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

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 of microorganisms.

Levofloxacin is active against most strains of microorganisms both in conditions in vitro and in vivo, in vitro:

Sensitive microorganisms (minimum inhibitory concentration (MIC) ≤ 2 mg / ml).

Aerobic Gram-positive microorganisms: Withrynebacterium diphtheriae. Enterococcus spp., Including. Enterococcus faecalis; Listeria monocytogenes; Staphylococcus spp. (including coagulase-negative methicillin-sensitive / moderately sensitive), Staphylococcus aureus (methicillin-sensitive), Staphylococcus epidermidis (methicillin-sensitive); Streptococci groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive / moderately sensitive / resistant), Streptococcus pyogenes, Streptococci groups Viridans.

Aerobic Gram-negative microorganisms: Acinetobacter spp., Including. Acinetobacter baumannii; Actinobacillus actinomycetemcomitans; Citrobacter freundii; Eikenella corrodens; Enterobacter spp., Including. Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae; Escherichia coli; Gardnerella vaginalis; Haemophilus ducreyi, Haemophilus influenzae (ampicillin sensitive / resistant), Haemophilus parainfluenzae; Helicobacter pylori; Klebsiella spp., Including. Klebsiella oxytoca, Klebsiella pneumoniae; Moraxella catarrhalis, Morganella morganii; Neisseria gonorrhoeae (not producing penicillinase). Neisseria meningitidis; Pasteurella spp., at t. h. Pasteurella conies, Pasteurella dagmatis, Pasteurella multocida; Proteus mirabilis, Proteus vulgaris; Providencia spp., at t. h. Providencia rettgeri, Providencia stuartii; Pseudomonas spp., at t. h. Pseudomonas aeruginosa; Salmonella spp .; Serratia marcescens; Serratia 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 spp., at t. h. Legionella pneumophila; Mycobacterium spp., at t. h. Mycobacterium leprae, Mycobacterium tuberculosis; Mycoplasma hominis. Mycoplasma pneumoniae; Rickettsia spp., Ureaplasma urealylicum.

Levofloxacin is moderately active (MIC> 4 mg / L):

Aerobic Gram-positive microorganisms: Corynebacterium urealylicum, Corynebacterium xerosis; Enterococcus faecium; Staphylococcus epidermidis (methicillin-resistant); Staphylococcus haemolyticus (methicillin-resistant).

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

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

To levofloxacin are stable (IPC ≥8 mg / l):

Aerobic Gram-positive microorganisms: Corynebacterium jeikeium; Staphylococcus aureus (methicillin-resistant), Staphylococcus spp. Coagulase-negative (methicillin-resistant).

Aerobic Gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

After intravenous infusion of levofloxacin at a dose of 500 mg for 60 min, the maximum plasma concentration is 6.2 μg / ml.

With intravenous single and repeated administration, the apparent volume of distribution after administration of the same dose is 89-112 liters.

The connection with plasma proteins is 30-40%. It penetrates well into organs and tissues - lungs, bronchial mucosa, sputum, organs of the genitourinary system, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

Metabolism and excretion: 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 is 6.4 hours.

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

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

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

- ENT organs (including acute sinusitis);

- urinary tract and kidneys (including acute pyelonephritis);

- bacterial chronic prostatitis;

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

- septicemia / bacteremia;

- intra-abdominal infections;

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

Contraindications:

- Hypersensitivity (incl. To other quinolones);

- epilepsy;

- lesions of the tendon during the previous treatment with quinolones;

- children and adolescence (growth period) to 18 years;

- pregnancy;

- lactation period.

Carefully:In the elderly (due to the high probability of concomitant decline in kidney function), with a deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

The drug is administered intravenously drip slowly, at least 60 minutes, 250-500 mg 1-2 times a day. Doses are determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility.

Dosing of the drug in patients with normal renal function (creatinine clearance> 50 ml / min).

- Acute antritis: 500 mg once a day, for 10-14 days.

- Community-acquired pneumonia: 500 mg 1-2 times a day, for 7-14 days.

- Exacerbation of chronic bronchitis: 250-500 mg once a day; within 7-10 days.

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

- Complicated urinary tract infections (including pyelonephritis): 250 mg I once a day (with a heavy course of the disease, the dose should be increased), 7-10 days.

- Bacterial chronic prostatitis: 500 mg once a day, 28 days.

- Infectious diseases of the skin and soft tissues: 500 mg twice a day, for 7-14 days.

- Septicemia / bacteremia: 500 mg 1-2 times a day, for 7-14 days.

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

- Complex therapy of drug-resistant forms of tuberculosis - 500 mg 1-2 times a day, up to 3 months.

Dosing of the drug in patients with impaired renal function (creatinine clearance <50 ml / min).

Clearance creatinine	Dosages for intravenous administration
Clearance creatinine	250 mg / 24 hour	500 mg / 24 hour	500 mg / 12 hour
	First dose: 250 mg	First dose: 500 mg	First dose: 500 mg
20-50 ml / min	Then: 125 mg / 24 hour	Then: 250 mg / 24 hour	Then: 250 mg / 12 hour
10-19 ml / min	Then: 125 mg / 48 hour	Then: 125 mg / 24 hour	Then: 125 mg / 12 hour
<10 ml / min (including hemodialysis and CAPD *)	Then: 125 mg / 48 hour	Then: 125 mg / 24 hour	Then: 125 mg / 24 hour

* after hemodialysis or long-term outpatient peritoneal dialysis (DAPD), no additional doses are required.

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: lowering blood pressure, cardiovascular collapse, tachycardia, atrial fibrillation, lengthening of the interval QT.

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

From the nervous system: headache, dizziness, weakness, drowsiness, insomnia, tremor, anxiety, paresthesia, fear, hallucinations, fright and awn of consciousness, depression, movement disorders, seizures, epileptic seizures (in predisposed patients).

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: 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.

Local reactions: pain, redness at the injection site, phlebitis.

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

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.

Interaction:

Increases the half-life of cyclosporine.

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.

Levofloxacin infusion solution is compatible with 0.9 % solution of sodium chloride, 5% dextrose solution, 2.5% Ringer's solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).

Do not mix with heparin and solutions that have an alkaline reaction.

Special instructions:

After normalization of body temperature, it is recommended to continue treatment with less than 48-72 hours.

The duration of intravenous infusion of 500 mg (100 ml infusion solution) should be at least 60 minutes.

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

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 trauma) may develop seizures,when insufficiency of glucose-6-phosphate dehydrogenase - the risk of hemolysis.

In the course of therapy, one should remember about the possibility of developing superinfection.

When levofloxacin is combined with vitamin K antagonists, control over the parameters of the blood coagulation system is necessary.

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 requiring increased attention and speed of psychomotor reactions.

Form release / dosage:Solution for infusions 5 mg / ml.

Packaging:

100 ml in plastic bottles. Bottles are sealed in polyethylene bags, which will interfere with the cardboard pack together with instructions for use.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-002475/10

Date of registration:26.03.2010 / 01.09.2016

Expiration Date:Unlimited

The owner of the registration certificate:M.Biotek LimitedM.Biotek Limited United Kingdom

Manufacturer: & nbsp

MARCK BIOSCIENCES, Ltd. India

Representation: & nbspSharan Pharma, LLCSharan Pharma, LLC

Information update date: & nbsp04.03.2018

Illustrated instructions

Instructions

Lefsan (Lefsan)