Active substanceKanamycinKanamycin
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Dosage form: & nbsp

Powder for solution for injection

Composition:

Kanamycin disulfate in terms of kanamycin 0.5 g, 1.0 g.

Description:

The powder is white or almost white, hygroscopic.

Pharmacotherapeutic group:Antibiotic, aminoglycoside
ATX: & nbsp

A.07.A.A.08   Kanamycin

Pharmacodynamics:

A broad-spectrum antibiotic from the aminoglycoside group penetrates into the microbial cell, binds to specific receptor proteins at 30S subunit of ribosomes. Disrupts the formation of a complex of transport and matrix ribonucleic acid (RNA) (30S subunit of the ribosome) and blocks the synthesis of proteins, damages the membranes of the microbial cell.

Effective against most Gram-positive and Gram-negative microorganisms, as well as acid-fast bacteria: Mycobacterium tuberculosis (including resistant to streptomycin, paraaminosalicylic acid (PASK), isoniazid and other anti-tuberculosis drugs, except viomycin), Escherichia coli, Shigella spp., Salmonella spp., Proteus spp., Enterobacter spp., Klebsiella pneumoniae, Neisseria gonorrhoeae et meningitidis, Staphylococcus spp.

The strains of these microorganisms, resistant to tetracycline, erythromycin, chloramphenicol, benzylpenicillin, streptomycin and others, in most cases remain sensitive to kanamycin.

Does not apply to Pseudomonas aeruginosa, Streptococcus spp., Bacteroides spp. and other anaerobic bacteria, yeast fungi, viruses and protozoa.

Pharmacokinetics:

The time to reach the maximum concentration (TCmax) in the blood plasma with intramuscular (IM) administration is 0.5-1.5 hours, after 30 minutes intravenous (IV) infusion - 30 minutes, after 60 minutes IV infusion - 15 minutes. The maximum concentration (C max) in the blood plasma after IV or IM injection at a dose of 7.5 mg / kg is 22 μg / ml.

Penetrates into the pleural cavity, lymphatic, synovial and peritoneal fluid, serum, bronchial secretion and bile. TSam in bile - 6 hours. High concentrations are found in urine; low concentrations - in bile, breast milk, watery moisture, bronchial secretion, sputum and cerebrospinal fluid. It penetrates well into all tissues of the body, where it accumulates intracellularly; high concentrations are noted in organs with good blood supply: lungs, liver, myocardium, spleen and especially in the kidneys where it accumulates in the cortical layer, lower concentrations - in muscles, adipose tissue and bones.

Fine kanamycin does not penetrate the blood-brain barrier, however, in case of inflammation of the meninges, the concentration of the drug in the cerebrospinal fluid reaches 30-60% of that in the plasma. Newborns develop higher concentrations in the cerebrospinal fluid than in adults; passes through the placenta - is found in the fetal blood and amniotic fluid. The volume of distribution in adults is 0.26 l / kg, in children 0.2-0.4 l / kg, in newborns less than 1 week old and weighing less than 1.5 kg to 0.68 l / kg, at the age of less than 1 week and a body weight of more than 1.5 kg - up to 0.58 l / kg, in patients with cystic fibrosis - 0.3-0.39 l / kg.

It is not metabolized. Half-life (T1/2) in adults - 2-4 hours, in newborns - 5-8 hours, in older children - 2.5-4 hours. End T1/2 - more than 100 hours (release from the intracellular depot).

It is excreted by the kidneys by glomerular filtration, mainly unchanged (70-95% is detected in the urine after 24 hours).

T1/2 in adults with renal dysfunction varies depending on the degree of impaired function up to 100 h, in patients with cystic fibrosis - 1-2 h, in patients with burns and hyperthermia T1/2 can be shorter compared with the average due to increased clearance.

It is excreted during hemodialysis (50% for 4-6 hours), peritoneal dialysis is less effective (25% for 48-72 hours).

Indications:

Infectious and inflammatory diseases caused by microorganisms sensitive to kanamycin: biliary tract, bone and joint, central nervous system, the abdominal cavity (peritonitis), respiratory system (including tuberculosis in combined therapy, pneumonia, empyema, lung abscess) skin and soft tissues (including infected burns), the urinary tract (including pyelonephritis, pyelitis, cystitis, urethritis), sepsis, postoperative infection.

Contraindications:

Hypersensitivity to kanamycin (including other aminoglycosides in the anamnesis). Severe chronic renal failure with azotemia and uremia, neuritis of the VIII pair of cranial nerves, preterm infants, neonatal period (up to 1 month).

If you have any of these diseases, consult a doctor before taking the drug.

Carefully:

Myasthenia gravis, parkinsonism, botulism (aminoglycosides may cause disruption of neuromuscular transmission, resulting in further weakening of skeletal muscle), renal failure,elderly age.

If you have any of these diseases, consult a doctor before taking the drug.

Pregnancy and lactation:

When pregnancy is contraindicated. During breastfeeding, use with caution, when the potential benefit to the mother exceeds the potential risk for the child. Aminoglycosides penetrate into breast milk in small amounts, because they are poorly absorbed from the gastrointestinal tract, complications associated with them in infants have not been recorded.

Dosing and Administration:

Intravenously (intravenously), drip, intramuscularly (in / m), in the cavity. It is not recommended to inject intravenously the undiluted kanamycin solution, in connection with the possibility of developing a neuromuscular blockade.

With infections of non-tuberculous etiology: single dose for adults - 0.5 g, daily - 1-1.5 g (0.5 g every 8-12 h). The maximum daily dose is 2 g (1 g every 12 hours).

The course of treatment is 5-7 days, depending on the severity and features of the course of the process.

Children (only in / m). Children from 1 month to 1 year are administered in an average daily dose of 0.1 g, from 1 to 5 years - 0.3 g, over 5 years - 0.3-0.5 g.The maximum daily dose is 15 mg / kg. The daily dose is divided into 2-3 injections.

With tuberculosis the drug is used as part of complex therapy.

Enter intramuscularly: adults - 1 g once a day or 0.5 g 2 times a day, children older than 1 month - 15 mg / kg / day 6 days a week with a break for 7 days, but not more than 0, 5-0.75 g per day. The number of cycles and the total duration of treatment is determined by the stage and features of the course of the disease and is 1 month or more.

Intraperitoneal (intraperitoneal): Only adults with peritonitis and with abdominal contamination of the contents of the large intestine during surgery - 0.5 g of the drug are dissolved in 20 ml of water for injection.

In the cavity (abdominal, pleural, articular): Only adults with abscessing, postoperative infections are administered in the form of 0.25% solution (2.5 mg / ml).

The maximum daily dose is no more than 2 g, taking into account other ways of drug administration.

In renal failure, the administration regimen is adjusted by decreasing the dose taking into account the body weight or increasing the intervals between the administrations, according to the calculated formulas:

initial dose (mg) = body mass x 7;

subsequent doses (mg) = initial dose / creatinine content in blood plasma (mg /100 ml);

interval (h) = creatinine content in blood plasma (mg/100 ml) x 9.

Multiplicity of administration 2-3 times a day. In days of hemodialysis after its carrying out in addition introduce a single dose of the drug.

To avoid overdose of the drug, it is recommended to periodically monitor the concentration of antibiotic in the patient's blood.

Preparation of solutions

For intramuscular injection a single dose (0.5 g or 1 g) is dissolved in 2 ml or 4 ml of water for injection or 0.25-0.5% solution of procaine.

For intravenous drip prepared at initial dilution, a solution containing a single dose of the preparation (0.5 g) is dissolved in 200 ml of a 5% dextrose solution and injected at a rate of 60-80 cap / min.

Intraperitoneal - 0.5 g (as a 2.5% solution), for which a single dose of 0.5 g is dissolved in 20 ml of water for injection.

In the cavity (pleural, abdominal, articular) for washing, 10-50 ml of 0.25% aqueous solution is administered.

The solutions are used immediately after preparation.

Side effects:

From the digestive system: nausea, vomiting, diarrhea, impaired liver function (increased activity of "liver" transaminases, hyperbilirubinemia).

On the part of the organs of hematopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the nervous system: headache, drowsiness, weakness, neurotoxic effect (muscle twitching, sensation of numbness, tingling, paresthesia, epileptic seizures), violation of neuromuscular transmission (respiratory arrest).

From the sense organs: ototoxicity (ringing or feeling in the ears, hearing loss, up to irreversible deafness), toxic effect on the vestibular apparatus (discoordination of movements, dizziness).

From the urinary system: nephrotoxicity - a violation of kidney function (increase or decrease in frequency of urination, thirst, cylindruria, microhematuria, albuminuria).

Allergic reactions: skin rash, itching and hyperemia of the skin, fever, angioedema.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: toxic reactions (hearing loss, ataxia, dizziness, urination disorders, thirst, loss of appetite, nausea, vomiting, ringing or feeling in the ears, respiratory failure).

Treatment: for the removal of the blockade of the neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis, cholinesterase inhibitors, calcium salts, artificial ventilation (IVL), and other symptomatic and supportive therapy.

Interaction:

Reduces the effect of antimiasthenic drugs (LS).

Strengthens the muscle relaxant effect of nondepolarizing muscle relaxants, general anesthetics and polymyxins.

Pharmaceutically incompatible with streptomycin, gentamicin, penicillins, heparin, cephalosporins, capreomycin, amphotericin B, erythromycin, nitrofurantoin, biomycin.

Beta-lactam antibiotics (cephalosporins, penicillins) in patients with severe chronic renal failure reduce the effect of aminoglycosides.

Nalidixic acid, polymyxin, cisplatin and vancomycin increase the risk of oto and nephrotoxicity.

Diuretics (especially furosemide), cephalosporins, penicillins, sulfonamides and non-steroidal anti-inflammatory drugs, competing for active secretion in the nephron tubules, block the elimination of aminoglycosides, increase their serum concentration, enhancing nephro- and neurotoxicity.

Cyclopropane increases the risk of developing apnea with intraperitoneal administration of kanamycin.

Parenteral administration of indomethacin increases the risk of developing toxic effects of aminoglycosides (lengthening T1/2 and reduced clearance).

Methoxyflurane, polymyxins for parenteral administration, and other drugs that block neuromuscular transmission (halogenated hydrocarbons as drugs for inhalation anesthetic, narcotic analgesics, transfusion of large amounts of blood to citrate preservatives), increase the risk of nefroksicheskogo action and cessation of breathing (by enhancing neuromuscular muscular blockade).

If you are taking other medications, consult your doctor..

Special instructions:

During the treatment period, it is necessary to monitor the function of the kidneys, cochlear nerve and vestibular apparatus at least once a week, and the concentration of the drug in the blood plasma.

The probability of nephrotoxicity was higher in patients with impaired kidney function, and also at high doses or for a long time (in this category of patients may require daily monitoring of renal function).

When unsatisfactory audiometric tests, the dose of the drug is reduced or discontinued.

Patients with infectious-inflammatory diseases of the urinary tract are advised to take an increased amount of fluid with adequate diuresis.

In the absence of positive clinical dynamics should be remembered the possibility of developing resistant microorganisms. In such cases, it is necessary to cancel treatment and begin appropriate therapy.

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

Care should be taken when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Powder for solution for injection, 0.5 g and 1.0 g of active substance.

Packaging:

In bottles of glass with a capacity of 10 ml.

1 bottle with instructions for use in a pack of cardboard.

10 bottles with instructions for use in a cardboard box.

For hospitals:

- 50 bottles with an equal number of instructions for use in a cardboard box;

- 1 to 50 vials with an equal number of instructions for use in a cardboard box.

Complete with solvent

Water for injection 5 ml in a glass ampoule.

1 bottle and 1 ampoule in a contoured cell package (NLC) made of a polyvinylchloride (PVC) film with instructions for use in a pack of cardboard.

5 bottles and 5 ampoules in separate KNU from PVC film with instructions for use in a pack of cardboard.

In the pack put a knife to open the ampoules or a scarifier ampoule. When using ampoules with notches, rings or break points, the ampoule opener opener or ampoule scarifier is allowed not to be inserted.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription
Registration number:LS-000348
Date of registration:07.06.2010 / 06.04.2015
Expiration Date:Unlimited
The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia
Manufacturer: & nbsp
Information update date: & nbsp22.11.2017
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