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

Excipients: dextrose anhydrous 5.0 g (5%), hydrochloric acid 0.113 ml, water for injection q.s. up to 100 ml, hydrochloric acid q.s., sodium hydroxide q.s.

Description:Transparent solution from yellow to greenish-yellow color.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Levofloxacin is a synthetic broad-spectrum antibacterial agent from the group of fluoroquinolones, containing as an active substance; levofloxacin - the left-handed isomer of ofloxacin.

Levofloxacin blocks the DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and bacterial membranes.

Levofloxacin is active against most strains of microorganisms in vitro and in vivo.

Sensitive microorganisms GMPK <2 mg / ml):

Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulase- negative methicillin-sensitive / -residually sensitive, Staphylococcus aureus methicillin-sensitive, Staphylococcus epidermidis methicillin-sensitive, Staphylococcus spp (CNS), Streptococci group C and G, Streptococcus agalactiae, Streptococcus pneumoniae penicillin-sensitive / -residually sensitive / -resistant, Streptococcus pyogenes, Viridans streptococci penicillin-sensitive / -resistant.

Aerobic Gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter spp, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampicillin-sensitive / -resistant, Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxella catarrhalis β+/β-, Morganella morganii, Neisseria gonorrhoeae (including those producing penicillinase), Neisseria meningitidis, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella spp, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp, Pseudomonas aeruginosa, Pseudomonas spp, Salmonella spp, Serratia marcescens, Serratia spp.

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp, Clostridium perfringens, Fusobacterium spp, Peptostreptococcus, Propionibacterium spp, Veilonella spp.

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

Moderately sensitive (MIC> 4 mg / l):

Aerobic Gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis methicillin-resistant, Staphylococcus haemolyticus methicillin-resistant.

Aerobic Gram-negative microorganisms: Burkholderia cepacia, Campilobacter jejuni/coli.

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

Sustainable (IPC >8 mg/l):

Aerobic Gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus methicillino-resistant, Staphylococcus coagulase-negative methicillino-resistant.

Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

Pharmacokinetic characteristics after a single dose of 500 mg of levofloxacin in / in, respectively, are: C max. - 6.2 ± 1.0 μg / ml, T max. - 1.0 ± 0.1 h, half-life 6.4 ± 0.7 h. The pharmacokinetics of levofloxacin are linear in single and multiple administration of the drug. The plasma profile of the concentrations of levofloxacin after intravenous administration is similar to that of tablets. Therefore, oral and intravenous routes of administration may be considered interchangeable.

The average volume of distribution of levofloxacin averages from 89 to 112 liters after a single and multiple IV administration of 500 mg.

Levofloxacin is excreted in the urine in an unchanged form. The average final half-life of levofloxacin is 6 to 8 hours after single and multiple administration.

With renal failure, a decrease in the clearance of the drug and. its excretion through the kidneys depends on the degree of decrease in the clearance of creatinine.

Indications:

Infectious-inflammatory diseases caused by micro-organisms that are sensitive to Elephlox:

community acquired pneumonia;

complicated urinary tract infections (including pyelonephritis); uncomplicated urinary tract infections;

chronic bacterial prostatitis;

septicemia / bacteremia associated with the above indications;

intra-abdominal infections (in combination with drugs acting on anaerobic microflora);

complex therapy of drug-resistant forms of tuberculosis.

Contraindications:

- hypersensitivity to levofloxacin or other quinolones;

- epilepsy;

- lesions of tendons during previous treatment with fluoroquinolones;

- children and adolescence (up to 18 years);

- pregnancy and lactation.

Carefully:

With caution, 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:

The infusion solution of Eleflox is administered once or twice a day. Doses are determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility. Patients with a creatinine clearance> 50 mL / min are recommended the following dosing regimen:

- Community-acquired pneumonia: 500 mg each Elelix 1-2 times a day - 7-14 days;

- Complicated urinary tract infections (including pyelonephritis): 250 mg each Elefox once a day (in case of severe infections, an increase in the dose is possible) - 7-10 days;

- uncomplicated urinary tract infections: 250 mg Elelixx once a day - 3 days;

- chronic bacterial prostatitis: 500 mg Eleflox once a day - 28 days, after iv introduction after a few days, it is possible to switch to oral administration at the same dose;

- septicemia / bacteremia: 500 mg Elelix 1-2 times a day - 10-14 days;

- intra-abdominal infection: by 500 mg Eleflox once a day - 7-14 days (in combination with antibacterial drugs acting on anaerobic flora);

- complex therapy of drug-resistant forms of tuberculosis: 500 mg Elelix 1-2 times a day - up to 3 months, after iv introduction after a few days, it is possible to switch to oral administration at the same dose.

Eleflox is excreted mainly through the kidneys, so when treating patients with impaired renal function, it is required to reduce the dose of the drug:

Clearance creatinine	Dosing regimen
	250 mg / 24 h	500 mg / 24 h	500 mg / 12 h
	the original dose: 250 mg	the original dose: 500 mg	the original dose: 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 / 12h
<10 ml / min (including hemodialysis and CAPD¹	then: 125 mg / 48 h	then: 125 mg / 24 h	then: 125 mg / 24 h

¹after hemodialysis or permanent ambulatory peritoneal dialysis (CAPD) does not require the introduction of additional doses.

If there is a violation of the liver function, there is no need to change the dosage regimen, since Elephlox is metabolized to a small extent in the liver.

The infusion solution of Eleflox is administered intravenously drip slowly. Duration of infusion of 100 ml of Eleflox solution (1 bottle) should be at least 60 minutes (see "Special instructions"). Depending on the patient's condition after a few days of treatment, it is possible to switch from intravenous drip administration to taking the same dose of the drug in a form intended for oral administration.

The Eleflox solution for infusions is compatible with the following infusion solutions: 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).

Solution Eleflox 500 mg / 100 ml can not be mixed with heparin or solutions that have an alkaline reaction (for example, with sodium bicarbonate solution).

As with other antibiotics, drug treatment it is recommended to continue for at least 48-72 hours after the normalization of body temperature or after a reliable destruction of the pathogen.

Side effects:

Frequency	The appearance of side effects
often:	in 1-10 patients out of 100
infrequently:	less than 1 patient out of 100
rarely:	less than 1 patient out of 1,000
rarely:	less than 1 patient out of 10 000
in some cases:	less than 1 patient out of more than 10 000

Skin reactions and general hypersensitivity reactions

Infrequently: itching and redness of the skin.

Rarely: general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, bronchospasm and laryngospasm.

In very rare cases: swelling of the skin and mucous membranes (for example, in the face and pharynx), sudden drop in blood pressure and shock; increased sensitivity to solar and ultraviolet radiation (see "Special instructions"); allergic pneumonitis; vasculitis.

In some cases: severe skin rashes with the formation of blisters, for example, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), and exudative erythema multiforme. Common hypersensitivity reactions can sometimes be preceded by lighter skin reactions. The above reactions may develop after the first dose through a few minutes or hours after the administration of the drug.

Action on the gastrointestinal tract and metabolism

Often: nausea, diarrhea.

Infrequently: loss of appetite, vomiting, abdominal pain, digestive disorders.

Rarely: diarrhea (including blood), which in very rare cases can be a sign of inflammation of the intestine and even pseudomembranous colitis (see section "Special instructions").

Rarely: decrease in concentration glucose in the blood (hypoglycemia), which is of particular importance for diabetics, with symptoms: increased appetite, nervousness, sweating, trembling.

The experience with the use of other quinolones indicates that they are capable of exacerbating porphyria (a very rare metabolic disease) in patients already suffering from this disease. A similar effect is not excluded even when using Eleflox.

Action on the nervous system

Infrequently: headache, dizziness and / or stupor, drowsiness, insomnia, "nightmarish" dreams.

Rarely: depression, anxiety, psychotic reactions (for example, with hallucinations), unpleasant sensations (for example, paresthesia in the hands), tremor, weakness, agitation, motor disorders, convulsions, confusion, peripheral sensory neuropathy, peripheral sensory-motor neuropathy, dyskinesia, extrapyramidal disorders, fear, agitation, mental disorders with behavioral disorders with self-harm, suicidal thoughts, suicidal attempts.

Rarely: visual and hearing impairments, ringing in the ears, violation of taste sensitivity and smell, a decrease in tactile sensitivity.

Action on the cardiovascular system

Rarely: sinus tachycardia, lowering blood pressure.

Rarely: (shock-like) vascular collapse.

In some cases: extension of the QT interval.

Action on muscles, tendons and bones

Rarely: affections of tendons (including tendonitis), joint and muscle pain.

Rarely: a rupture of tendons (for example, the Achilles tendon) can develop from both sides within 48 hours after initiation of treatment (see also section "Special instructions"); muscle weakness, which has special significance for patients suffering from asthenic bulbar paralysis.

In some cases: muscle damage (rhabdomyolysis).

Action on the liver and kidneys

Often: increased activity of liver enzymes (eg, alanine aminotransferase and aspartate aminotransferase).

Rarely: an increase in the concentration of bilirubin and creatinine in the blood serum (a sign of decreased liver or kidney function).

Rarely: impaired liver function (eg, hepatitis, acute liver failure); impairment of kidney function up to acute renal failure, for example, due to allergic reactions (interstitial nephritis).

Action on the blood

Infrequently: an increase in the number of eosinophils, a decrease in the number of leukocytes.

Rarely: neutropenia; thrombocytopenia, which may be accompanied by increased bleeding.

Rarely: agranulocytosis and the development of severe infections (persistent or relapsing fever, sore throat and persistent deterioration of health).

In some cases: hemolytic anemia; pancytopenia.

Other side effects

Often: pain, redness at the injection site and phlebitis.

Infrequently: general weakness (asthenia).

Rarely: fever, dyspnea.

Any antibiotic therapy can cause changes in the microflora (bacteria and fungi), which is normally present in humans, secondary infection or superinfection, which may require additional treatment.

Overdose:

Symptoms: manifested primarily from the central nervous system (confusion, dizziness, impaired consciousness and seizures like epileptic seizures). In addition, there may be gastrointestinal disorders (eg, nausea) and erosive lesions of the gastrointestinal mucosa, prolongation of the QT interval.

Treatment: symptomatic. Levofloxacin is not excreted by dialysis (hemodialysis, peritoneal dialysis and permanent peritoneal dialysis). There is no specific antidote.

In connection with the possible prolongation of the QT interval, ECG monitoring should be performed.

Interaction:

Quinolones in combination with other drugs (for example, with theophylline, fenbufen or similar non-steroidal anti-inflammatory drugs) can cause a marked decrease in the threshold of convulsive activity.

The use of glucocorticosteroids increases the risk of rupture of tendons.

When used simultaneously with indirect anticoagulants, Coumarin derivatives require control over the blood coagulation system.

Excretion (renal clearance) Levofloxacin is slowed by cimetidine and probenecid. It should be noted that this interaction practically has no clinical significance. Nevertheless, with the simultaneous use of drugs such as probenecid and cimetidine blocking a certain way of excretion (tubular secretion), treatment with levofloxacin should be done with caution. This concerns, first of all, patients with impaired renal function. Levofloxacin increases the half-life of cyclosporine.

Eleflox, like other fluoroquinolones, should be used with caution in combination with medications,causing an elongation interval QT (for example: antiarrhythmic medicines of a class IA and III, tricyclic antidepressants, macrolides, neuroleptics).

Special instructions:

Eleflox can not be used to treat children and adolescents because of the risk of joint cartilage damage.

In the treatment of elderly patients, it should be borne in mind that they often have impaired renal function (see section "Method of administration and dose").

In severe community-acquired pneumonia caused by Streptococcus pneumoniae, levofloxacin may not provide the optimal therapeutic effect. Hospital infections caused by certain pathogens (Pseudomonas aeraginosa), may require combined treatment.

After normalization of body temperature, it is recommended to continue treatment at least 48-78 hours. Since levofloxacin excreted mainly through the kidneys, in patients with impaired renal function, control over the kidney function is required, as well as correction of the dosing regimen.

In patients with diabetes who receive oral hypoglycemic agents, (eg, glibenclamide) or insulin, the use of levofloxacin increases the risk of developing hypoglycemia. Thus, patients need monitoring concentration of glucose in the blood.In patients receiving fluoroquinolones, including levofloxacin, sensory and sensory-motor peripheral neuropathy, the beginning of which can be rapid. When the appearance of symptoms in the patient neuropathy, the use of levofloxacin should be discontinued (minimizes the possible risk of developing irreversible changes). Levofloxacin should be use with caution in patients with pseudoparalytic myasthenia gravis (myasthenia gravis).

Follow strictly the recommended duration administration, which should be at least 60 minutes (100 ml infusion solution). Experience of application levofloxacin shows that during an infusion, increased heart rate and transient drop in blood pressure can occur. In rare cases, the expressed fall in blood pressure pressure can cause vascular collapse. If during the infusion of levofloxacin (Lisofloxacin), a marked drop in blood pressure is observed, the infusion is immediately stopped.

During treatment with Eleflox, an episode of seizures may develop in patients with previous brain damage due, for example, to a stroke or severe trauma.Convulsive activity may also increase with simultaneous use of fenbufen, similar non-steroidal anti-inflammatory drugs or theophylline (see "Interactions").

Despite the fact that photosensitization is noted with the use of levofloxacin very rarely, in order to avoid it, patients are not recommended to undergo sunlight and artificial ultraviolet irradiation.

If you suspect a pseudomembranous colitis should be Immediately cancel the Eleflox and begin appropriate treatment. 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 corticosteroids increases the risk of rupture of tendons. If you suspect a tendonitis, you should immediately stop the treatment with Eleflox and begin appropriate treatment of the affected tendon, for example, by providing him with a resting state (see "Contraindications" and "Side effects").

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

When using fluoroquinolones, including levofloxacin, caution should be exercised in patients with known risk factors for lengthening the interval Q-T: elderly age; violation of electrolyte balance (hypokalemia, hypomagnesemia); congenital lengthening syndrome Q-T; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous reception of drugs that can lengthen the interval Q-T.

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

Such side effects when taking EleFlox, like dizziness or stupor, drowsiness and vision disorders (see "Side effect"), can worsen the ability to speed reactions and concentration, which represents a certain risk in situations, when these abilities are of particular importance. During the period of treatment, 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 500 mg / 100 ml.

Packaging:

For 100 ml of the solution for infusion in a sterile sealed polyethylene bottle (type FFS) with a lid; 1 bottle is packed in a plastic bag, and placed along with instructions for use in a cardboard pack.

Storage conditions:

At a temperature of no higher than 25 ° C in a dark place. Do not freeze. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006074/08

Date of registration:31.07.2008

The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India

Manufacturer: & nbsp

RANBAXY LABORATORIES, Ltd. India

Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED

Information update date: & nbsp26.10.2015

Illustrated instructions

Instructions

Eleflox (Eleflox)