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Manufacturers: Synthesis
Active ingredients
- Kanamycin
Disease class
- Bacterial meningitis, not elsewhere classified
- Blepharitis
- Conjunctivitis, unspecified
- Corneal ulcer
- Keratitis, unspecified
- Acute and subacute endocarditis
- Pneumonia without specifying the pathogen
- Abscess of the lung and mediastinum
- Pyothorax
- Peritonitis
- Liver failure, not elsewhere classified
- Cholecystitis
- Cholangitis
- Respiratory tuberculosis, confirmed bacteriologically and histologically
- Diarrhea and gastroenteritis of suspected infectious origin
- Septicemia, unspecified
- Cystitis
- Diagnosis of gastrointestinal diseases
Clinical and pharmacological group
- Antibacterial agents
Pharmacological action
- Antituberculosis
- Antibacterial
- Bactericidal
Pharmacological group
- Aminoglycosides
Powder for the preparation of an injection solution for intramuscular administration Kanamycin (Kanamycin)
Instructions for medical use of the drug
Description of pharmacological action
Aminoglycoside antibiotic of the first generation, anti-tuberculosis drug of the second line. Produced by the radiant fungus Streptomyces kanamyceticus or other related microorganisms. It is a complex of three components, the main component of which is kanamycin A (usually defined as kanamycin), and kanamycins B and C are two minor components. Available in the form of two salts - kanamycin monosulfate (tablets for oral administration) and kanamycin sulfate (powder/solution for parenteral use, ophthalmic films). Kanamycin monosulfate is a white crystalline powder without taste or odor. Easily soluble in water, practically insoluble in alcohol. Stable in alkali solutions. Kanamycin sulfate is a white powder or porous mass. Very easily soluble in water.
Indications for use
Infectious diseases caused by susceptible pathogens. Parenteral administration: tuberculosis in combination with other anti-tuberculosis drugs, infections of the biliary tract, bones and joints, respiratory organs (including pneumonia, pleural empyema, lung abscess), skin and soft tissues (including infected burns), urinary tract (including pyelonephritis, pyelitis, cystitis), severe purulent-septic diseases (sepsis, meningitis, peritonitis, septic endocarditis), postoperative infections. Orally: intestinal decontamination before planned colorectal operations (in combination with erythromycin, metronidazole); gastrointestinal infections caused by microorganisms sensitive to kanamycin (dysentery, dysentery bacteria carriage, bacterial colitis, enterocolitis); hepatic encephalopathy and hepatic coma (as an auxiliary drug). Ophthalmic films: conjunctivitis, blepharitis, keratitis, corneal ulcers.
Pharmacodynamics
Actively penetrates the cell membrane and irreversibly binds to specific receptor proteins on the 30S ribosomal subunit. It disrupts the formation of a complex between messenger RNA and the 30S ribosomal subunit. As a result, erroneous reading of information from RNA occurs and defective proteins are formed, polyribosomes disintegrate and lose the ability to synthesize protein. It disrupts the structure and function of cytoplasmic membranes, causing the death of microbial cells. Active against Mycobacterium tuberculosis, incl. strains resistant to streptomycin, PAS, isoniazid and other anti-tuberculosis drugs, except viomycin and capreomycin. Effective on most gram-positive and gram-negative microorganisms (Escherichia coli, indole-positive and indole-negative strains of Proteus spp., Salmonella spp., Shigella spp., Haemophilus influenzae, Enterobacter spp., Yersinia spp., Klebsiella pneumoniae, Neisseria gonorhoeae, Neisseria meningitidis , Serratia marcescens, Staphylococcus spp., except methicillin-resistant strains), including microorganisms resistant to tetracycline, erythromycin, chloramphenicol and acid-fast bacteria. Less active against Pseudomonas spp. Does not affect Pseudomonas aeruginosa, Streptococcus spp., anaerobes, yeasts, viruses and protozoa. Bacteria quickly acquire resistance to kanamycin; for the treatment of tuberculosis, it is used when the pathogen is resistant to other first and second line anti-tuberculosis drugs (with the exception of viomycin).
Pharmacokinetics
When taken orally, kanamycin monosulfate is poorly absorbed from the gastrointestinal tract (about 1%) and, unchanged, is almost completely excreted in feces; the absorbed portion is quickly excreted by the kidneys. It is absorbed in large quantities through ulcerated or damaged intestinal mucosa and in the presence of inflammation. When used in the form of aerosol inhalation, kanamycin sulfate is poorly absorbed into the blood, resulting in high concentrations in the lungs and upper respiratory tract. With intramuscular administration, kanamycin sulfate is quickly and completely absorbed and is determined in therapeutic concentrations in the blood within 8 hours after administration. With intravenous drip administration of kanamycin sulfate, the therapeutic concentration in the blood is maintained for 12 hours. After intramuscular or intravenous administration at a dose of 7.5 mg/kg, Cmax is 22 mcg/ml. Plasma protein binding is low (less than 10%). The volume of distribution is 0.2–0.4 l/kg, in newborns up to 0.68 l/kg. Penetrates into abscess fluid, cavity contents, pericardial, pleural, peritoneal, synovial fluid. High concentrations are observed in the liver, lungs and kidneys (may accumulate in the cortex). Lower concentrations are observed in bile, aqueous humor, bronchial secretions and sputum, in muscle, bone and adipose tissue. At therapeutic concentrations in adults, kanamycin does not pass through the BBB; in children, its concentration in the cerebrospinal fluid is 10–20% of the level in the blood plasma. With inflammation of the meninges, the concentration in the cerebrospinal fluid is 30–60% in adults, and more than 50% of that in the blood plasma in children. May cause blockade of neuromuscular transmission (curare-like effect). It is not subject to metabolism. T1/2 in adults is 2-4 hours, in newborns - 5-8 hours. It is excreted by glomerular filtration and is not reabsorbed in the renal tubules. It is excreted by the kidneys within 24–48 hours; if their function is not impaired, it does not accumulate. In case of renal failure, depending on the degree of renal dysfunction, T1/2 can increase to 70–100 hours, in patients with cystic fibrosis it can be shortened to 1–2 hours. Concentration in urine can exceed the concentration in blood plasma by 10–20 times, and the activity of kanamycin with an alkaline urine reaction it is much higher than with an acidic one. It is excreted in small quantities in bile. It is excreted during hemodialysis (every 4–6 hours the concentration in the blood plasma decreases by 50%) and to a lesser extent during peritoneal dialysis (approximately 25% of the dose is excreted within 48–72 hours). There is evidence of the effectiveness of kanamycin in the treatment of cholangiohepatitis, necrotizing enterocolitis of newborns, acute prostatitis, and appendiceal abscess.
Use during pregnancy
During pregnancy, use only for health reasons (there are no adequate and strictly controlled studies in humans). Passes through the placental barrier, is determined in fetal blood serum in concentrations of 16–50% of concentrations in maternal blood serum, and is also determined in amniotic fluid. In experiments on rats and rabbits, no teratogenic effect was found. In experiments on rats and guinea pigs, it was shown that at doses of 200 mg/kg/day, kanamycin led to hearing impairment in fetuses. Has an ototoxic effect on the fetus. FDA category of effect on the fetus is D. Breastfeeding should be discontinued during treatment. In breast milk the concentration is 18 mcg/ml. It may have an effect on the intestinal microflora of the child, however, due to low absorption from the gastrointestinal tract, no other complications have been reported in infants.
Contraindications for use
Hypersensitivity, incl. to other aminoglycosides; neuritis of the VIII pair of cranial nerves, severe chronic renal failure with azotemia and uremia. Kanamycin monosulfate: intestinal obstruction.
Side effects
From the nervous system and sensory organs: paresthesia, convulsions, muscle twitching, epileptic seizures, headache, neuromuscular blockade (muscle weakness, difficulty breathing), drowsiness, damage to the VIII pair of cranial nerves (tinnitus, feeling of “stuffiness” in the ears , hearing loss, up to complete deafness, gait instability, uncoordinated movements, dizziness). From the cardiovascular system and blood (hematopoiesis, hemostasis): anemia, leukopenia, granulocytopenia, thrombocytopenia. From the gastrointestinal tract: nausea, vomiting, dysbacteriosis, diarrhea, malabsorption syndrome (with prolonged oral administration), liver dysfunction (increased activity of liver transaminases, hyperbilirubinemia). From the genitourinary system: impaired renal function (increased/decreased frequency of urination, cylindruria, microhematuria, albuminuria, proteinuria, oliguria). Allergic reactions: drug fever, skin rash, anaphylactic reactions, asthmatic episodes. When using eye films: sensation of a foreign body in the eye (within 3–5 minutes), lacrimation, swelling and hyperemia of the eyelids.
Directions for use and doses
IM, IV drip, intracavity, inhalation, local. Kanamycin sulfate. IM, IV drip, in the cavity, inhalation. For tuberculosis: intramuscularly, adults - 1 g once a day daily, elderly patients or patients with renal failure - no more than 750 mg/day; maximum daily dose 2 g; for infections of non-tuberculosis etiology, a single dose for adults is 0.5 g, a daily dose is 1–1.5 g (0.5 g every 8–12 hours). IV drip, 15 mg/kg/day (30 min), maximum daily dose 1 g. Duration of treatment for tuberculosis is 1 month or more, for infections of non-tuberculous etiology 5–7 days. 10–50 ml of a 0.25% aqueous solution is injected into the cavities for rinsing. When performing peritoneal dialysis, dissolve 1–2 g in 500 ml of dialysate fluid. The injection solution can be used for inhalation - 250 mg 2-4 times a day. Intraperitoneally, 500 mg (as a 2.5% solution).
Overdose
Symptoms: neuromuscular blockade up to respiratory arrest, in infants - central nervous system depression (lethargy, stupor, coma, deep respiratory depression). Treatment: intravenous calcium chloride, anticholinesterase drugs (neostigmine subcutaneously), atropine, symptomatic therapy, and, if necessary, mechanical ventilation. Hemodialysis, peritoneal dialysis for renal dysfunction. Newborns undergo exchange blood transfusion.
Interactions with other drugs
It is unacceptable to mix kanamycin in the same syringe or infusion system with beta-lactam antibiotics (penicillins, cephalosporins), as well as with heparin due to physicochemical incompatibility. Indomethacin, phenylbutazone and other NSAIDs that interfere with renal blood flow may slow down the elimination of kanamycin from the body. With the simultaneous and/or sequential use of two or more aminoglycosides (neomycin, streptomycin, gentamicin, monomycin, tobramycin, netilmicin, amikacin), their antibacterial effect is weakened (competition for one mechanism of “capture” by the microbial cell), and the toxic effects are enhanced. Kanamycin can be used no earlier than 10–12 days after the end of treatment with these antibiotics. Do not use simultaneously with viomycin, polymyxin B, methoxyflurane, amphotericin B, vancomycin, capreomycin and other oto- and nephrotoxic drugs, as well as furosemide, ethacrynic acid and other diuretics. When used simultaneously with drugs for inhalation anesthesia, incl. methoxyflurane, curare-like drugs, opioid analgesics, magnesium sulfate, polymyxins for parenteral administration, as well as transfusion of large amounts of blood with citrate preservatives, the neuromuscular blockade increases. Reduces the effectiveness of antimyasthenic drugs (during and after treatment with kanamycin, dose adjustment of antimyasthenic drugs is required).
Precautions for use
Due to the high toxicity and rapid development of resistance of microorganisms, use for other infections (except tuberculosis) should be strictly limited. Kanamycin is prescribed to newborns and premature babies only for health reasons, since their kidney functions are not sufficiently developed, which can lead to an increase in T1/2 and toxic effects. Treatment should be carried out under close medical supervision. If there are risk factors for the development of toxic effects, peak (Cmax) and residual (Cmin) concentrations of kanamycin in the blood serum should be regularly determined (pharmacokinetic monitoring). Before starting and during treatment, the functions of the auditory nerve (audiometry) and kidneys (including the level of creatinine and urea in the blood) should be monitored weekly. At the first signs of oto- or nephrotoxicity, kanamycin is discontinued. Activity is expressed in action units (AU); 1 IU corresponds to the activity of 1 μg of kanamycin A (base). Given the poor distribution of aminoglycosides in adipose tissue, in patients whose body weight exceeds the ideal body weight by more than 25%, the daily dose based on actual body weight should be reduced by 25%. In debilitated patients, the dose is increased by 25%.
Best before date
24 months
ATX classification:
J Antimicrobials for systemic use
J01 Antimicrobials for systemic use
J01G Aminoglycosides
J01GB Other aminoglycosides
J01GB04 Kanamycin
Pharmacological properties
Pharmacodynamics.
kanamycin is a broad-spectrum antibiotic. 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, Pask, and isoniazid. By binding to the 30s subunit of the ribosomal membrane, it disrupts 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.
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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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** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Kanamycin is provided for informational purposes only and is not intended for prescribing treatment without the participation of a doctor. Patients need to consult a specialist!
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Overdose
Symptoms of overdose are increased manifestations of adverse reactions. with parenteral administration, neuromuscular blockade may occur (curare-like effect).
Treatment: There is no specific antidote. If there are symptoms of an overdose, it is necessary to immediately stop taking the drug and prescribe symptomatic therapy. In case of blockade or respiratory depression, prozerin with atropine is administered; if necessary, mechanical ventilation is indicated. If toxic reactions occur, peritoneal dialysis or hemodialysis. Newborns undergo exchange blood transfusion.
Note!
Description of the drug Kanamycin sulfate. d/r-ra d/in. 1g fl. on this page is a simplified author's version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
