Active substanceAmikacinAmikacin
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  • Dosage form: & nbspPowder for solution for infusion and intramuscular injection
    Composition:

    Per 1 bottle:

    Amicacin Sulfate (in terms of amikacin) 500 mg.

    Description:The powder is white or almost white.
    Pharmacotherapeutic group:Antibiotic-aminoglycoside
    ATX: & nbsp

    J.01.G.B.06   Amikacin

    Pharmacodynamics:

    Semisynthetic broad-spectrum antibiotic, kanamycin derivative. It is bactericidal. Communicating with 30S a subunit of ribosomes, prevents the formation of a complex of transport and matrix RNA, blocks the synthesis of protein, and also destroys the bacterial cell membranes. Highly active in vitro in a relationship Pseudomonas spp. (incl. Pseudomonas aeruginosa), Escherichia coli, indol-positive and indolotricative strains Proteus spp., Providencia spp., Klebsiella pneumoniae, Enterobacter cloacae, Serratia spp., Acinetobacter spp. and Citrobacter freundii. Active in vitro for most strains Pseudomonas aeruginosa and other gram-negative bacteria resistant to tobramycin, gentamicin and netilmicin.

    Also active in vitro with respect to the production and non-producing penicillinase Staphylococcus spp., including strains resistant to methicillin; moderately active against Streptococcus pyogenes, Enterococcus spp. and Streptococcus pneumoniae.

    Amicacin is resistant to most bacterial enzymes that destroy gentamicin, tobramycin and kanamycin.

    In combination with beta-lactam antibiotics acts synergistically with respect to clinically significant Gram-negative bacteria.

    To determine the sensitivity of isolated pathogens disco-diffusion (according to the Kirby-Bauer method), discs containing 30 μg of amikacin are used. With a diameter of a growth free zone of 17 mm or more, the microorganism is considered sensitive, from 15 to 16 mm - moderately sensitive, less than 14 mm - resistant.

    Pharmacokinetics:

    After intramuscular (IM injection) absorbed quickly and completely. Maximum serum concentrations (Cma) after a single intravenous injection at doses of 250 mg (3.7 mg / kg), 375 mg (5 mg / kg), 500 mg (7.5 mg / kg) are achieved after approximately 1 hour and are 12, 16 and 21 μg / ml, respectively. After 10 hours, the serum concentrations were 0.3 μg / ml, 1.2 μg / ml and 2.1 μg / ml, respectively.

    Studies in healthy volunteers revealed good local tolerability of amikacin after repeated I / m injections. When administered at the maximum recommended doses, oto- and nephrotoxicity were not observed. Data indicating the cumulation of the drug after repeated administration within 10 days was not revealed.

    It is excreted by the kidneys in an unchanged form, mainly by glomerular filtration. After the / m introduction about 92% of the administered dose is withdrawn within 8 hours and 98% - within 24 hours.

    In newborns with different body weight (less than 1.5 kg, 1.5 to 2 kg, more than 2 kg), T1 / 2 depends on the renal clearance of amikacin, body weight and age. The volume of distribution indicates a preferential distribution of amikacin in the extracellular fluid. After repeated intramuscular injections at a dose of 7.5 mg / kg every 12 hours for 5 days, the cumulation effect was not observed.

    After a single intravenous (IV) infusion at a dose of 500 mg Cmah - 38 mcg / ml.After 30 minutes, 1 hour and 10 hours, the concentration of amikacin in serum was 24 μg / ml, 18 μg / ml and 1 μg / ml. It is excreted by the kidneys unchanged: 84% of the administered dose for 9 hours and 94% - within 24 hours after intravenous administration.

    The half-life (T1 / 2) in adults with normal renal function is about 2 hours. The volume of distribution is 24 liters. Communication with blood proteins varies from 0 to 10%. The serum clearance, on average, is 100 ml / min with creatine clearance of 94 ml / min.

    In patients with impaired renal function or reduced filtration pressure in the glomeruli, the excretion of amikacin slows, T1 / 2 increases.

    After intravenous or IV injections at recommended doses, therapeutic concentrations are determined in the bones, heart, gall bladder, lung tissue, as well as in bile, bronchial secretions, urine, interstitial, pleural and synovial fluids. In newborns, the concentration of amikacin in the cerebrospinal fluid is 10-20% of the serum; this figure can be increased to 50% with inflammation of the meninges. Passes through the placenta and is found in fetal blood and amniotic fluid.

    Indications:Treatment of infections caused mainly by Gram-negative microorganisms, including those resistant to gentamicin, kanamycin and tobramycin,or associations of gram-positive and gram-negative microorganisms: bacterial septicemia (including sepsis in newborns), respiratory infections, bone and joint infections, central nervous system infections (including meningitis), skin and soft tissue infections, intra-abdominal infections (including peritonitis) , burn and wound infections, postoperative infectious complications (including complications after vascular surgery), severe recurrent urinary tract infections.
    Contraindications:

    Hypersensitivity (including other aminoglycosides in the anamnesis), defeat of the VIII pair of cranial nerves, severe chronic renal failure with azotemia and uremia, pregnancy.

    Carefully:

    Myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause disruption of neuromuscular transmission, which leads to further weakening of skeletal muscles); conditions accompanied by dehydration; kidney failure; period of newborns, prematurity of children; elderly age.

    Pregnancy and lactation:

    Amikacin is contraindicated in pregnancy.

    If you need to use the drug during lactation, breastfeeding is discontinued.

    Dosing and Administration:

    Enter intramuscularly (in / m) and intravenously (intravenously) drip.

    Adults and children older than 1 month 5 mg / kg every 8 hours or 7.5 mg / kg every 12 hours. The maximum daily dose is 15 mg / kg / day, but not more than 1.5 g / day.

    For treatment of uncomplicated urinary tract infections in adults, 250 mg IM is administered every 12 hours.

    In newborns treatment starts with the introduction of an initial (loading) dose of 10 mg / kg, then administered at 7.5 mg / kg every 12 hours.

    The duration of treatment is, on average, 7-10 days.

    Table 1 presents the doses of amikacin in children and adults, depending on the mode of administration chosen.

    Table 1.

    Body weight, kg

    Dosing regimen

    7.5 mg / kg every 12 hours

    5 mg / kg every 12 hours

    45

    337.5 mg

    225 mg

    50

    375 mg

    250 mg

    55

    412.5 mg

    275 mg

    60

    450 mg

    300 mg

    65

    487.5 mg

    325 mg

    70

    525 mg

    350 mg

    75

    562.5 mg

    375 mg

    80

    600 mg

    400 mg

    85

    637.5 mg

    425 mg

    90

    675 mg

    450 mg

    95

    712.5 mg

    475 mg

    100

    750 mg

    500 mg

    Dosing in patients with impaired renal function

    There are the following ways to correct the dosing regimen in patients with impaired renal function:

    1) it is possible to increase the interval between the administration of medium doses of amikacin,which is determined by the formula: interval (h) = concentration of creatinine (mg / 100 ml) x 9; for example, at a serum creatinine concentration of 2 mg / 100 ml, 7.5 mg / kg administered every 18 hours;

    2) for the selection of a dose of amikacin administered at a fixed time interval are guided by the therapeutic monitoring data; here Cmah, measured 60 minutes after IM or after IV infusion, should not exceed 35 μg / ml; if it is not possible to determine the concentration of amikacin in the blood serum, the treatment starts with the usual therapeutic dose of 7.5 mg / kg as a loading dose; the maintenance dose is calculated in accordance with the creatinine clearance according to the formula

    supportive dose = Creatinine clearance in the patient, ml / min / Creatine clearance is normal, ml / min X The loading dose, mg / kg

    and administered every 12 hours.

    Rules for the preparation of solution and administration

    To prepare a solution for the / m introduction, the contents of the vial are dissolved in 2-3 ml of water for injection. Enter deeply intramuscularly into areas of the body with a pronounced muscular layer (upper-outer quadrant of the buttock or lateral surface of the thigh). It is recommended that an aspiration test be carried out to avoid undesirable introduction of the solution into the blood vessel.

    To prepare a solution for IV infusion, the contents of the vial are dissolved in 3-5 ml of water for injection. The resulting solution is transferred to 100-200 ml of a compatible infusion medium - 0.9% sodium chloride solution, 5% dextrose solution, an aqueous solution containing 5% dextrose and 0.2% sodium chloride, an aqueous solution containing 5% dextrose and 0, 45% sodium chloride, Ringer's lactate solution, Normosol M solution or Plasma-Lit solution 148. The concentration of amikacin in the solution for intravenous administration should not exceed 5 mg / ml. Enter in / in the drip for 30-60 minutes. In children, the volume of injected fluid should be reduced depending on the dose of the antibiotic. The duration of IV infusion in infants is 1 -2 hours.

    Side effects:

    From the nervous system: headache, drowsiness, neurotoxic effect (muscle twitching, numbness sensation, tingling sensations, epileptic seizures), violation of neuromuscular transmission (including paralysis of the respiratory musculature).

    From the sense organs: ototoxicity (hearing loss, vestibular and labyrinthine disorders, irreversible deafness), toxic effect on the vestibular apparatus (discoordination of movements, dizziness, nausea, vomiting).

    From the urinary system: nephrotoxicity - renal dysfunction (oliguria, proteinuria, microhematuria, hypercreatininaemia, azotemia).

    From the digestive system: nausea, vomiting, increased activity of "liver" transaminases, hyperbilirubinemia.

    On the part of the organs of hematopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia.

    Allergic reactions: skin rash, itching and hyperemia of the skin, fever, eosinophilia, angioedema.

    Local reactions: pain in the injection site.

    Other: arthralgia.
    Overdose:

    Symptoms: hearing loss, ataxia, dizziness, urination disorders, thirst, decreased appetite, nausea, vomiting, ringing or feeling in the ears, respiratory failure.

    Treatment: for the removal of the blockade of the neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis. To improve neuromuscular conduction, anticholinesterase medications are administered (neostigmine methylsulfate), as well as calcium preparations. In severe cases of respiratory depression, artificial ventilation is necessary.

    Interaction:

    When used simultaneously with carbenicillin, benzylpenicillin,Cephalosporins have a pronounced synergism of antimicrobial action (in patients with severe renal insufficiency, due to high serum concentrations, beta-lactam antibiotics can reduce the effect of aminolucosides). Pharmaceutically incompatible with penicillins, cephalosporins, heparin, capreomycin, amphotericin B, erythromycin, group B vitamins and ascorbic acid. When used simultaneously, they should not be mixed in one syringe or one infusion medium; with the / m introduction to enter into different parts of the body; when iv introduction introduce separately.

    Nalidixic acid, polymyxin AT, cisplatin and vancomycin increase the risk of oto and nephrotoxicity.

    Diuretics (ethacrynic acid and furosemide), cephalosporins, penicillins, sulfonamides and non-steroidal anti-inflammatory drugs (incl. indomethacin), competing for active secretion in the tubules of the nephron, block the elimination of aminoglycosides, increase their concentration in the serum, enhancing nephro- and neurotoxicity.

    Enhances the muscle relaxant effect of nondepolarizing muscle relaxants. Polymyxins for parenteral administration, capreomycin and other drugs that block neuromuscular transmission (including halogenated hydrocarbons as drugs for inhalation anesthesia), transfusion of large amounts of blood with citrated preservatives increases the risk of stopping breathing.

    Reduces the effect of antimiasthenic drugs.

    Special instructions:

    Patients receiving treatment with amikacin, especially with urinary tract infections, are advised to take an increased amount of fluid.

    Whenever possible, therapeutic drug monitoring should be used to prevent the administration of low ineffective doses or, conversely, drug overdose. Therapeutic concentrations of amikacin are: peak (measured after 30-90 minutes after administration) not more than 35 mg / ml and residual (measured before the introduction of the next dose) not more than 10 μg / ml.

    In the period of treatment with amikacin, it is necessary to monitor the function of the kidneys, pre-collar nerve and vestibular apparatus at least once a week.

    The probability of oto and nephrotoxicity is higher in patients with impaired renal function (including in the elderly),and also with the appointment of high doses of antibiotic. Such patients may require daily monitoring of kidney function.

    When unsatisfactory audiometric tests, the dose of the drug is reduced or discontinued.

    It is not recommended to take the drug for more than 14 days, since the safety of its use beyond this time has not been established. In the absence of positive clinical dynamics should be remembered the possibility of developing resistant microorganisms. In such cases, it is necessary to cancel treatment and begin appropriate therapy. It is advisable to avoid the simultaneous use of oto- and nephrotoxic drugs.

    Effect on the ability to drive transp. cf. and fur:

    Studies on the effect of amikacin on the performance of potentially hazardous activities requiring special attention and rapidity of reactions have not been conducted. Given the possible development of dizziness, drowsiness with the use of amikacin, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:Powder for solution for infusion and intramuscular injection 500 mg.
    Packaging:

    500 mg of active substance into 10 ml glass vials, hermetically sealed with rubber stoppers, crimped with aluminum caps or crimped caps with combined (aluminum with safety plastic covers).

    The solvent - "Water for injection" in glass ampoules of 5 ml.

    1) 1 bottle with the drug and instructions for use are placed in a pack of cardboard.

    2) 1 bottle with the drug and 1 ampoule with solvent are packed in a contour mesh box made of polyvinyl chloride film and foil of aluminum lacquered or without foil. One contour mesh package and instructions for use are put in a pack of cardboard.

    3) 5 bottles of the drug are packed in contour mesh packaging from polyvinyl chloride film and foil of aluminum lacquered or without foil. One contour mesh package and instructions for use are put in a pack of cardboard.

    4) 5 bottles with the preparation complete with 5 ampoules of the solvent are packed in contoured cell packs made of polyvinylchloride film and foil of aluminum lacquered or without foil.One contour mesh package with the preparation, one contour mesh package with a solvent and instruction for use is put in a pack of cardboard.

    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001384
    Date of registration:20.12.2011 / 15.02.2013
    Expiration Date:20.12.2016
    The owner of the registration certificate:ABOLMED, LLC ABOLMED, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp03.08.2017
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