Kanamycin (Tablets, Powder) Instructions for Use

ATC Code

J01GB04 (Kanamycin)

Active Substance

Kanamycin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibiotic of the aminoglycoside group

Pharmacotherapeutic Group

Antibiotic-aminoglycoside

Pharmacological Action

A broad-spectrum antibiotic of the aminoglycoside group, produced by Streptomyces kanamyceticus. It has a bactericidal effect.

It is active against Mycobacterium tuberculosis, gram-negative bacteria: Escherichia coli, Shigella spp., Salmonella spp., Proteus spp., Enterobacter spp., Klebsiella pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis; gram-positive cocci: Staphylococcus spp. (including strains producing penicillinase).

Pseudomonas spp. and Streptococcus spp. are poorly sensitive or resistant to kanamycin.

Anaerobic bacteria, yeasts, viruses, and most protozoa are resistant to kanamycin.

Pharmacokinetics

When taken orally, it is practically not absorbed (only about 1% is absorbed through the intact intestinal mucosa; larger amounts may be absorbed through damaged or ulcerated gastrointestinal mucosa), exerting a local effect. The time to reach C_max after intramuscular administration is 0.5-1.5 hours, after a 30-minute intravenous infusion – 30 minutes, after a 60-minute intravenous infusion – 15 minutes. C_max after intravenous or intramuscular administration of 7.5 mg/kg is 22 µg/ml. It penetrates into the pleural cavity, lymphatic, synovial, and peritoneal fluids, blood serum, bronchial secretion, and bile. C_max in bile is reached after 6 hours. High concentrations are found in urine; low concentrations are found in bile, breast milk, aqueous humor, bronchial secretion, sputum, and cerebrospinal fluid.

It penetrates well into all body tissues, 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 cortex; lower concentrations are found in muscles, adipose tissue, and bones. Normally, Kanamycin does not cross the blood-brain barrier; however, with inflammation of the meninges, the concentration of the drug in the cerebrospinal fluid reaches 30-60% of that in plasma. In newborns, higher concentrations are achieved in the cerebrospinal fluid than in adults. It crosses the placental barrier and is found in fetal blood and amniotic fluid. V_d in adults is 0.26 L/kg, in children – 0.2-0.4 L/kg, in newborns under 1 week of age and weighing less than 1.5 kg – up to 0.68 L/kg, in those under 1 week of age and weighing 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.

T_1/2 in adults is 2-4 hours, in newborns – 5-8 hours, in older children – 2.5-4 hours. The terminal T_1/2 is more than 100 hours (release from intracellular depots). After parenteral administration, it is excreted by the kidneys via glomerular filtration predominantly unchanged (70-95% is found in urine within 24 hours); when taken orally, it is excreted in feces. T_1/2 in adults with impaired renal function varies depending on the degree of impairment up to 100 hours; in patients with cystic fibrosis – 1-2 hours; in patients with burns and hyperthermia, T_1/2 may be shorter than average due to increased clearance. It is removed by hemodialysis (50% in 4-6 hours); peritoneal dialysis is less effective (25% in 48-72 hours).

Indications

For parenteral use: infectious and inflammatory diseases caused by microorganisms sensitive to kanamycin; tuberculosis (in case of resistance of mycobacteria to streptomycin and phthivazid).

For oral administration: intestinal infections caused by sensitive microflora (including dysentery, dysentery carrier state, bacterial colitis, enterocolitis); preparation for gastrointestinal surgery.

For local use in ophthalmology: conjunctivitis, blepharitis, keratitis, corneal ulcers.

ICD codes

Dosage Regimen

Tablets, Powder

For infections of non-tuberculous etiology, adults are administered 500 mg intramuscularly or intravenously (drip) every 8-12 hours; the daily dose is 1-1.5 g; the maximum single dose is 1 g with an interval between administrations of 12 hours, the maximum daily dose is 2 g. The duration of treatment is 5-7 days. Children are administered only intramuscularly; the maximum daily dose is 15 mg/kg, the frequency of administration is 2-3 times/day.

For tuberculosis, adults – 1 g once/day, children – 15 mg/kg. It is administered daily for 6 days, with a break on the 7th day. The number of courses and the total duration of treatment are determined individually.

Kanamycin is administered into cavities (pleural, joint cavity) as an aqueous solution, used as an aerosol and warm-moist inhalations.

When performing peritoneal dialysis, 1-2 g is dissolved in 500 ml of dialysate fluid.

In renal failure, the dose should be reduced or the intervals between administrations should be increased.

When taken orally, the single dose for adults is 0.5-1 g. For children, the dose is 50 mg/kg/day. The frequency of use depends on the indications.

Adverse Reactions

From the digestive system: nausea, vomiting, diarrhea, impaired liver function (increased activity of hepatic transaminases, hyperbilirubinemia); with long-term oral use – malabsorption syndrome (diarrhea, flatulence, light, foamy, oily stools).

From the hematopoietic system: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the central and peripheral nervous system: headache, drowsiness, weakness, neurotoxic effect (muscle twitching, numbness, tingling, paresthesia, epileptic seizures); with parenteral administration (mainly with intravenous and intracavitary), neuromuscular blockade is possible.

From the sensory organs: ototoxicity (ringing or feeling of fullness in the ears, hearing loss up to irreversible deafness), toxic effect on the vestibular apparatus (impaired coordination of movements, dizziness, nausea, vomiting), auditory neuritis; with local use – sensation of a foreign body in the eye (for 3-5 minutes), lacrimation, swelling and hyperemia of the eyelids.

From the urinary system: increase or decrease in the frequency of urination, thirst, impaired renal function (cylindruria, microhematuria, albuminuria).

Allergic reactions: skin rash, itching, skin hyperemia, fever, angioedema.

Contraindications

Impaired liver function, hearing loss (including due to damage to the auditory nerve), gastrointestinal obstruction, history of hypersensitivity to kanamycin and other aminoglycosides.

For parenteral administration: severe chronic renal failure with azotemia and uremia, neuritis of the VIII pair of cranial nerves, pregnancy.

Use in Pregnancy and Lactation

Kanamycin is contraindicated for use during pregnancy. If it is necessary to use kanamycin during lactation, the issue of discontinuing breastfeeding should be considered.

Use in Hepatic Impairment

Contraindicated in impaired liver function.

Use in Renal Impairment

A contraindication for parenteral administration is severe chronic renal failure with azotemia and uremia.

Use with caution and only for vital indications in renal failure.

Pediatric Use

Use with caution and only for vital indications in premature infants, in children under 1 month of age.

Geriatric Use

Use with caution and only for vital indications in elderly patients.

Special Precautions

Do not use simultaneously or sequentially with other antibiotics that have ototoxic and nephrotoxic properties (including streptomycin, monomycin, neomycin, gentamicin, florimycin), together with diuretics (including furosemide, mannitol) and muscle relaxants (increased and prolonged muscle relaxation).

Use with caution and only for vital indications in myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause impaired neuromuscular transmission, leading to further weakening of skeletal muscles), renal failure, and in elderly patients.

If symptoms of adverse reactions to Kanamycin appear, it should be discontinued.

During treatment, it is recommended to monitor renal function and perform audiometry – at least once a week when treating infections of non-tuberculous etiology and at least once a month when treating tuberculosis.

With intravenous or intrapleural administration, if signs of respiratory depression appear, the administration of kanamycin should be stopped and a solution of calcium chloride intravenously and a solution of proserin with atropine subcutaneously should be immediately administered. If necessary, the patient is transferred to controlled breathing.

Patients with infectious and inflammatory diseases of the urinary tract are recommended to take an increased amount of fluid. In the absence of positive clinical dynamics, the possibility of the development of resistant microorganisms should be considered. In such cases, it is necessary to discontinue treatment and initiate appropriate therapy. Due to the possibility of developing neuromuscular blockade, intravenous administration of undiluted kanamycin is not recommended. In hepatic coma, it is used for long-term suppression of intestinal flora bacteria to reduce ammonia intoxication.

Use with caution and only for vital indications in premature infants, in children under 1 month of age.

Drug Interactions

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

With simultaneous use, nalidixic acid, polymyxin, cisplatin, and vancomycin increase the risk of oto- and nephrotoxicity.

With simultaneous use, diuretics (especially furosemide), cephalosporins, penicillins, sulfonamides, and NSAIDs, competing for active secretion in the nephron tubules, block the elimination of aminoglycosides, increase their concentration in blood serum, enhancing nephro- and neurotoxicity.

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

Parenteral administration of indomethacin increases the risk of toxic effects of aminoglycosides (increased T_1/2 and decreased clearance).

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

With simultaneous use, methoxyflurane, polymyxins for parenteral administration, and other drugs that block neuromuscular transmission (halogenated hydrocarbons as drugs for inhalation anesthesia, opioid analgesics, transfusion of large amounts of blood with citrate preservatives) increase the risk of nephrotoxic effects and respiratory arrest (as a result of enhanced neuromuscular blockade).

Kanamycin is pharmaceutically incompatible with streptomycin, gentamicin, monomycin, penicillins, heparin, cephalosporins, capreomycin, amphotericin B, erythromycin, nitrofurantoin, viomycin.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.