urinary tract infections, including pyelonephritis;

- uncomplicated urinary tract infections;

- prostatitis;

- septicemia / bacteremia associated with the above indications;

- intra-abdominal infections.

Contraindications:

- hypersensitivity to levofloxacin or other quinolones;

- epilepsy;

- affections of tendons associated with taking quinolones in anamnesis;

- children and adolescents under 18;

- pregnancy;

- lactation period (breastfeeding).

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 liquid.

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

Patients with normal or slightly impaired renal function (CK> 50 ml / min) the drug is recommended to be administered in the following doses.

Sinusitis: 500 mg once a day. The course of treatment is 10-14 days.

Exacerbation of chronic bronchitis: on 250-500 mg 1 time / sut. The course of treatment is 10-14 days.

Community-acquired pneumonia: 500 mg 1-2 times / day. The course of treatment is 7-14 days.

Uncomplicated urinary tract infections: 250 mg once a day. The course of treatment is 3 days.

Complicated urinary tract infections (including pyelonephritis): 250 mg once a day. The course of treatment is 7-10 days.

Prostatitis: 500 mg once a day. The course of treatment is 28 days.

Septicemia / bacteremia: 500 mg 1-2 times / day. The course of treatment is 10-14 days.

Intraabdominal infection: 500 mg once a day. The course of treatment is 7-14 days, in combination with antibacterial drugs acting on anaerobic flora.

Infections of the skin and soft tissues: 250 mg 1-2 times / day or 500 mg 1 time / day. The course of treatment is 7-14 days.

In the composition complex therapy of drug-resistant forms of tuberculosis 500-1000 mg of levofloxacin 1 time / day. The course of treatment is up to 3 months.

Application for violations of kidney function

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

Creatinine clearance	Doses for oral administration
	250 mg / 24 h	500 mg / 24 h	500 mg / 12 h
	the first dose of 250 mg	the first dose of 500 mg	the first dose of 500 mg
50-20 ml / min	then 125 mg / 24 h	then 250 mg / 24 h	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

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

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

Application for violations of liver function

If the liver function is not required, a special dose selection is required, since levofloxacin is metabolized in the liver slightly.

The duration of treatment, depending on the course of the disease, is no more than 14 days. As with the use of other antibiotics, treatment with Levoleth® R 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 effects:

The incidence of side effects is classified according to the incidence of the event: often (1-10: 100), sometimes (less than 1: 100), rarely (less than 1: 1000), very rarely (less than 1:10 000), in some cases .

On the part of the blood system and hemopoiesis: sometimes - eosinophilia, leukopenia; rarely - neutropenia, thrombocytopenia; very rarely - pronounced agranulocytosis; in some cases - hemolytic anemia, pancytopenia.

From the digestive system: often - nausea, diarrhea, increased activity of alanine aminotransferase (ALT), aspartate aminotransferase (ACT), dysbiosis; sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders, increased serum bilirubin levels; rarely - diarrhea with an admixture of 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 - lengthening the interval QT.

From the central and peripheral nervous system: sometimes - headache, dizziness, stiffness of movements, drowsiness, sleep disturbance; rarely - paresthesia in the hands, trembling, anxiety, states of fear, convulsions, confusion; very rarely - psychotic reactions such as hallucinations and depressions, movement disorders.

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

From the side of metabolism: very rarely - hypoglycemia (manifested by a sharp increase in appetite, nervousness, perspiration,trembling); in some cases - exacerbation of existing porphyria.

From the urinary system: rarely - increased serum creatinine levels; 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 damage (including tendonitis), joint and muscle pain; very rarely - rupture of the Achilles tendon (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 sudden 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.

From the skin and subcutaneous fat: very rarely photosensitization.

Other: sometimes - asthenia; very rarely - persistent fever, development of superinfection.

Overdose:

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

Treatment: symptomatic, dialysis is ineffective.

Interaction:

Increases the half-life of cyclosporine.

Completeness of absorption is reduced by drugs that depress intestinal motility, sucralfate, antacid medicines containing salts of aluminum and magnesium, as well as preparations containing iron salts (a break between taking at least 2 hours is necessary). Non-steroidal anti-inflammatory drugs, theophylline increase convulsive readiness, glucocorticosteroids increase the risk of rupture of tendons. Cimetidine and drugs that block tubular secretion, slow down excretion.

Special instructions:

Treatment with levofloxacin is recommended to continue for at least 48-72 hours after the normalization of body temperature or after a reliable eradication of the pathogen.

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

When there are signs of tendonitis, pseudomembranous colitis levofloxacin immediately cancel.

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

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:Film-coated tablets, 250 mg or 500 mg.

Packaging:

For 10 tablets in PVC / aluminum blister. One blister along with instructions for use are packed in a cardboard pack.

Storage conditions:In a dry, protected from light 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:LSR-005809/09

Date of registration:17.07.2009

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp12.10.2015

Illustrated instructions

Instructions

Levoleth® Р (Levolet® R)