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

Excipients: sodium chloride 900.00 mg, disodium edetate 100.00 mg, hydrochloric acid 0.126 ml, sodium hydroxide 2.80 mg, water for injection q.s. up to 100 ml.

Description:

A clear solution of a greenish-yellow color.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

Antimicrobial drug from the group of fluoroquinolones, the left-handed isomer of ofloxacin. Has a wide spectrum of antimicrobial action.

Levofloxacin blocks 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 active against most strains of microorganisms both in conditions in vitro, and in vivo.

In vitro sensitive (IPC ≤ 2 mg / ml) aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (incl. Enterococcus faecalis). Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive / methicillin-moderately sensitive strains), Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive / moderately sensitive; strains), Streptococcus spp. group C and G (incl. Streptococcus agalactiae. Streptococcus pneumoniae (penicillin-sensitive / moderately sensitive / resistant strains). Streptococcus pyogenes, Streptococcus spp. groups viridans (penicillin-sensitive / resistant strains);

aerobic gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp., Actinobacillus actinomycetemcomitans, Citrobacter freundii. Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (at t.h. 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 (strains, producing and non-reducing R-lactamase), Morganella morganii, Neisseria gonorrhoeae (strains, producing and non-reducing penicillinase), 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), Salmonella spp., Serratia spp. (Serratia marcescens);

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 pneumophila, Legionella spp., Mycobacterium spp. (at t.h. Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Levofloxacin moderately active (IPC ≥ 4 mg/l) at respect aerobic gram-positive microorganisms: Corynebacterium urealyticum, 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.

TO levofoloxacin are stable (IPC ≥ 8 mg/l) aerobic gram positive microorganisms: Corynebacterium jeikeium. Staphylococcus aureus (methicillin-resistant strains), Staphylococcus spp. (coagulase-negative methicillin-resistant strains);

aerobic gram-negative microorganisms: Alcaligenes xylosoxidans;

other microorganisms: Mycobacterium avium.

Pharmacokinetics:

Distribution

Binding to proteins - 30-40%. Cumulation at a dose of 500 mg once a day is insignificant. When administered at a dose of 500 mg twice daily, cumulation may be observed to a small extent. Equilibrium concentrations are achieved 3 days after the start of application.

It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, urinary system organs, genital organs, bone tissue, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

Levofloxacin poorly penetrates into the cerebrospinal fluid.

Average concentrations in the urine 8-12 hours after a single administration of 150, 300 or 500 mg of levofloxacin were, respectively, 44, 91 and 200 g / l.

Metabolism.

In the liver, a small portion of levofloxacin undergoes metabolism with the formation of desmethyllevofloxacin and levofloxacin-Noxide, which constitute <5% of the levofloxacin output by the kidneys.

Excretion

After the administration of a single dose of 500 mg, the half-life (T1 / 2) is 6-8 hours. It is excreted mainly by the kidneys by glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. Unchanged in the form of kidneys within 24 hours is deduced 70% and 48 hours - 87 %.

Indications:

Infectious-inflammatory diseases caused by susceptible to levofloxacin microorganisms:

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

- acute maxillary sinusitis;

- uncomplicated urinary tract infections;

- Complicated urinary tract infections (including acute pyelonephritis):

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

- septicemia / bacteremia;

- chronic bacterial prostatitis;

- intra-abdominal infection;

- complex therapy of drug-resistant forms of tuberculosis.

Contraindications:

Hypersensitivity to levofloxacin, any other component of the drug or other drugs from the group of fluoroquinolones, epilepsy, tendon damage previously conducted treatment with quinolones, pregnancy, lactation, children and adolescence (up to 18 years).

Carefully:

Elderly age (high probability of concomitant decrease in kidney function), deficiency of glucose-6-phosphate dehydrogenase. In patients with a history of brain injury (stroke or severe trauma), patients receiving concurrent medications lowering the threshold for convulsive readiness of the brain (possibly developing seizures). In patients with pseudo-paralytic myasthenia gravis (myasthenia gravis); with known risk factors for lengthening the interval QT.

Dosing and Administration:

The drug is administered intravenously drip. The duration of intravenous infusion of 500 mg levofloxacin (100 ml infusion solution) should not beless than 60 min.

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

Patients with normal renal function (creatinine clearance> 50 ml / min) are recommended the following dosing regimen:

- exacerbation of chronic bronchitis: 250-500 mg of levofloxacin once a day for 7-10 days;

- Community-acquired pneumonia: 500 mg of levofloxacin 1-2 times a day for 7-14 days;

- acute maxillary sinusitis: 500 mg of levofloxacin once a day for 10-14 days;

- uncomplicated urinary tract infections: 250 mg of levofloxacin once a day for 3 days;

- complicated urinary tract infections (including acute pyelonephritis): by 250 mg of levofloxacin once a day for 7-10 days;

- skin and soft tissue infections: 500 mg of levofloxacin 2 times a day for 7-14 days;

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

- chronic bacterial prostatitis: 500 mg of levofloxacin once a day for 28 days;

- intra-abdominal infection: 500 mg of levofloxacin 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 of levofloxacin 1-2 times a day for up to 3 months.

Patients with impaired renal function (creatinine clearance <50 ml / min) the following dosing regimen is recommended:

Creatinine clearance, 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 when hemodialysis and permanent 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 (CAPD), no additional doses are required.

If the liver function is not corrected, dose adjustment is not required, since levofloxacin metabolized in the liver to an insignificant extent.

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.

Side effects:

From the digestive system: nausea, vomiting, diarrhea (including with blood), digestive disorders, decreased appetite, abdominal pain, pseudomembranous colitis,increased activity of "liver" transaminases. hyperbilirubinemia. hepatitis, dysbiosis.

From the cardiovascular system: lowering blood pressure, cardiovascular collapse, tachycardia, increased interval QT on cardiogram, atrial fibrillation.

Co side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia.

Co the sides of the nervous system: headache, dizziness, weakness, drowsiness, insomnia, anxiety, paresthesia in the hands, fear, hallucinations, confusion, depression, movement disorders, seizures, peripheral sensory neuropathy, peripheral sensory-motor neuropathy, mental disorders with behavioral disorders self harm, including suicidal thought suicidal attempts.

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: hypercreatininemia, interstitial nephritis, acute renal failure.

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

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, anaphylactic shock, allergic pneumonitis, vasculitis.

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

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

Overdose:

Symptoms are manifested primarily from the central nervous system (confusion, dizziness, impaired consciousness and seizures as epileptic seizures).

In addition, gastrointestinal disorders (eg, nausea) and erosive lesions of the mucous membranes of the gastrointestinal tract, lengthening of the interval QT.
Treatment: symptomatic. Dialysis is ineffective.The specific antidote is not known.

Interaction:

Levofloxacin increases the half-life of cyclosporine.

Non-steroidal anti-inflammatory drugs, theophylline increase the risk of seizures.

Admission of glucocorticosteroids increases the risk of rupture of tendons (especially in the elderly).

Cimetidine and drugs that block tubular secretion, slow the withdrawal of levofloxacin.

The solution for infusion is compatible with 0.9% sodium chloride solution, 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 (for example, with sodium bicarbonate solution).

In patients with diabetes mellitus receiving oral hypoglycemic agents or insulin, against the background of the administration of levofloxacin hypo- and hyperglycemic conditions are possible, therefore it is recommended to control the concentration of glucose in the blood. Levofloxacin enhances the anticoagulant activity of warfarin. Alcohol can increase side effects from the central nervous system (dizziness, numbness, drowsiness).

Special instructions:

When the body temperature is normal, it is recommended to continue treatment at least 48-72 h. During treatment, sunlight and artificial ultraviolet irradiation should be avoided to avoid damage to the skin (photosensitization).

When there are signs of tendinitis, pseudomembranous colitis, allergic reactions levofloxacin immediately cancel.

It should be borne in mind that the development of seizures is possible in patients with a history of brain injury (stroke or severe trauma), with the risk of hemolysis of erythrocytes in the absence of glycojo-6-phosphate dehydrogenase.

During treatment, alcohol should be avoided.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving and potentially dangerous mechanisms due to possible dizziness, drowsiness, stiffness and visual disturbances, which can lead to a slowing of the speed of psychomotor reactions and a decrease in the ability to concentrate.

Form release / dosage:

Solution for infusions 5 mg / ml.

Packaging:

For 100 ml of the drug in a plastic bottle.The bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

In a dry, dark place at a temperature not above 25 ° С. Do not freeze.

Keep out of the reach of children.

Shelf life:2 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:PL-000396

Date of registration:28.02.2011 / 01.06.2016

Expiration Date:Unlimited

The owner of the registration certificate: Simpex Pharma Pvt Ltd. Simpex Pharma Pvt Ltd. India

Manufacturer: & nbsp

SIMPEX PHARMA, Pvt. Ltd. India

Information update date: & nbsp05.10.2015

Illustrated instructions

Instructions

Remedy (Remedia)