Kanamycin - description of the drug, instructions for use, reviews

Pharmacodynamics and pharmacokinetics

The principle of action is based on damage to the cell membrane of the microorganism, blocking the production of proteins, and disrupting the process of formation of the matrix and transfer RNA complex.

The main substance penetrates into the cell of the microorganism and binds to special receptor proteins. Kanamycin affects gram-negative flora, gram-positive bacteria, Proteus, staphylococci, Neisseria, Shigella, Escherichia coli, Klebsiella, Salmonella. Strains of these microorganisms do not respond to the action of erythromycin, tetracycline, chloramphenicol , streptomycin, benzylpenicillin.

The drug does not affect protozoa, yeast fungi, anaerobic flora, viruses, streptococci.

Pharmacological properties of the drug Kanamycin

Pharmacodynamics . Kanamycin is a broad-spectrum antibiotic. It has a bactericidal effect on most gram-positive and gram-negative microorganisms, as well as acid-fast bacteria. Acts on strains of Mycobacterium tuberculosis, including those resistant to streptomycin, PAS, and isoniazid. By binding to the 30S subunit of the ribosomal membrane, it inhibits protein synthesis in the microbial cell. Effective, as a rule, against microorganisms resistant to tetracycline, erythromycin, and chloramphenicol. Does not affect anaerobic microorganisms, yeast, viruses and most protozoa. Pharmacokinetics. When administered intramuscularly, it quickly enters the blood, the therapeutic concentration is maintained for 8–12 hours. Penetrates into the pleural cavity, synovial fluid, bronchial secretions, bile, and through the placental barrier. Normally, kanamycin does not penetrate the BBB, but with inflammation of the meninges, its concentration in the CSF reaches 30–60% of that in the blood plasma. Excreted by the kidneys within 24–48 hours.

Indications for use

Kanamycin is prescribed for various infectious diseases. For pleural empyema, pneumonia, tuberculosis , infected burns, infections of the biliary tract, nervous system, respiratory system, abdominal cavity, joints, bones, for cystitis, pyelitis, pyelonephritis and other infectious lesions of the urinary system, as well as for sepsis and after surgical interventions, medication administered parenterally.

Tablet forms of the drug are indicated for hepatic coma, enterocolitis , dysentery bacteria carriage, dysentery , intestinal infections, and before operations on the digestive tract.

Kanamycin eye films are used for ulcerative lesions of the cornea, blepharitis , bacterial conjunctivitis, and keratitis .

Special instructions for the use of Kanamycin

Before using the drug, it is necessary to determine the state of kidney function and the sensitivity of microflora to kanamycin. During treatment, audiometric monitoring and monitoring of renal function should be periodically performed. During pregnancy and breastfeeding, as well as in children of the first year of life, the use of the drug is allowed only for health reasons. In elderly patients, Kanamycin should be prescribed only if it is impossible to use less toxic antibiotics. When using the drug, do not exceed the recommended dose. During treatment, renal function must be carefully monitored.

Side effects

Digestive tract: flatulence, diarrhea, oily stool, foamy stool, diarrhea, malabsorption syndrome, increased levels of liver enzymes, vomiting, nausea.

Hematopoietic organs: thrombocytopenia , leukopenia, anemia, granulocytopenia.

Nervous system: the neurotoxic effect manifests itself in epileptic seizures, paresthesia, tingling, numbness, muscle twitching , weakness, drowsiness, headaches, respiratory arrest due to disruption of neuromuscular transmission.

Sense organs: Kanamycin has an ototoxic effect, which is manifested by decreased hearing to deafness, congestion in the ears, and ringing. The drug affects the vestibular apparatus, causing vomiting, nausea, dizziness, and incoordination of movements .

Urinary system: nephrotoxicity, albuminuria, microhematuria, cylinduria, thirst , increased frequency of urination.

Possible development of angioedema , fever, itching, skin rash.

The use of eye films causes a foreign body sensation in the eye for several minutes and can cause eyelid hyperemia, swelling and lacrimation.

Kanamycin, instructions for use (Method and dosage)

Administered by injection intramuscularly or intravenously.

According to the instructions for use of Kanamycin, a single dosage for intravenous drip infusion is 0.5 grams, diluted in 200 ml of 5% dextrose solution, the rate of administration is 60-80 drops per minute.

For infectious lesions of non-tuberculosis etiology, the antibiotic is administered in a single dose of 0.5 grams, no more than 2 grams per day. The duration of antimicrobial therapy is 5-7 days.

For tuberculosis, Kanamycin is administered intramuscularly once a day, one gram, or the dose is divided into 2 doses of 0.5 grams. In the preoperative period, for the purpose of intestinal sanitation, adults are prescribed an antibiotic of 0.75 grams every 5 hours, no more than 4 grams per day.

Hepatic encephalopathy: 2-3 grams orally every 6 hours.

A 0.25% solution in an amount of 10-50 ml is injected into the articular, pleural, and abdominal cavities for washing.

To carry out peritoneal dialysis, 1-2 grams of kanamycin are dissolved in 500 ml of dialysate fluid.

Aerosol inhalations can be carried out with an injection solution 2-4 times a day, 250 mg.

It is administered intraperitoneally as a 2.5% solution of 500 mg.

The eye film is removed from the bottle or pencil case using sterile ophthalmic tweezers, the lower eyelid is pulled back with your fingers and the film is placed in the space between the eyeball and the eyelid, after which the eyelid is lowered, holding the eye in a stationary, calm state for a minute to wet the eye film and subsequent transition it into a soft, elastic state.

Eye films are used up to two times daily.

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use Kanamycin, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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Overdose

It manifests itself as toxic reactions in the form of thirst, decreased appetite, ataxia , hearing loss, dizziness, decreased appetite, respiratory failure, congestion in the ears, ringing in the ears, nausea.

Hemodialysis is carried out to relieve the blockade of neuromuscular transmission and eliminate its consequences.

The administration of calcium salts, anticholinesterase drugs , and the use of peritoneal dialysis .

Interaction

Kanamycin enhances the muscle relaxant effect of polymyxin , general anesthetics , curare-like drugs, and reduces the effectiveness of antimyasthenic drugs .

with gentamicin , streptomycin, heparin, penicillin, viomycin, nitrofurantoin , erythromycin, amphotericin B, capreomycin, and cephalosporins.

Cephalosporins , penicillins and other beta-lactam antibiotics can reduce the effectiveness of the aminoglycoside in patients with severe chronic renal failure.

Vancomycin , cisplatin , polymyxin, nalidixic acid increase the likelihood of nephrotoxicity and ototoxicity .

NSAIDs, sulfonamides, penicillins, cephalosporins, diuretics, especially furosemide, increase neurotoxicity and nephrotoxicity by blocking the elimination of aminoglycosides when competing for active secretion in the nephron tubules, which ultimately leads to an increase in their concentration in the blood serum.

When an antibiotic is administered intraperitoneally, the risk of developing apnea increases significantly with simultaneous intake of cyclopropane .

Parenteral administration of indomethacin increases the likelihood of toxic effects of aminoglycosides by reducing clearance and prolonging the half-life.

Respiratory arrest and nephrotoxicity are observed with the administration of polymyxins, methoxyflurane, and narcotic analgesics .

Kanamycin

Stylab / Catalog / Antibacterial drugs / Kanamycin

STYLAB offers test systems for the analysis of kanamycin in animal meat, milk, honey and vaccines by ELISA, as well as pure kanamycin substance and its mixtures with other aminoglycosides to ensure traceability of analyzes in accordance with GOST 32798-2014 and MUK No. 759/5.3.

Kanamycin is a broad-spectrum bactericidal antibiotic belonging to the group of aminoglycosides. It is produced in the form of a complex of three substances - kanamycins A, B and C by the bacteria Streptomyces kanamyceticus. Kanamycin is active against mycobacteria, including the causative agents of tuberculosis. In addition, it destroys many gram-positive and gram-negative bacteria, including E. coli , salmonella , shigella, enterobacter, yersinia, klebsiella, gonococcus, meningococcus, staphylococcus and other bacteria. Kanamycin is effective against microorganisms resistant to tetracycline , chloramphenicol , erythromycin , streptomycin and many other antibiotics. In medicine, kanamycin is prescribed for tuberculosis, diarrhea, infectious gastroenteritis, eye and skin diseases, cystitis, osteomyelitis, as well as pneumonia, peritonitis and endocarditis. In veterinary medicine, it is used for the prevention and treatment of postpartum endometritis in cows and pigs, as well as for other bacterial diseases. As of 2019, 3 kanamycin preparations intended for veterinary use were registered in the Russian Federation.

Like other aminoglycosides, kanamycin irreversibly binds to the 30S ribosomal subunit, which leads to cell death due to impaired protein synthesis. Kanamycin has no effect on streptococci, Pseudomonas aeruginosa , anaerobic bacteria, as well as yeast, protozoa and viruses. Bacteria quickly develop resistance to kanamycin. This resistance may be cross-resistance.

Kanamycin is poorly absorbed from the gastrointestinal tract and is excreted mainly unchanged in feces. This allows it to be used to treat intestinal diseases. However, ulcers and other gastrointestinal injuries or inflammation improve the absorption of this antibiotic. In this case, it is excreted by the kidneys. When used as an aerosol, kanamycin is also poorly absorbed and creates high concentrations in the lungs and respiratory tract. When administered intramuscularly, kanamycin is well and quickly absorbed and distributed throughout the organs and tissues of the body. Particularly high concentrations of kanamycin are created in body fluids, as well as in the liver, lungs and kidneys, and this antibiotic can accumulate in their cortex. Smaller concentrations of kanamycin are present in muscles, fat, bones, sputum, and bile. In healthy adults, kanamycin does not cross the blood-brain barrier. However, with inflammation of the meninges and in children, kanamycin creates noticeable (10–60% of the content in the blood plasma) concentrations in the cerebrospinal fluid. Kanamycin is not metabolized in the body and is excreted unchanged. Its half-life is 2-4 hours in adults and 5-6 hours in newborns. In small quantities, kanamycin can be excreted in both breast milk and animal milk.

The acute toxicity of kanamycin to humans and other mammals is low. The LD50 of kanamycin for mice when administered orally was 20500 mg/kg body weight, when administered intravenously – 115 mg/kg body weight. LD50 for rats when administered intravenously is 437 mg/kg.

Side effects and consequences of an overdose of kanamycin in humans have been well studied. These include nausea, vomiting, diarrhea, malabsorption of nutrients and minerals, headache, liver and kidney problems, changes in blood composition and allergic skin reactions. Kanamycin has a curare-like effect - it can disrupt signal transmission from nerves to muscles. This leads to sensory disturbances, convulsions and difficulty breathing until it stops. The ability of kanamycin to act on the auditory nerves determines its ototoxicity. It can manifest as tinnitus, hearing loss, or complete deafness. In addition, kanamycin can cause impaired coordination of movements and dizziness. Due to ototoxicity, kanamycin is not prescribed for inflammation of the auditory nerve, and due to hepatotoxicity and nephrotoxicity, it is not prescribed for liver and kidney diseases.

Kanamycin is able to overcome the placental barrier and penetrate both the amniotic fluid and the fetus. In animal studies, this antibiotic caused damage to the auditory nerves in fetal guinea pigs and rats. Therefore, kanamycin is not prescribed during pregnancy. This antibiotic did not show carcinogenic or mutagenic properties in animal studies. It also did not cause skin irritation in either rabbits or human volunteers.

When kanamycin and other aminoglycosides are simultaneously introduced into the body, their medicinal effect is reduced because these substances compete for capture by bacterial cells. The side effects of aminoglycosides are enhanced. Therefore, kanamycin can be used for treatment only 10-12 days after stopping taking other aminoglycosides. Due to its toxic properties and because kanamycin can lead to the emergence of antibiotic-resistant microorganisms, its content in food products must be controlled.

In the Russian Federation and the EAEU, the maximum permissible levels of kanamycin are specified in TR CU 034/2013 “On the safety of meat and meat products.” According to it, meat and raw fat of all types of animals can contain no more than 0.1 mg/kg of kanamycin, in the liver - no more than 0.6 mg/kg, in kidneys - no more than 2.5 mg/kg. Decision No. 28 of the Board of the Eurasian Economic Commission dated February 13, 2021 supplements these MRL restrictions for milk - 0.15 mg/kg. The same restriction for milk applies in European Union countries. In Korea, the maximum permissible content of kanamycin in milk is 0.1 mg/kg.

STYLAB offers Kanamycin ELISA Kit test systems for the analysis of kanamycin in meat and other animal tissues, milk, honey and vaccines. They allow you to quickly screen large numbers of samples and do not require expensive equipment. STYLAB also offers certified standard solutions to ensure traceability of measurements: pure kanamycin substance and its mixtures with other aminoglycosides to ensure traceability of analyzes in accordance with GOST 32798-2014 “Food products, food raw materials. Method for determining the residual content of aminoglycosides using high-performance liquid chromatography with a mass spectrometric detector" and MUK No. 759/5.3.

Literature

1. Kanamycin. Register of medicines in Russia.
2. Kanamicin. Pubchem
3. Na-Reum Ha, In-Pil Jung, Im-Joung La, Ho-Sup Jung, and Moon-Young Yoona. Ultra-sensitive detection of kanamycin for food safety using a reduced graphene oxide-based fluorescent aptasensor. Sci Rep. 2017; 7:40305.
4. Yong Jin, Jin-Wook Jang, Chang-Hoon Han, Mun-Han Lee. Development of immunoassays for the detection of kanamycin in veterinary fields. J Vet Sci. 2006 Jun; 7(2): 111–117.
5. The European Agency for the Evaluation of Medical Products Veterinary Medicines and Inspections. Committee For Veterinary Medicinal Products Kanamycin Summary Report (1). EMEA/MRL/514/98-FINAL January 1999
6. The European Agency for the Evaluation of Medical Products Veterinary Medicines and Inspections. Committee For Veterinary Medicinal Products Kanamycin Summary Report (2). EMEA/MRL/886/03-FINAL October 2003

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special instructions

The risk of developing nephrotoxicity increases significantly in patients with severe pathology of the renal system.

During the period of antimicrobial therapy, monitoring the condition of the vestibular apparatus, auditory nerve , and the functioning of the renal system is mandatory. If unsatisfactory results of audiometric tests are registered, the drug is discontinued or its dosage is reduced.

Aminoglycosides are capable of passing into breast milk in small quantities, but complications in infants have not been reported due to poor absorption of the drug from the digestive tract.

Patients with inflammatory and infectious lesions of the urinary tract need to drink more fluids during the treatment period.

The development of bacterial resistance may be indicated by the lack of positive dynamics, which requires a change in the antibacterial agent.

Infusions of undiluted kanamycin are not recommended due to the risk of developing neuromuscular blockade .

In hepatic coma, Kanamycin is used for a long time to suppress the bacterial intestinal flora to reduce ammonia intoxication.