Kanamycin (When ATH J01GB04)

When ATH:
J01GB04

Characteristic.

Aminoglycosides I generation, TB drug II series. Producing radiant fungus Streptomyces kanamyceticus or other related microorganisms. It is a complex of three components, the main component of which is - kanamycin A (It is generally defined as kanamycin), and kanamycin B and C - the two minor components.

Available in two salts - kanamycin bisulfate (Tablets for oral administration) and kanamycin sulfate (powder / solution for parenteral application, Film eye).

Kanamycin monosulfate - white crystalline powder odorless and tasteless. Easily soluble in water, practically insoluble in alcohol. Stable in alkaline solutions.

Kanamycin sulfate - Powder or porous mass of white. Very easily soluble in water.

Pharmacological action.
Broad-spectrum antibacterial, bactericide, TB.

Application.

Infectious diseases, caused by susceptible pathogens. Parenteral administration: tuberculosis in combination with other anti-tuberculosis agents, biliary tract infections, bone and joints, Respiratory (incl. pneumonia, empyema, lung abscess), skin and soft tissue (incl. infected burns), urinary tract (incl. pyelonephritis, pyelitis, cystitis), severe pyo-septic diseases (sepsis, meningitis, peritonitis, bacterial endocarditis), postoperative infections.

Inside: intestinal decontamination before elective colorectal operations (in combination with erythromycin, metronidazolom); GI infections, caused by microorganisms sensitive to kanamycin (dysentery, dysenteric bacteriocarrier, bakterialynыy colitis, enterocolitis); pechenochnaya эntsefalopatiya and pechenochnaya coma (as an auxiliary drug).

Films eye: conjunctivitis, .Aloe, keratit, corneal ulcer.

Contraindications.

Hypersensitivity, incl. other aminoglycosides; neuritis of the VIII cranial nerves, severe chronic renal failure with azotemia and uremia. Kanamycin monosulьfat: bowel obstruction.

Restrictions apply.

Botulism, myasthenia gravis and Parkinson (aminoglycosides can cause a violation of neuromuscular transmission, which leads to a further weakening of the skeletal muscles), the liver and kidneys, children of the first months of life and premature. Kanamycin monosulьfat: ulcerative lesions of intestine.

Pregnancy and breast-feeding.

During pregnancy, used only for health (adequate and well-controlled studies in humans have not held). It passes through the placental barrier, It determined the serum concentrations of fetal, constituting 16-50% of the concentration in maternal serum, determined in amniotic fluid. In experiments on rats and rabbits revealed no teratogenic effect. In experiments on rats and guinea-pigs was shown, at doses that 200 mg / kg / day kanamycin resulted in hearing loss in fetuses. It has ototoxic effect on the fetus.

Category actions result in FDA - D. (There is evidence of the risk of adverse effects of drugs on the human fetus, obtained in research or practice, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk, if the drug is needed in life-threatening situations or severe disease, when safer agents should not be used or are ineffective.)

At the time of treatment should stop breastfeeding. Breast milk is the concentration 18 ug / ml. It may have an impact on the intestinal microflora of the child, However, due to the low absorption from the gastrointestinal tract of other complications in infants is not registered.

Side effects.

From the nervous system and sensory organs: paraesthesia, convulsions, vellication, seizures, headache, neyromыshechnaya blockade (muscular weakness, difficulty breathing), drowsiness, defeated VIII pair of cranial nerves (noise in ears, the feeling of "stuffiness" ear, hearing loss, up to complete deafness, unsteady gait, uncoordinated movements, dizziness).

Cardio-vascular system and blood (hematopoiesis, hemostasis): anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the digestive tract: nausea, vomiting, dysbiosis, diarrhea, malabsorption (with prolonged ingestion), abnormal liver function (increase in liver transaminases, giperʙiliruʙinemija).

With the genitourinary system: impairment of renal function (increase / decrease the frequency of urination, цilindrurija, mikrogematuriâ, albuminuria, proteinuria, oligurija).

Allergic reactions: drug fever, skin rash, anaphylactic reactions, asthmatic episodes.

When using eye films: foreign body sensation in the eye (3-5 min), lacrimation, swelling and redness century.

Cooperation.

It is unacceptable to mix kanamycin one syringe or a fluid system with beta-lactam antibiotics (penicillins, cephalosporins), and heparin due physicochemical incompatibility. Indomethacin, phenylbutazone and other NSAIDs, violate renal blood flow, may slow excretion from the body of kanamycin. With the simultaneous and / or sequential use of two or more aminoglycosides (neomycin, Streptomycin, gentamicin, monomicin, tobramycin, netilmycin, amikacin) their antibacterial activity is weakened (competition for a mechanism of "capture" of microbial cells), and toxic effects are amplified. Kanamycin can be applied not earlier than 10-12 days after the end of treatment with these antibiotics. It should not be used in conjunction with viomycin, полимиксином B, metoksifluranom, амфотерицином B, vancomycin, capreomycin and other GTR- and nephrotoxic agents, and furosemide, ethacrynic acid and other diuretics. In an application with means for inhalation anesthesia, incl. metoksifluranom, kurarepodobnymi drugs, opioid analgesics, Magnesium sulfate, polymyxins for parenteral administration, as well as large quantities of blood transfusions with citrate preservative enhanced neuromuscular blockade. Reduces the effectiveness of drugs antimiastenicheskih (during and after treatment with kanamycin requires adjustment of doses antimiastenicheskih funds).

Overdose.

Symptoms: neuromuscular blockade until the cessation of breathing, infants - CNS depression (slackness, stupor, coma, profound respiratory depression).

Treatment: calcium chloride / in, anticholinesterase agents (neostigmine n / a), atropyn, simptomaticheskaya therapy, if necessary - IVL. Hemodialysis, peritoneal dialysis when kidney function. Newborns spend exchange transfusion.

Dosing and Administration.

/ M, I / drop, in cavity, inhalation, locally.

Kanamycin sulfate. / M, / drip, in cavity, inhalation. In tuberculosis: / m, adults - 1 g 1 once daily, elderly patients or patients with renal failure - not more than 750 mg / day; the maximum daily dose 2 g; nontuberculous infections etiology single dose for adults - 0,5 g, daily - 1-1.5 g (by 0,5 g every 8-12 hours). B / drip, 15 mg / kg / day (30 m), the maximum daily dose 1 g. The duration of treatment for tuberculosis 1 months or more, nontuberculous infections etiology 5-7 days. The cavity washings administered in 10-50 mL 0,25% aqueous. In carrying out peritoneal dialysis dissolved 1-2 g 500 ml of dialysis fluid. Injection solution can be used for inhalations - for 250 mg 2-4 times a day. Vnutrybryushynno, by 500 mg (as 2,5% solution).

Kanamycin monosulьfat. Inside, decontamination of the intestine - on 0,5 g 4 times a day for 1-2 days before surgery; hepatic encephalopathy (adjuvant) - 2-3 g every 6 no.

Films eye. Applied 1-2 times per day. The film with a clean ophthalmic forceps removed from the vial, or foam, and, pulling the fingers of his free hand lower eyelid, lay it in the space formed between the eyelid and eyeball. Then the lid is released and hold the eye in a quiet (fixed) state for 30-60 seconds to wet the film and its transition into the elastic (soft) state.

Precautions.

Due to the high toxicity and the rapid development of resistance of microorganisms with the use of other infections (except tuberculosis) It should be strictly limited. Newborn and premature babies kanamycin appoint only for health, since renal function have not sufficiently developed, that may increase T_1/2 and the manifestation of the toxic effect. Treatment should be under close medical supervision. If you have risk factors for toxic effects should regularly identify peak (C_max) and residual (C_min) kanamycin concentration in serum (conduct pharmacokinetic monitoring). Before and during treatment should control the weekly function of the auditory nerve (audiometria) and kidney (incl. serum creatinine and blood urea). At the first sign of GR- or nephrotoxicity kanamycin overturned.

The activity is expressed in units of (ED); 1 ED activity 1 ug kanamycin A (grounds).

Given the poor distribution of aminoglycosides in adipose tissue, patients, body weight exceeds the ideal more than 25%, daily dose, calculated on actual body weight, must be reduced by 25%. In malnourished patients increase the dose 25%.

Cooperation