MACLEVO - instructions for use, doses, side effects, contraindications

Levofloxacin is a fluoroquinolone, a broad-spectrum antibacterial agent. The mechanism of action is the inhibition of bacterial topoisomerase IV and DNA gyrase (topoisomerase II), the enzymes necessary for replication, transcription, reduction, and recombination of bacterial DNA.

Antimicrobial activity:

In vitro levofloxacin demonstrates broad antimicrobial activity against Gram-positive and Gram-negative microorganisms.

There is cross-resistance between levofloxacin and other fluoroquinolones, but some microorganisms resistant to other fluoroquinolones are susceptible to levofloxacin.

In vitro and in clinical conditions the drug is most effective against the following microorganisms:

Aerobic Gram-negative microorganisms: Enterobacter cloacae, Legionella pneumoniae, Escherichia coli, Moraxella catarrhalis, Haemophilus influenzae, Proteus mirabilis, Haemophilus parainfluenzae, Pseudomonas aeruginosa, Klebsiella pneumoniae, Acinetobacter baumannii, Klebsiella oxytoca, Bordetella pertussis, Proteus vulgaris, Enterobacter agglomerans, Acinetobacter calcoaceticus, Morganella morganii, Citrobacter diversus, Providencia rettgeri, Citrobacter freundii, Providencia stuartii, Enterobacter aerogenes, Pseudomonas fluorescens, Enterobacter sakazakii, Serratia marcescens.

Aerobic gram positive microorganisms: Enterococcus faecalis (many kinds have a moderate sensitivity), Staphylococcus aureus (methicillin sensitive kinds), Staphylococcus epidermidis (including penicillin resistant strains), Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Viridans group streptococci.

Anaerobic microorganisms: Clostridium perfringens.

Other microorganisms: Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma pneumoniae, Mycoplasma hominis, Ureaplasma urealyticum, Mycobacterium spp., Mycobacterium leprae, Mycobacterium tuberculosis, Rickettsia spp.

Pharmacokinetics:

The pharmacokinetics of levofloxacin is linear. Peak concentration in plasma with intravenous infusion of 500 mg of the drug for 60 min is 6.2 μg / ml. Time to reach the maximum concentration (T_m_Oh) is 1.0 ± 0.1 h, the half-life (T1 / 2) is 6.4 ± 0.7 h. For intravenous single and repeated administration, the apparent volume of distribution after administration of the same dose is 89-112 liters.

It penetrates well into tissues and body fluids: lungs, bronchial mucosa, urogenital system, bone tissue, sputum, cerebrospinal fluid; leukocytes, macrophages.The concentration of levofloxacin in the lung tissue is higher than in plasma, 2-5 times. Connection with blood plasma proteins - 30-40%. A slight cumulation is noted only when 500 mg of levofloxacin is administered twice a day.

Kidney clearance is 70% of the total clearance.

The drug is partially metabolized. In the liver, a small portion is oxidized and / or deacetylated. It is excreted mainly by the kidneys through glomerular filtration and canaliculia secretion. In unchanged form, about 70% of the kidneys are excreted within 24 hours, and 87% in 48 hours; in the form of inactive metabolites is withdrawn less than 5% within 48 hours.

Special groups of patients:

Renal failure. In patients with impaired renal function, the half-life of levofloxacin from plasma is increased, which requires a dose adjustment to avoid cumulation. Levofloxacin It is not eliminated from the body by hemodialysis or prolonged outpatient peritoneal dialysis.

Liver failure. The violation of liver function does not have a significant effect on the metabolism of levofloxacin.

Indications:

Infectious and inflammatory diseases caused by microorganisms sensitive to the preparation:

- ENT organs (including acute maxillary sinusitis);

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

- urinary tract and kidneys (including acute pyelonephritis);

- genital organs;

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

- sepsis;

- intraabdominal infection.

Contraindications:

Individual hypersensitivity to levofloxacin, other quinolones, or individual components of the drug; disorders of the central nervous system (epilepsy, severe form of cerebral atherosclerosis), damage to tendons with previously treated quinolones; pregnancy and lactation; children and adolescence up to 18 years.

Carefully:

Carefully the drug should be used in the elderly due to the high likelihood of concomitant decline in kidney function, with a deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

Intravenous drip slowly, not less than 60 minutes 500 mg (100 ml infusion solution) 1-2 times a day.

In patients with normal renal function with different indications, the following doses of the drug are used:

	Indications	Dose	Duration (days)
1	Infectious diseases of the skin and soft tissues.	500 mg 2 times a day	7-14 days
2	Community-acquired pneumonia	500 mg 1-2 times a day	7-14 days
3	Exacerbation of chronic bronchitis	250-500 mg once a day	7-10 days
4	Acute maxillary sinusitis	500 mg once a day	10-14 days
5	Complicated urinary tract infections (including acute pyelonephritis)	250 mg once a day (in severe cases, the dose can be increased)	7-10days
6	Uncomplicated urinary tract infections	250 mg once a day	3 days
7	Sepsis	500 mg 1-2 times a day	7-14 days
8	Intra-abdominal infection	500 mg once a day (in combination with antibacterial drugs acting on anaerobic flora)	7-14 days

Dosage of the drug in patients with impaired renal function:

Dosing regimen	250 mg / day	500 mg / day	500mg / 12h
Creatinine clearance	Initial dose of 250 mg	Initial dose 50Q mg	Initial dose of 500 mg
50-20 ml / min	Further 125 mg / 24 h	Then 250 mg / 24 h	Further 250 mg / 12 h
19-10 ml / min	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 12 h
<10 ml / min (incl. in hemodialysis and permanent outpatient peritoneal dialysis)	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 24 h

The duration of treatment depends on the type and severity of the course of the disease, the maximum duration is 14 days.After reducing the symptoms of acute inflammation and normalizing the temperature, levofloxacin therapy continues for at least 48-72 hours. Then you can go on taking the drug inside at the same dose, considering the equivalence of both ways of administration

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

Side effects:

From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis; increased activity of "hepatic" transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

From the side of the cardiovascular system: lowering blood pressure, cardiovascular collapse, lengthening of the interval QT, tachycardia, extremely rare-ciliary arrhythmia.

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

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

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

From the side of the musculoskeletal system: arthralgia, myalgia, tendon rupture, muscle weakness, rhabdomyolysis, tendonitis.

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

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

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

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

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

Overdose:

Symptoms: confusion, dizziness, convulsions, gastrointestinal disorders (eg, nausea) and erosive lesions of the mucous membranes, lengthening of the interval QT.

Treatment: symptomatic, dialysis is not effective.

Interaction:

Levofloxacin increases half-life cyclosporine.

The excretion of levofloxacin slows down under the action of cimetidine, probenecid and drugs that block the tubular secretion.

Non-steroidal anti-inflammatory drugs and theophylline: when used with levofloxacin increase convulsive readiness.

With simultaneous application antagonists of vitamin K it is necessary to control the coagulability of the blood.

Glucocorticosteroids: increase the risk of rupture of tendons.

Antidiabetic drugs: Strict control over the level of glucose in the blood is necessary, since there is a possibility of hyper- and hypoglycemia while using them with levofloxacin.

The solution for intravenous administration is compatible with 0.9% solution NaCl, 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:

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

When there are signs of tendonitis levofloxacin immediately cancel.

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

If insufficiency of glucose-6-phosphate dehydrogenase increases the risk of hemolysis.

If there is a suspicion of pseudomembranous colitis, levofloxacin should be immediately canceled, and the patient should be given appropriate therapy.

In patients receiving quinolone therapy, including levofloxacin, in rare cases, reactions of immediate hypersensitivity, up to anaphylaxis, were noted. If after receiving levofloxacin appears pruritus or other signs of immediate hypersensitivity, the drug should be discontinued. Although levofloxacin and more soluble than other quinolones, patients should conduct adequate hydration of the body.

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

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for infusions 5 mg / ml.

Packaging:100 ml into a bottle of low-density polyethylene using FFS technology (formation - filling - sealing). The sealed nose of the bottle is covered with a cap made of the same material.

1 bottle in a bag of sealed plastic is placed together with instructions for use in a cardboard pack.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004668/09

Date of registration:10.06.2009

The owner of the registration certificate:McLeodz Pharmaceuticals Co., Ltd. McLeodz Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

MARCK BIOSCIENCES, Ltd. India

Representation: & nbspAdvansd Trading, OOOAdvansd Trading, OOO

Information update date: & nbsp12.10.2015

Illustrated instructions

Instructions

MACLEVO® (Maclevo®)