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

Fluoroquinolone, an antibacterial (bactericidal) remedy of a wide spectrum of action. It blocks DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, inhibits DNA synthesis, causes morphological changes in the cytoplasm, cell wall and bacterial membranes.

Effective with respect to:

aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcuscus spp. (incl. Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp., coagulase-negative and methicillin-sensitive strains (including moderately sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus spp. (leukotoxin-containing); Streptococcus spp. (groups C and G), Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-sensitive, moderately sensitive, resistant strains), Streptococcus pyogenes, Streptococcus 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 t.h. Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive, resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (at t.h. Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (producing and non-reducing beta-l acts aza strains), Morganella morganii, Neisseria gonorrhoeae (producing and non-reducing penicillinase strains), Neisseria meningitidis, Pasteurella spp. (at t.h. Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (at t.h. Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (at t.h. Pseudomonas aeruginosa), Serratia spp, (at t.h. Serratia marcescens), Salmonella spp .;

anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veillonella 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.

Moderately sensitive microorganisms (the minimum suppressive concentration is more than 4 mg / l):

aerobic Gram-positive microorganisms: Corynebacterium urealylicum, 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. (coagulasethe methicillin-resistant strains).

aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.

others microorganisms: Mycobacterium avium.

Pharmacokinetics:

After intravenous (iv) infusion of 500 mg for 60 minutes, the maximum concentration in the blood plasma (C_m_a_x) - 6.2 μg / ml. With iv in a single and repeated administration, the apparent volume of distribution after administration of the same dose is 89-112 L, C_max_- 6.2 μg / ml, half-life (T1 / 2) - 6.4 hours.

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 clearance. T1/ 2 - 6-8 hours.

It is excreted from the body mainly by the kidneys through glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form with urine within 24 hours 70% are deduced and in 48 hours - 87%; in the stool for 72 hours 4% of the dose taken internally is detected.

Indications:

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

- community acquired pneumonia;

- complicated kidney and urinary tract infections, including pyelonephritis;

- uncomplicated urinary tract infections;

- bacterial prostatitis;

- septicemia / bacteremia associated with the above indications;

- intra-abdominal infection;

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

Contraindications:

-hypersensitivity (including other drugs of the quinolone group);

-epilepsy;

- the damage of tendons during the previous treatment with quinolones;

-baby and adolescence (up to 18 years);

-pregnancy;

-period of lactation;

-longitudinal interval Q-T;

-hypokalemia;

-the reception of antiarrhythmic drugs IA class (quinidine, procainamide) or III class (amiodarone, sotalol).

Carefully:

Elderly people due to the high likelihood of concomitant decline in kidney function, with a deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

Intravenous, drip, slow.

The duration of administration of 500 mg (100 ml infusion solution) should be at least 60 minutes 1-2 times a day. The duration of treatment depends on the type and severity of the course of the disease, the course of treatment is 7-14 days. After reducing the symptoms of acute inflammation and normalizing the temperature, levofloxacin therapy continues for at least 48-72 hours. Depending on the patient's condition after a few days of treatment, it is possible to switch to taking the drug inside at the same dose, considering the equivalence of both routes of administration.

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

Indications	Daily dose	Duration course
Community-acquired pneumonia	500 mg 1-2 times a day	7-14 days
Complicated urinary tract infections (including pyelonephritis)	250 mg once a day (in case of severe disease, the dose should be increased)	7-10 days
Uncomplicated urinary tract infections	250 mg once a day	3 days
Bacterial prostatitis	500 mg once a day	28 days
Septicemia / bacteremia	For 500 mg 1 -2 times a day	10-14 days
Intra-abdominal infection	500 mg once a day (in combination with antibacterial drugs acting on anaerobic flora).	7-14 days
Complex therapy of drug-resistant forms of tuberculosis	For 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, ml / min	Dosages for intravenous administration
	250 mg / 24 h	500 mg / 24 h	500 mg / 12 h
	Initial dose of 250 mg	Initial dose of 500 mg	Initial dose of 500 mg
50-20	Further 125 mg / 24 h	Then 250 mg / 24 h	Further 250 mg / 12 h
19-10	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 12 h
<10 (including hemodialysis and continuous outpatient peritoneal dialysis)	Further 125 mg / 48 h	Further 125 mg / 24 h	Further 125 mg / 24 h

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

Do not require dose adjustment in patients with impaired liver function.

Side effects:

On the part of the digestive system: nausea, vomiting, diarrhea (including with blood), decreased appetite, abdominal pain, pseudomembranous colitis; increased activity of "hepatic" transaminases, hyperbilirubinemia, hepatitis, dysbacteriosis.

From the cardiovascular system (CVS): lowering blood pressure (BP), lengthening the interval Q-T, cardiovascular collapse, tachycardia, extremely rare - atrial fibrillation.

On the part of metabolism: hypoglycemia (increased appetite, sweating, nervousness, trembling).

From the side of the nervous system: headache, dizziness and / or numbness, weakness, drowsiness, insomnia, paresthesia, anxiety, fear, hallucinations, confusion, depression, movement disorders, convulsions.

From the senses: visual, hearing, smell, taste and tactile sensitivity.

From the musculoskeletal system: arthralgia, myalgia, myasthenia gravis, rupture of tendons, rhabdomyolysis, tendonitis.

From the side of the urinary system: hypercreatininaemia, interstitial nephritis.

On the part of the organs of hematopoiesis: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

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

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

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

Overdose:

Symptoms: gastrointestinal disorders (nausea), erosive lesions of the mucous membrane of the gastrointestinal tract (GIT), change in the interval Q-T, confusion, dizziness, convulsions.

Treatment: symptomatic therapy, dialysis is ineffective, a specific antidote is unknown.

Interaction:

The drug increases T1 / 2 cyclosporine.

Compatible with 0.9% sodium chloride solution, 5% dextrose solution, 2.5% Ringer's solution with dextrose, combined solutions for parenteral nutrition.

With the simultaneous use of vitamin K antagonists, control over the blood coagulation system is necessary.

Cimetidine and drugs that block tubular secretion slow down excretion.

The drug solution can not be mixed with heparin and solutions that have an alkaline reaction (for example, with sodium bicarbonate solution).

Hypoglycemic drugs: a strict control of the concentration of glucose in the blood, as there is a possibility of hyper- and hypoglycemia while using them with levofloxacin.

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

Glucocorticosteroids (GCS): increase the risk of rupture of tendons.

Special instructions:

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

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

In patients who received quinolone therapy, including levofloxacin, in rare cases, hypersensitivity reactions of immediate type were noted, up to anaphylaxis. If after the levofloxacin appears pruritus or other signs of immediate type hypersensitivity, the drug should be discontinued.

If pseudomembranous colitis is suspected, levofloxacin should be immediately discontinued and appropriate treatment initiated. In such cases, drugs that depress intestinal motility should not be used.

Rarely observed with the use of the drug tendonitis (primarily, inflammation of the Achilles tendon) can lead to rupture of tendons. The elderly are more prone to tendinitis.Treatment with glucocorticosteroids increases the risk of rupture of tendons. If suspicion of tendonitis should immediately stop treatment with levofloxacin and begin appropriate treatment of the affected tendon, for example, providing him with a resting state.

Patients with insufficiency of glucose-6-phosphate dehydrogenase can react to fluoroquinolones by destruction of erythrocytes (hemolysis). In this regard, treatment of such patients with levofloxacin should be carried out with great care.

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

Such side effects of levofloxacin as dizziness or stupor, drowsiness, and visual impairment may impair the ability to respond quickly and to concentration, which is a risk in situations where these abilities are of particular importance (for example, when driving, servicing machines and mechanisms, when performing work in an unstable situation).

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

Packaging:

100 ml in bottles of glass with a capacity of 100 ml.

Bottle with instructions for use in a pack of cardboard.

For hospital:

- 12 bottles of 100 ml without packs with 12 instructions for use are placed in a box of corrugated cardboard.

- 1 bottle with instructions for use (from 1 to 12 bottles with an equal number of instructions for use) without a bundle in a box of corrugated cardboard.

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-001900/10

Date of registration:15.11.2012

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp29.09.2015

Illustrated instructions

Instructions

Levofloxacin (Levofloxacin)