Vero-Netilmicin (Vero-Netilmicin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceNethylmycinNethylmycin
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  • Vero-Netilmicin
    solution w / m in / in 
    VEROPHARM SA     Russia
  • Nettavisk
    ointment d / eye 
    SIIFI SpA     Italy
  • Nettacine
    drops d / eye 
    SIIFISpA     Italy
    • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the solution contains:

    active substance:

    Nethylmicin sulfate in terms of netilmicin base

    25.0 mg

    100.0 mg

    Excipients:

    Gasoline alcohol

    -

    10 mg

    Disodium Edetate

    0.1 mg

    0.1 mg

    Sodium disulfite (sodium metabisulfite)

    2.1 mg

    2.4 mg

    Sodium sulfite (Sodium sulfite anhydrous)

    1.2 mg

    0.8 mg

    Methylparahydroxybenzoate (Methylparaben)

    1.3 mg

    -

    Propyl parahydroxybenzoate (Propylparaben)

    0.2 mg

    -

    Sodium sulfate (Sodium sulfate anhydrous)

    2.6 mg

    -

    1 M sodium hydroxide solution

    to pH 3.5 - 6.0


    1 M sulfuric acid solution

    to pH 3.5 - 6.0


    Water for injections

    up to 1 ml
    Description:Transparent, colorless or slightly yellowish solution.
    Pharmacotherapeutic group:Antibiotic - aminoglycoside
    ATX: & nbsp

    J.01.G.B   Other aminoglycosides

    J.01.G.B.07   Nethylmycin

    Pharmacodynamics:

    Semisynthetic aminoglycoside bactericidal antibiotic of broad spectrum of action. Communicates with 30S a subunit of ribosomes of microorganisms and violates protein synthesis, preventing the formation of a complex of transport and information RNA,the reading of the genetic code and the formation of non-functional proteins; polyribosomes split and lose the ability to synthesize a protein.

    Nethylmycin is highly active in vivo in respect of the following microorganisms: Escherichia coli, Enterobacter spp., Citrobacter spp., Klebsiella spp., Neisseria gonorrhoeae, Proteus spp. (indole-positive and indole-negative strains, including Proteus mirabilis, Proteus morganii, Proteus vulgaris), Providencia rettgeri, Pseudomonas aeruginosa, Serratia spp.

    In vitro Netilmicin is also active against: Haemophilus influenzae, Salmonella spp., Shigella spp., Morganella morganii, Staphylococcus spp. (pecillin-producing and penicillinase-forming strains, including methicillin-resistant strains), some strains Providencia spp., Acinetobacter spp., Aeromonas spp., Streptococcus spp. Many strains of microorganisms resistant to other aminoglycosides, such as kanamycin, gentamicin, tobramycin and sisomycin in vitro sensitive to netilmicin. The combination of netilmicin with penicillins has a synergistic effect on some strains Streptococcus spp., and with carbenicillin or ticarcillin - against many strains Pseudomonas aeruginosa. Strains Serratia spp., resistant to many antibiotics, are sensitive to a combination of netilmicin with azlocillin, mezlocillin, cefamandol, cefotaxime.

    Pharmacokinetics:

    After intramuscular injection absorbed quickly and completely.The time to reach the maximum concentration in the blood plasma with intramuscular injection is 0.5-1.5 hours. The maximum concentration in the blood plasma with intramuscular injection of netilmicin at a dose of 2 mg / kg is 5.5 μg / ml, after 30 minutes of intravenous infusion in a dose 2 mg / kg-11.8 μg / ml. The connection with plasma proteins is 0-10%.

    It is well distributed in the extracellular fluid (in the contents of abscesses, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal fluids); high concentrations are found in the urine; low in bile, breast milk, bronchial secretion, sputum and cerebrospinal fluid. It penetrates well into all tissues of the body, where it accumulates intracellularly; high concentrations are noted in organs with good blood supply: in the lungs, liver, myocardium, spleen and especially in the kidneys, where accumulates in the cortex, lower concentrations - in muscles, adipose tissue and bones. In therapeutic concentrations in adults does not penetrate the blood-brain barrier, with inflammation of the meninges, the permeability slightly increases. In newborns, concentrations in the cerebrospinal fluid are higher than in adults.Passes through the placenta - found in the blood of the fetus and amniotic fluid.

    The volume of distribution in adults is 0.26 l / kg, in children 0.2-0.4 l / kg, in newborns less than 1 week old and weighing less than 1500 g - up to 0.68 l / kg, at the age of less than 1 week and a body weight of more than 1500 grams - up to 0.58 l / kg, in patients with cystic fibrosis - 0.3-0.39 l / kg. The average therapeutic concentration for intravenous (intravenous) or intramuscular (IM) administration is maintained for 10-12 hours. It is not metabolized.

    Elimination half-life in adults (T1/2) - 2-4 hours, in newborns - 5-8 hours, in older children - 2.5-4 hours. End T1/2 - more than 100 hours (release from the intracellular depot). It is excreted by the kidneys by glomerular filtration (65-94%), mainly unchanged. T1/2 in adults with renal dysfunction varies depending on the degree of disturbance up to 100 h, in patients with cystic fibrosis -1-2 h, in patients with burns and hyperthermia, the half-life can be shorter compared with the average values ​​due to increased clearance.

    It is excreted during hemodialysis (50% for 4-6 hours), peritoneal dialysis is less effective (25% for 48-72 hours).

    Indications:

    Bacterial infections (including severe infections) caused by sensitive microorganisms:

    - sepsis and bacteremia;

    - urinary tract infection and genital tract (including acute uncomplicated gonococcal infection);

    - infections of the respiratory system (including pneumonia, empyema of the pleura, lung abscess);

    - infections of the skin and soft tissues (including infected burns and wounds, including postoperative ones);

    - infection of the abdominal cavity (including peritonitis);

    - infections of the gastrointestinal tract (including acute gonorrhea proctitis);

    - infection of bones and joints.

    In combination with carbenicillin or ticarcillin: infections caused by Pseudomonas aeruginosa.

    In combination with penicillins: endocarditis caused by Streptococcus spp .; suspected sepsis or pneumonia caused by Staphylococcus spp., in newborns.
    Contraindications:

    Hypersensitivity to netilmicin or other components of the drug, as well as to other aminoglycosides, neuritis of the auditory nerve, severe chronic renal insufficiency with azotemia and uremia, pregnancy, lactation, children under 3 years (only for a dosage of 100 mg / ml due to the presence of benzyl alcohol in this form of release).

    Carefully:Myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause a violation of neuromuscular transmission, which leads to further weakening of skeletal muscles), dehydration, renal failure,period of newborns, prematurity of children, old age.
    Pregnancy and lactation:Contraindicated.
    Dosing and Administration:
    Netilmicin is administered in / m and in / in struyno (for 3-5 min) or drip (for 0.5-2 h). The doses recommended for IV and IM are identical. Doses are determined by the severity of the infection and are calculated based on body weight; patients with an increased body weight take into account the ideal body weight, i.е. without taking into account the excess weight of subcutaneous fat. Typically, the duration of therapy with neitilmicin is 7-14 days, sometimes a longer course of treatment may be required. Adults with infections of moderate severity 4-6 mg / kg per day, divided into 3 injections every 8 hours or 2 injections every 12 hours, or 1 injection per day. Adults with a body weight of 50-90 kg usually receive 150 mg every 12 hours or 100 mg every 8 hours. In severe infections, an increase in the dose to 7.5 mg / kg / day, divided into 3 injections every 8 hours, is possible. When the condition improves, the dose is reduced to 6 mg / kg / day (usually after 48 hours).

    In uncomplicated urinary tract infections - once a day at a rate of 3 mg / kg body weight for 7-10 days.

    With gonorrhea in men and women, a single intravenous injection of 300 mg is recommended.Injection of a solution with a concentration of 100 mg / ml should be done deep into the upper outer quadrant of the gluteus muscle, injecting half the dose into each gluteus muscle.

    Children the drug is administered depending on the age and body weight.

    Newborns, incl. premature, at the age of 1 week: 6 mg / kg / day (3 mg / kg every 12 hours); at the age of 1 week and infants up to 1 year: 7.5-9 mg / kg / day (2.5-3.0 mg / kg every 8 hours); children older than 1 year: 6 - 7.5 mg / kg / day (2 - 2.5 mg / kg every 8 hours).

    Patients with impaired renal function Correction of dosing is performed by increasing the intervals between administrations or reducing the single dose. If possible, monitor the concentration of netilmicin in the blood plasma. The following dosing regimens are presented for orientation in the event that it is not possible to determine the content of netilmicin in the blood plasma. In this case, to correct the dose of netilmicin, it is most advisable to focus on the serum creatinine concentration and creatinine clearance (CK).

    Correction by increasing the intervals between the administrations. To calculate the time interval, multiply the value of the concentration of creatinine in the blood plasma (expressed in mg / 100 ml) by 8.(For example, a patient with a body weight of 60 kg with a creatinine concentration of 3 mg / 100 ml can receive 120 mg of the drug (2 mg / kg) every 24 hours (3.0x8).

    Correction of a single dose. Such methods of dose calculation are proposed:

    1. After applying the usual initial dose, an approximate reduced dose is determined (when applied at intervals of 8 hours) by dividing the recommended dose by the value of the creatinine concentration in the blood plasma (Table 1). For example, after applying an initial dose of 120 mg (2 mg / kg), a patient weighing 60 kg and a serum creatinine concentration of 3 mg / 100 ml can receive 40 mg of the drug every 8 hours (120: 3).

    Table 1. Recommendations for dose adjustment for persons with impaired renal function (administration every 8 hours after the introduction of the standard initial dose)

    Concentration of creatinine in blood plasma, mg / 100 ml

    Approximate value of SC, ml / min / 1,73 m2

    Percent

    the standard dose

    <1

    >100

    100

    1,1-1,3

    70-100

    80

    1,4-1,6

    55-70

    65

    1,7-1,9

    45-55

    55

    2-2,2

    40-45

    50

    2,3-2,5

    35-40

    40

    2,6-3

    30-35

    35

    3,1-3,5

    25-30

    30

    3,6-4

    20-25

    25

    4,1-5,1

    15-20

    20

    5,2-6,6

    10-15

    15

    6,7-8

    <10

    10
    2. If the clearance of creatinine is known, the maintenance dose, which is administered every 8 hours, can be calculated by the formula:

    Maintenance dose (every 8 hours) = (patient's CK * value / normal value * CC) x standard maintenance dose.

    * SC ml / min / 1.73 m2.

    The initial dose corresponds to the recommended dose for a patient with undisturbed renal function.

    Patients on hemodialysis should be injected at the end of each hemodialysis procedure at a dose of 2 mg / kg for adults and 2-2.5 mg / kg for children.

    Rules for the preparation and administration of a solution for intravenous administration:

    For IV introduction to adults, the required dose of the drug is diluted in 50-200 ml sterile 0.9% solution of sodium chloride or 5% aqueous solution of dextrose; For children, the volume of the solvent depends on the patient's need for fluids. The resulting solution is introduced dropwise for 0.5-2 hours.

    In some cases, it is permissible to inject the solution directly into the vein or into the venous catheter slowly for 3-5 minutes.

    Side effects:

    From the digestive system: decreased appetite, nausea, vomiting, diarrhea, impaired liver function (increased activity of "liver" transaminases, hyperbilirubinemia).

    From the hematopoiesis: Anemia, leukopenia, granulocytopenia, thrombocytopenia, thrombocytosis.

    From the nervous system: headache, disorientation, neurotoxic action (muscle twitching, numbness sensation, paresthesia), neuromuscular transmission disorder (breathing disorder, weakness), drowsiness.

    From the sense organs: ototoxicity (hearing loss, ringing or feeling in the ears, irreversible deafness, labyrinthine disorders, vestibular disorders, including discoordination of movements, dizziness, nausea, vomiting); impaired vision.

    From the urinary system: nephrotoxicity - a violation of kidney function (increase or decrease in frequency of urination, thirst, oliguria, proteinuria, hematuria, cylindruria, decreased glomerular filtration, increased urea concentration, fluid retention, aminoaciduria, metabolic acidosis); The nephrotoxic effect is usually moderately expressed and reversible.

    From the cardiovascular system: tachycardia, palpitation, lowering of blood pressure.

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

    Laboratory indicators: hyperglycaemia, hyperkalemia, increased prothrombin time, increased activity of alkaline phosphatase (AFP), decreased hemoglobin. Local reactions: soreness at the injection site.

    Overdose:

    Symptoms: toxic reactions (hearing loss, ataxia, dizziness, urination disorders, thirst, loss of 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, cholinesterase inhibitors, calcium salts, artificial ventilation, other symptomatic and supportive therapy.

    Interaction:It should be avoided to use drugs with potential neurotoxic and / or nephrotoxic effects (aminoglycosides, vancomycin, polymyxin In, colistin, platinum preparations, methotrexate (in high doses), ifosfamide, pentamidine, foscarnet, some antiviral agents (acyclovir, ganciclovir, adefovir, cidofovir, tenofovir), amphotericin B, immunosuppressants such as ciclosporin, tacrolimus, and iodine-contrast substances). In the case when it is impossible to avoid joint use with these drugs, during the treatment it is necessary to closely monitor the function of the kidneys of the patient by conducting the necessary laboratory tests.The risk of developing nephrotoxicity is higher in elderly patients and in dehydration.

    When combined with "loop" diuretics (ethacrynic acid, furosemide) the concentration of netilmicin in the blood serum increases, which increases the risk of toxic effects.

    The likelihood of developing neuromuscular blockade and paralysis of the respiratory muscles with concomitant administration with muscle relaxants, anesthetics, polymyxins, halogenated hydrocarbons as a medicament for inhalation anesthesia, opioid analgesics, citrate preservatives in the transfusion of large quantities of conserved blood should be considered. Pharmaceutical interaction

    Nethylmicin is physically compatible with the following listed solutions for parenteral administration, does not lose its activity at a concentration of at least 3 mg / ml when stored in the refrigerator or at room temperature for up to 7 days: sterile water for injection, 0.9% sodium chloride solution, 3% and 5% sodium chloride solution, 5% dextrose solution, injection solution containing 5% dextrose solution and 0.9% sodium chloride solution, 50% dextrose solution,5% sodium hydrogen carbonate solution, 6% solution of Dextran 75 in 5% dextrose solution, 10% solution of dextran 40, 10% solution of dextrin 40 in a 5% dextrose solution, 10% dextrose, Ringer's solution, Ringer's lactate, Ringer's lactate solution 5% dextrose solution, amino acid solutions for parenteral nutrition, 10% fructose solution.

    In vitro mixing aminoglycosides with beta-lactam antibiotics (penicillins or cephalosporins) can lead to significant mutual inactivation.

    Special instructions:

    The use of netilmicin is recommended as an initial therapy for infections caused by gram-negative microorganisms; if suspected of such an infection, the decision to continue therapy should be taken based on the results of the sensitivity tests and based on the clinical efficacy of the therapy in this patient and the tolerability of the drug. In severe infections and an unidentified pathogen netilmicin can be prescribed and as an initial therapy in combination with antibiotics from the penicillin or cephalosporin group until the results of the sensitivity tests are obtained.If anaerobic flora is suspected in combination with non-linimentin, appropriate antibiotic therapy should be given. After identifying the pathogen and determining its sensitivity, it is necessary to continue the administration of netilmicin or other appropriate antimicrobial therapy. The possibility of using netilmicin should be considered when treating severe staphylococcal infections, when there are contraindications to the use of penicillins or other less toxic antibiotics, and tests for determining the sensitivity of microorganisms and evaluating clinical data indicate the possibility of using the drug. The possibility of using netilmitin should be considered in the treatment of mixed infections caused by susceptible strains of staphylococci and gram-negative microorganisms.

    With a long course of treatment (more than 7-10 days), it is necessary to periodically monitor kidney function (general urine analysis, creatinine clearance, urea concentration in the blood plasma, creatinine), determine electrolyte balance and auditory nerve function.

    During the treatment period, it is desirable to monitor the concentration of the drug in the plasma.

    The likelihood of developing toxic effects is higher in patients with impaired renal function, as well as in the administration of high doses or for a long time (this category of patients may require daily monitoring of kidney function).

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

    There are reports of complete irreversible bilateral deafness in children whose mothers received aminoglycosides (incl. netilmicin) during pregnancy. If netilmicin was used during pregnancy or pregnancy occurred during the treatment with neilimmicin, it is necessary to warn the woman about the potential harm to the fetus. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

    The concentration of the drug in the blood serum in patients with hyperthermia or anemia may be somewhat lower due to a shorter T1/2 (correction of the dosing regimen is usually not required).

    In patients with extensive burns, there may be a decrease in the concentration of netilmicin in the serum, which may require an increase in the administered dose.

    Patients with infectious and inflammatory diseases of the urinary tract is recommended to take an increased amount of liquid.

    In the absence of positive clinical dynamics, one should remember the possibility of the development of resistant microorganisms (it is necessary to cancel treatment and begin appropriate therapy).

    The risk of toxic effects increases in elderly patients and with dehydration.

    The composition of the drug includes sodium metabisulphite and sodium sulfite, which can cause severe allergic reactions (including anaphylactic) in sensitive people, as well as an attack of bronchospasm.

    Among the aminoglycosides, cross allergic reactions were noted.

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

    Information on the effect of netilmicin on the ability to drive vehicles and other mechanisms is not available. However, given the possible side effects (incl. visual impairment) should be careful when doing this kind of activity.

    Form release / dosage:

    Solution for intravenous and intramuscular administration, 25 mg / ml and 100 mg / ml (50 mg / 2 ml, 200 mg / 2 ml).

    Packaging:2 ml per ampoule of neutral glass.

    1 or 10 ampoules in a box of cardboard or in a pack of cardboard with partitions or a liner of paper.

    1 or 10 ampoules in a contour cell box made of a polyvinylchloride film and aluminum foil printed lacquered or foil-free.

    One contour pack in a pack of cardboard.

    Each instruction box or bundle contains instructions for use, an ampoule opener or ampoule scarifier.

    When using ampoules with a notch or rupture ring, the ampoule scaler or knife for opening ampoules is not inserted.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005996/10
    Date of registration:25.06.2010 / 02.10.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp01.02.2017
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