Ivacin - 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, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and bacterial membranes.

Levofloxacin is active in in vivo and in vitro the following microorganisms:

Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (incl. Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (leukotoxin-containing and coagulase-negative methicillin-sensitive / moderately sensitive strains), including Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains); Streptococcus spp. groups C and G, 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 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-lactamase 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., Veilonella spp.

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

Moderately sensitive microorganisms (minimum inhibitory concentration more than 4 mg / l):

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, Campilobacter 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. (coagulase-negative methicillin-resistant strains).

Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

After intravenous infusion of 500 mg for 60 min, the maximum concentration (Cmah) is about 6 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, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated.

Kidney clearance is 70% of the total clearance. The half-life period (T1 / 2) is 6-8 hours. It is excreted mainly by the kidneys through glomerular filtration and tubular secretion. Less than 5% of levofloxacin is excreted as metabolites. In unchanged form, 70% are excreted by the kidneys within 24 hours and 87% in 48 hours.

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 lesions with previously treated quinolones, pregnancy, lactation, children and adolescence (up to 18 years).

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

Dosing and Administration:

Solution for infusion is administered intravenously drip. Duration of intravenous infusion

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

Doses are determined by the nature and severity of the infection, as well as sensitivity the prospective pathogen.

Patients with normal renal function (creatinine clearance> 50 ml / min) recommended the following dosage 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): 250 mg of levofloxacin once a day for 7-10 days;

- Infections of the skin and soft tissues: 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;

- Intraabdominal 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 each Levofloxacin 1-2 times a day until 3 months.

Patients with impaired renal function (creatinine clearance <50 mL / min) recommended the following dosage regimen:

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 for hemodialysis and permanent ambulatory 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 degree

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 (incl.with blood), digestive disorders, decreased appetite, abdominal pain, pseudomembranous colitis, increased activity of "liver" transaminases, hyperbilirubinemia, hepatitis, dysbiosis.

From the cardiovascular system: decrease in arterial pressure, vascular collapse, tachycardia, lengthening of the interval QT, atrial fibrillation.

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

From the nervous system: headache, dizziness, weakness, drowsiness, insomnia, anxiety, paresthesia, 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, 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, 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, anaphylactic shock, allergic pneumonitis, vasculitis.

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

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

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 use of levofloxacin hypo- and hyperglycemic conditions are possible, therefore it is recommended to control the concentration of glucose in the blood.

Levofloxacin increases the anticoagulant activity of warfarin.

Special instructions:

After normalization of body temperature, it is recommended to continue treatment for at least 48-72 hours.

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

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 damage (stroke, severe trauma), and the risk of hemolysis is a deficiency in glucose-6-phosphate dehydrogenase.

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 that require increased concentration and speed of psychomotor reactions.

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

Packaging:

For 100 ml of solution in a vial of polyethylene, closed with a lid. Each vial is wrapped with a polypropylene BOPP film. For 1 bottle in a cardboard pack together with instructions for use.

Storage conditions:

In dry, 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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000203

Date of registration:11.02.2011

The owner of the registration certificate:Clarice LifeSinceys LimitedClarice LifeSinceys Limited India

Manufacturer: & nbsp

CLARIS LIFESCIENCES, Ltd. India

Representation: & nbspClarice LifeSinceys LimitedClarice LifeSinceys Limited

Information update date: & nbsp07.10.2015

Illustrated instructions

Instructions

Ivacin (Ivacine)