Kanamycinum

General characteristics. Structure:

Active ingredient: 1 bottle contains Kanamycinum of sulfate of acid 1 g, sterile in terms of Kanamycinum.

Pharmacological properties:

Pharmacodynamics. Kanamycinum – an antibiotic of a broad spectrum of activity. Has bactericidal effect on the majority of gram-positive and gram-negative microorganisms, and also on acid resisting bacteria. Affects strains of mycobacteria of tuberculosis, including on steady against streptomycin, PASK, an isoniazid. Communicating with 30S in subunit of a ribosomalny membrane, breaks synthesis of protein in a microbic cell.

It is effective, as a rule, concerning microorganisms, resistant to tetracycline, erythromycin, levomycetinum.

Does not affect anaerobic microorganisms, yeast, viruses and the majority of protozoa.

Pharmacokinetics. At intramuscular introduction quickly comes to blood, therapeutic concentration remains for 8-12 h. Gets into a pleural cavity, synovial fluid, a bronchial secret, bile, through a placental barrier. Normal Kanamycinum does not pass through a blood-brain barrier, however at an inflammation of a meninx concentration it in cerebrospinal fluid reaches 30-60% of that in a blood plasma.

It is removed by kidneys for 24-48 h.

Pharmaceutical characteristics.

Main physical and chemical properties: powder of white or almost white color. Hygroscopic. Sticking of drug is allowed to bottle walls.

Incompatibility. Not to apply with other solvents, except specified (water to injections or 0,25-0,5% novocaine solution for intramuscular introduction, isotonic solution of sodium of chloride or 5% glucose solution to intravenous administration). Kanamycinum pharmaceutical is incompatible with streptomycin, gentamycin, Monomycinum, penicillin, heparin, cephalosporins, kapreomitsiny, Amphotericinum In, erythromycin, nitrofurantoin, Viomycinum. Their mixing in one volume is not allowed.

Indications to use:

Heavy it is purulent - septic diseases (sepsis, meningitis, peritonitis, a septic endocarditis);
infectious and inflammatory diseases of a respiratory organs (pneumonia, pleura empyema, abscess of lungs);
infections of kidneys and urinary tract;
purulent complications in the postoperative period;
the infected burns;
pulmonary tuberculosis and the tubercular damages to other bodies caused by microorganisms, resistant to противотуберкулезнымсредствамІ that ІІ a row and sensitive to Kanamycinum.

Route of administration and doses:

Kanamycinum is applied intramusculary.

Before purpose of drug in the absence of contraindications it is necessary to take skin samples on portability.

Solution for intramuscular introduction is prepared by ex tempore, adding to bottle contents    (1 g) of 4 ml of sterile water for injections or 0,25-0,5% of a rastvoranovokain, enter deeply into a verkhniynaruzhny quadrant of a buttock not more often than 2-3 times a day. For children as solvent use only water for injections.

For a vzroslykhrazovy dose at treatment of infections of not tubercular etiology makes 0,5 g each 8-12 h, the daily dose makes 1-1,5 g; the maximum single dose – 1 g with an interval between introductions of 12 h, the maximum daily dose – 2 g. Treatment duration – 5-7 days. Depending on disease severity, an effektivnostilecheniye and the course of a disease duration of treatment can be changed.

1 years at infections of not tubercular etiology (in exceptional cases) drug appoint by Detyamdo in an average daily dose 0,1 g; from 1 to 5 years – 0,1-0,3 g;  5 years – 0,3-0,5 g are more senior; the maximum daily dose – 15 mg/kg, frequency rate of introduction – 2-3 times a day. Duration of a course of treatment – 5-7 days.

At treatment туберкулезаканамицин enter the adult of 1 times a day in a dose 1 g, to children – on 15 mg/kg of 6 days a week with a break for the 7th day. The quantity of cycles and the general duration of treatment are defined by a stage and features of a course of a disease.

At renal the nedostatochnostiskhema of introduction of Kanamycinum korrigirutsya by reduction of doses or uvelicheniyainterval between introductions.

Dlyarascheta of intervals between injections taking into account degree of a renal failure can be recommended such formula: an interval between introductions (in hours) = the content of creatinine in a blood plasma (in mg / 100 ml) × 9.

For example: if concentration of creatinine in a blood plasma of 2 mg, the recommended dose has to be accepted by the patient each 18 h.

The initial dose of drug is calculated taking into account body weight by a formula:  a dose (in mg) = body weight (in kg) × 7.

The subsequent doses (in mg) = 

content of creatinine in

to blood serum (in mg / 100 ml) at frequency rate of introduction

2-3 times a day

In days of a hemodialysis after its carrying out in addition enter a single dose of drug.

Features of use:

The basis to use of Kanamycinum is inefficiency of other antibiotics. At nonsensitivity of the activator to drugs of group of Neomycinum (gentamycin, Neomycinum) cross resistance and to Kanamycinum obychnonablyudatsya.

Risk factors of a razvitiyaototoksichnost and/or nephrotoxicity of drug is: genetically determined exposure to ototoksichesky action (it is necessary to find out existence of cases of manifestation of ototoxicity of aminoglycosides from relatives); advanced age; an initial hearing disorder (otitis, meningitis, a birth trauma, a hypoxia in labor); high doses, long course of treatment; simultaneous use of other ototoksichesky and nephrotoxic medicines (see the section "Interaction with Other Medicines and Other Types of Interaction"); the diseases of kidneys and cardiovascular system leading to drug cumulation; dehydration; diabetes mellitus;   HIV infection; renal failure.

In this regard prior to treatment, and also during treatment by drug it is necessary to carry out:

- careful control of function of kidneys (urine retests, definition of creatinine of blood serum and calculation of glomerular filtering each 3 days, in case of decrease in this indicator by 50% it is necessary to cancel drug);

- research of acoustical function (carrying out audiometriya at least 2 weekly);

- monitoring of concentration of Kanamycinum in blood. At the first signs of ototoksichesky action (even an insignificant sonitus) or nephrotoxic action Kanamycinum is cancelled.

At balance disturbances the interval between injections needs to be increased.

It is necessary to consider possibility of neuromuscular blockade (to carry out an injection in the presence of all necessary conditions for implementation of iskusstvennoyventilyatsiilegky). The risk of development of heavy neuromuscular blockade of a priprimeneniya of drug increases at patients with: parkinsonism, a myasthenia, botulism, at simultaneous use of Kanamycinum with muscle relaxants. Apply Calcii chloridum to stopping of manifestations of neuromuscular blockade intravenously or antikholinesterazny drugs.

At emergence of signs of respiratory depression it is necessary to stop introduction of Kanamycinum and to urgently enter intravenously solution of Calcii chloridum and subcutaneously solution of a prozerin with atropine. In need of the patient transfer to the managed breath.

At decrease in level of potassium it is necessary to control the content of magnesium and calcium in blood serum.

People of advanced age should appoint Kanamycinum only at impossibility of use of less toxic antibiotics.

Slowed more down metabolism of drug at elderly patients leads to its longer circulation in blood even at normal function of kidneys that leads to increase in risk of ototoksichesky manifestations at this category of patients.

In case of use of drug it is not necessary to exceed the recommended doses.

Patients with disturbance of a funktsiypechena. At patients with liver pathology drug level in blood does not change (except the heavy alcoholic cirrhosis with ascites leading to the bigger volume of distribution of drug).

Purpose of Kanamycinum is considered the patient with serious pathology of a liver safe, but at the same time it is recommended to observe extra care as at some patients perhaps bystry progressing of a gepatorenalny syndrome.

Ability to influence speed of response at control of motor transport or work with other mechanisms. There are no data on influence on ability to drive the car or mechanisms. However it is necessary to consider a possibility of development of vestibular disturbances (dizziness, an incoordination of movements) and to refrain from potentially dangerous works.

Side effects:

Disturbances from a nervous system: ototoxicity (defeat of the VIII couple of cranial nerves). At prolonged use development of neuritis of an acoustical nerve which is shown by noise, a ring or feeling of a congestion in ears, decrease in auditory acuity is possible. The specified symptoms can have irreversible character. The perception of high frequencies (revealed at an audiometriya) is originally broken; the irreversible disturbance of recognition of the speech noticeable for the patient, dobavlyaetsyapozdny.

Damage of a vestibular mechanism is shown by dizziness or вертиго, a lack of coordination of movements. At symmetric damage of a vestibular mechanism these disturbances at the first stages can be imperceptible. Cases of ototoxicity of irreversible character are noted.

Neurotoxicity (encephalopathy, confusion of consciousness, lethargy, hallucinations, depression). Peripheral neuropathy.

The neuromuscular blockade which is shown respiratory depression owing to paralysis of respiratory muscles, a headache, the general weakness, drowsiness, twitching of muscles, paresthesia, spasms is also possible.

From a mochevydelitelnoysistema: nephrotoxicity. The damage of kidneys which is shown a reversible renal failure of usually easy degree is rare – an acute tubular necrosis, intersticial nephrite, reduction in the rate of glomerular filtering (it is observed after several days of treatment or after the therapy termination), increase in level of creatinine in blood serum, a microhematuria, an albuminuria, a cylindruria.

Except high concentration of drug in the blood plasma which is especially increasing risk of development of ototoxicity and nephrotoxicity there are many other risk factors (see. "Features of use").

Disturbances of electrolytic balance: hypomagnesiemia, hypocalcemia, hypopotassemia.

Disturbances from a digestive tract: nausea, vomiting, diarrhea, dysbacteriosis.

From cardiovascular system: arterial hypotension.

From skin of islizisty covers: stomatitis.

Allergic reactions: seldom – rash, an itch, hypostasis, a dermahemia. In isolated cases emergence of anaphylactoid reactions is possible.

Changes together introductions: the irritation and pain in an injection site is possible. Are also possible: hyperemia, bruises, hematoma, consolidation, atrophy or necrosis of hypodermic cellulose.  

From system of a blood coagulation: purpura.

From storonylaboratorny indicators: increase in level of aminotransferases of blood serum, increase in level of bilirubin. Changes from blood (anemia, a leykopeniiya, a granulocytopenia, a trombotsitopeniiya).

Interaction with other medicines:

It is necessary to avoid co-administration with loopback diuretics (furosemide, Acidum etacrynicum) as the last can strengthen ototoksichesky and nephrotoxic effect of Kanamycinum.

Emergence of dysfunctions of breath (respiratory depression and apnoea) owing to neuromuscular blockade at patients to whom along with Kanamycinum not depolarizing muscle relaxants (сукцинилхолин, tubocurarine, dekametony), anesthetics, narcotic analgetik, magnesium sulfate, and also in case of transfusion of a large amount of blood with citrate preservatives are appointed is possible. It is necessary to avoid their co-administration, and if necessary to adjust doses of muscle relaxants and to carry out rigid monitoring of neuromuscular function.

It is necessary to avoid simultaneous and/or consecutive system or topical administration of Kanamycinum with other neurotoxic and/or nephrotoxic means (such as Cisplatinum, other aminoglikozidny antibiotics, polymyxin B, acyclovir, ганцикловир, Amphotericinum In, drugs of platinum and gold, dextrans – Polyglucinum, реополиглюкин, cyclosporine, cephalosporins І generation, капреомицин, Vancomycinum).

At reception of streptomycin, Monomycinum, florimitsin treatment by Kanamycinum can be begun not earlier than in 10 days after the end of treatment with the specified antibiotics.

Mixing of Kanamycinum with penicillin or cephalosporins leads to Kanamycinum inactivation, and at their separate introduction a synergism is observed.

The indometacin, phenylbutazone and other NPVS breaking a renal blood stream can slow down removal of aminoglycosides from an organism.

Simultaneous use of Kanamycinum with intravenous solution of indometacin at premature newborns leads to increase in concentration in a blood plasma, to prolongation of action and strengthening of toxic effect of aminoglycoside.

At tuberculosis Kanamycinum can be applied at the same time with all fixed and reserve antituberculous remedies (an exception – streptomycin, флоримицин and капреомицин), and at infections of not tubercular etiology – with penicillin.

Contraindications:

Hypersensitivity to Kanamycinum and other aminoglycosides in the anamnesis;
neuritis of an acoustical nerve;
myasthenia;
parkinsonism;
botulism;
impassability of intestines;
heavy renal failures (clearance of creatinine less than 10 ml/min.) (see the section "Route of Administration and Doses").

Use during pregnancy or feeding by a breast. Kanamycinum gets into breast milk in small amounts (to 18 mkg/ml) and is badly soaked up from a GIT therefore the related complications at children are not registered. Nevertheless for the period of treatment it is necessary to stop breastfeeding.

Kanamycinum is contraindicated during pregnancy. At use of Kanamycinum during pregnancy cases of inborn deafness were noted. Use of drug is allowed in some cases only according to vital indications when antibiotics of other groups were inefficient or cannot be applied.

Children. At premature children and newborns, in connection with insufficiently developed function of kidneys, longer elimination half-life is noted that can lead to accumulation of drug and its toxic action. Poetomuprimeneniye of Kanamycinum of this category of patients and detyampervy year of life is allowed only on vital to indications.

Overdose:

Overdose symptoms – strengthening of manifestations of side reactions. At parenteral administration emergence of neuromuscular blockade (kurarepodobny action) is possible.

Treatment: the specific antidote does not exist. At symptoms of overdose it is necessary to stop urgently administration of drug and to appoint symptomatic therapy.

In case of blockade or respiratory depression enter прозерин with atropine; if necessary artificial ventilation of the lungs is shown.

At emergence of toxic reactions – peritoneal dialysis or a hemodialysis. Carry out by the newborn exchange hemotransfusion.

Storage conditions:

Period of validity 3 years. To store in original packaging at a temperature not above 20 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe