Kanamycinum

General characteristics. Structure:

Active ingredient: 1 g of Kanamycinum of sulfate (in terms of Kanamycinum).

Antibiotic of a broad spectrum of activity from group of aminoglycosides.

Pharmacological properties:

Pharmacodynamics. Antibiotic of group of aminoglycosides. In low concentration has bacteriostatic action (due to disturbance of synthesis of protein in microbic cells), in high - bactericidal (damages cytoplasmic membranes of a microbic cell). Gets into a microbic cell, contacts specific proteins receptors on 30S subunit of ribosomes. Breaks formation of a complex transport and template-RNA (30S in ribosome subunit) and stops synthesis of proteins.

It is effective concerning the majority of gram-positive and gram-negative microorganisms, and also acid resisting bacteria: Mycobacterium tuberculosis (including steady against streptomycin, PASK, an isoniazid, etc. to antitubercular drugs, except Viomycinum), Escherichia coli, Shigella spp., Salmonella spp., Proteus spp., Enterobacter spp., Klebsiella pneumoniae, Neisseria gonorrhoeae et meningitidis, Staphylococcus spp. The strains of these microorganisms steady against tetracycline, erythromycin, chloramphenicol, benzylpenicillin, streptomycin, chloramphenicol, etc. in most cases keep sensitivity to Kanamycinum. Does not affect Pseudomonas aeruginosa, Streptococcus spp., Bacteroides, etc. anaerobic bacteria, barmy mushrooms, viruses and protozoa. Are poorly active against Streptococcus spp

Pharmacokinetics. The maximum concentration of Kanamycinum of sulfate in a blood plasma at intramuscular introduction is reached in 0,5-1,5 h and makes 7.5 mg/kg - 22 mkg/ml. Gets into a pleural cavity, lymphatic, synovial and peritoneal liquids, blood serum, a bronchial secret and bile.

The maximum concentration in bile of-6 h. High concentration are found in urine; low concentration - in bile, breast milk, watery moisture, a bronchial secret, a phlegm and cerebrospinal fluid. Well gets into all body tissues where collects intracellularly; high concentration are noted in bodies with good blood supply: lungs, a liver, a myocardium, a spleen, and especially in kidneys where collects in cortical substance, lower concentration - in muscles, fatty tissue and bones.

Normal sulfate does not pass Kanamycinum through a blood-brain barrier, however at an inflammation of a meninx concentration of drug in cerebrospinal fluid reaches 30-60% of that in plasma. At newborns higher concentration in cerebrospinal fluid, than at adults are created; passes through a placenta (it is found in blood of a fruit and amniotic liquid). It is not metabolized.

The elimination half-life at adults makes 2-4 h, at newborns - 5-8ch, children of more advanced age have 2,5-4 h. A final elimination half-life - more than 100 h (release from intracellular depots). It is removed by kidneys by glomerular filtering preferential in not changed, a look (70-95% are found in urine in 24 h), the elimination half-life at adults at a renal failure varies depending on extent of dysfunction to 100 h, patients with a mucoviscidosis have 1-2 h, at patients with burns and a hyperthermia the elimination half-life can be shorter in comparison with average values owing to the increased clearance. It is removed at a hemodialysis (50% for 4-6 h), peritoneal dialysis - is less effective (25% for 48-72 h)

Indications to use:

The infectious diseases caused by sensitive activators. Parenteral administration - infections of biliary tract, bones and joints, the central nervous system, an abdominal cavity, a respiratory organs (including tuberculosis, pneumonia, a pleura empyema, abscess of lungs), skin and soft tissues (including the infected burns), urinary tract (including pyelonephritis, a pyelitis, cystitis), sepsis, postoperative infections.

Route of administration and doses:

Intramusculary, in a cavity and orally (for local action). At infections of not tubercular etiology a single dose for adults – 0,5 g, daily - 1-1,5 g (on 0,5 g each 8-12 h). The highest daily dose - 2 g. A course of treatment - 5-7 days. To children - on 50 mg/kg/days; premature and to children of the first month of life - only according to "vital" indications.

At tuberculosis - the adult - on 1 g of 1 times a day or on 0,5 g 2 times a day, to children - on 15-20 mg/kg/days, but no more than 0,5-0,75 g. Each 7 day - a break.

Inside, at intestinal infections equal doses, 4-6 times a day (irrespective of a form and disease severity). A single dose for adults – 0,5-0,75 g, daily - 3 g the Highest daily dose - 4 g.

At hepatic encephalopathy (as the auxiliary medicine (M)) - inside, on 2-3 g each 6 h.

(Pleural, belly, joint) for washings enter into cavities on 10-50 ml 0,25% of aqueous solution. When carrying out peritoneal dialysis dissolve 1-2 g in 500 ml of the dialyzing liquid.

It is possible to use solution for injections also in the form of aerosol inhalations on 250 mg 2-4 times a day.
Intraperitoneally - on 500 mg (in the form of 2,5% of solution).

Features of use:

Use at pregnancy and during breastfeeding. Kanamycinum is contraindicated to use at pregnancy. In need of use of Kanamycinum in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

During treatment it is necessary at least 1 time a week to control function of kidneys, an acoustical nerve and vestibular mechanism.

The probability of development of nephrotoxicity is higher at patients with a renal failure, and also at appointment in high doses or for a long time (at this category of patients daily control of function of kidneys can be required).

At unsatisfactory audiometric tests the dose of drug is reduced or stop treatment.

Aminoglycosides get into breast milk in small amounts (as they are badly soaked up from a digestive tract, the related complications at babies it was not registered).

Patients with infectious and inflammatory diseases of urinary tract are recommended to accept the increased amount of liquid.

In the absence of positive clinical dynamics it is necessary to remember a possibility of development of resistant microorganisms. In similar cases it is necessary to cancel treatment and to begin performing the corresponding therapy.

Due to a possibility of development of neuromuscular blockade intravenous administration of undiluted Kanamycinum is not recommended.

At a hepatic coma apply for the purpose of long oppression of bacteria of an indestinal flora to reduction of intoxication ammonia.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, abnormal liver function (increase in activity of "hepatic" transaminases, hyperbilirubinemia); at chronic ingestion - a sprue (diarrhea, a meteorism, light, foamy, oil kcal).

From bodies of a hemopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From a nervous system: headache, drowsiness, weakness, neurotoxic action (twitching of muscles, feeling of numbness, pricking, paresthesia, epileptic seizures), neuromuscular transmission disturbance (apnoea). From sense bodys: ototoxicity (a ring or feeling of a mortgaging in ears, decrease in hearing, up to irreversible deafness), toxic action on a vestibular mechanism (a diskoordination of movements, dizziness, nausea, vomiting).

From an urinary system: nephrotoxicity - a renal failure (increase or reduction of frequency of an urination, thirst, a cylindruria, a microhematuria, an albuminuria).

Allergic reactions: skin rash, itch and dermahemia, fever, Quincke's disease.

If any of the side effects specified in the instruction are aggravated, or any other side effects which are not specified in the instruction are noted, it is necessary to report about it to the doctor immediately.

Interaction with other medicines:

Reduces effect of anti-myasthenic HP. Strengthens myorelaxation action of kurarepodobny HP, the general anesthetics and polymyxins.

Pharmaceutical it is incompatible with streptomycin, gentamycin, Monomycinum, penicillin, heparin, cephalosporins, kapreomitsiny, Amphotericinum In, erythromycin, nitrofurantoin, Viomycinum.

Beta лактамные antibiotics (cephalosporins, penicillin) at patients with a heavy chronic renal failure reduce effect of aminoglycosides.

Acidum nalidixicum, polymyxin, Cisplatinum and Vancomycinum increase risk of development from - and nephrotoxicity.

Diuretics (especially furosemide), cephalosporins, penicillin, streptocides and non-steroidal anti-inflammatory drugs, competing for active secretion in nephron tubules, block elimination of aminoglycosides, increase their concentration in blood serum, strengthening nefro-and a neurotoxicity.

Cyclopropane increases risk of development of an apnoea at intraperitoneal introduction of Kanamycinum.

Parenteral administration of indometacin increases risk of development of toxic effects of aminoglycosides (lengthening of T½ and decrease in clearance).

Metoksifluran, polymyxins for parenteral administration, etc. The hp blocking neuromuscular transmission (halogenated hydrocarbons as HP for inhalation anesthesia, narcotic analgetics, transfusion of large amounts of blood with citrate preservatives), increase risk of emergence of nephrotoxic action and an apnoea (as a result of strengthening of neuromuscular blockade).

Contraindications:

Hypersensitivity (including to other aminoglycosides in the anamnesis).

Parenteral administration - a heavy chronic renal failure with an azotemia and uraemia, neuritis of the VIII couple of cranial nerves, pregnancy.

With care. A myasthenia, parkinsonism, botulism (aminoglycosides can cause neuromuscular transmission disturbance that leads to further weakening of skeletal muscles), a renal failure, advanced age, premature children, the neonatality period (up to 1 month), the lactation period.

Overdose:

Symptoms: toxic reactions (a hearing loss, an ataxy, dizziness, frustration of an urination, thirst, a loss of appetite, nausea, vomiting, a ring or feeling of a mortgaging in ears, breath disturbance).

Treatment: for lifting the siege of neuromuscular transmission and its effects - a hemodialysis or peritoneal dialysis, inhibitors of cholinesterase, calcium salt, artificial ventilation of the lungs, other symptomatic and maintenance therapy.

Storage conditions:

Period of validity 4 years. Not to use after expiry date. List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intramuscular introduction of 1,0 g to bottles. On 50 bottles together with application instructions place a box from a cardboard (for hospitals).