Active substanceTeicoplaninTeicoplanin
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    lyophilizate
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  • Teicoplanin
    lyophilizate inwards w / m in / in 
    JODAS EKSPOIM, LLC     Russia
  • Dosage form: & nbsplyophilizate for the preparation of solution for intravenous and intramuscular administration
    Composition:

    Targcid®, 200 mg

    1 bottle contains:

    active substance: teicoplanin * - 200 ** mg;

    Excipients: sodium chloride - 24.0 mg, sodium hydroxide - up to pH 7.5.

    Composition of the applied solvent: water for injection - 3 ml.

    Targocid®, 400 mg

    1 bottle contains:

    active substance: teicoplanin * - 400 ** mg;

    Excipients: sodium chloride - 24.8 mg, sodium hydroxide - up to pH 7.5.

    Composition of the applied solvent: water for injection - 3 ml.

    * - teicoplanin is a mixture of 50% monosodium salt and 50 % zwitterion ions.

    ** - is put in excess of 10% (200 mg + 20 mg = 220 mg) or 15 % (400 mg + - 60 mg = 460 mg), since part of the drug in the form of a solution is not extracted from the vial.

    Description:Description of the contents of the bottle: a porous homogeneous mass of light yellow color Description of the contents of the ampoule with a solvent: clear and colorless liquid.
    Pharmacotherapeutic group:Antibiotic glycopeptide.
    ATX: & nbsp

    J.01.X.A.02   Teicoplanin

    Pharmacodynamics:

    Teykoplanin is an antibiotic of a glycopeptide structure demonstrating in vitro bactericidal activity against anaerobic and aerobic Gram-positive microorganisms. Teicoplanin suppresses the growth of sensitive microorganisms by inhibiting the biosynthesis of the microbial cell membrane in places other than those in the envelope of the microbial cells, which are affected by beta-lactam antibiotics.

    Teicoplanin has activity against Staphylococcus spp. (including strains resistant to methicillin and other beta-lactam antibiotics), Streptococcus spp., Enterococcus spp., Listeria monocytogenes, Micrococcus spp., Corenebacterum spp. groups J/K and Gram-positive anaerobes, including Clostridium difficile, Peptococcus spp.

    In vitro synergism was demonstrated with respect to bactericidal action on Staphylococcus aureus when combining teicoplanin with aminoglycosides or imipenem. In vitro additive and synergistic effects in relation to Staphylococcus aureus showed a combination of teicoplanin and rifampicin. In a relationship Staphylococcus epidermidis Synergism of teicoplanin with ciprofloxacin was observed.

    In vitro One-step resistance to teicoplanin was not obtained, and only after multiple passages in vitro multistage resistance was developed. An increase in the minimum inhibitory concentrations (MIC) of teicoplanin was reported for some strains of hemolytic staphylococci.

    As a rule, teicoplanin does not exhibit "cross-resistance" with antibiotics of other groups, however, Enterococcus spp. there was a small "cross-resistance" to teicoplanin and another glycopeptide, vancomycin. When determining the sensitivity of microorganisms to teicoplanin, discs (sensidiski) containing 30 micrograms of teicoplanin are used. Strains in which the growth inhibition zone has a diameter of 14 mm or more are considered to be sensitive, the same strains whose growth inhibition zone is 10 mm in diameter or less are considered resistant.

    Pharmacokinetics:

    Bioavailability after a single intramuscular injection of teicoplanin at a dose of 3-6 mg / kg body weight is about 90%.

    After oral administration teicoplanin Not absorbed and in the absence of lesions of the digestive system does not enter the systemic circulation; 40% of the ingested dose is present in the feces in a microbiologically active form.

    The study of the profile of plasma concentrations of teicoplanin in humans after its intravenous administration at a dose of 3-6 mg / kg showed a two-phase distribution of teicoplanin (with a fast distribution phase with a plasma half-life of about 0.3 hours followed by a phase of a slower distribution with a half-life from the plasma, which is about 3 hours), after which a slow removal of teicoplanin with a finite half-life of about 150 hours is observed. Such a long half-life period allows the drug to be administered once a day.

    With the intravenous administration of Targoside® at a dose of 6 mg / kg of body weight as a 30-minute infusion three times in 12 hours and then once a day (every 24 hours), the minimum plasma teicoplanin concentration of 10 mg / l could be is reached by the 4th day. The calculated maximum and minimum plasma concentrations in the equilibrium state of 64 mg / L and 16 mg / L could be achieved by the 28th day of treatment. Teicoplanin quickly spreads into the skin (subcutaneous fat) and blister fluid, myocardium, lung tissue and pleural fluid, bone tissue and synovial fluid, but poorly penetrates into the cerebrospinal fluid.Weakly affinity binding with plasma proteins is 90-95%. The volume of distribution in the equilibrium state with intravenous administration of teicoplanin at a dose of 3-6 mg is 0.94-1.41 l / kg. The volume of distribution in children does not differ significantly from that in adults.

    After parenteral administration of teicoplanin, its metabolism is minimal (about 3%). 97% of injected teykoplanin is excreted from the body in unchanged form. Approximately 80% of the administered dose is excreted by the kidneys. Renal clearance after intravenous administration of 3-6 mg / kg is in the range of 10.4 - 12.1 mg / h / kg. The total plasma clearance is in the range of 11.9-14.7 ml / h / kg.

    Indications:

    Severe infections caused by drug-sensitive Gram-positive bacteria, including those resistant to other antibiotics (such as penicillins, including methicillin, and cephalosporins), including these infections in patients who are allergic to penicillins and cephalosporins:

    - endocarditis;

    - septicemia;

    - infection of bones and joints;

    - infections of the lower respiratory tract;

    - infections of the skin and soft tissues;

    - urinary tract infections;

    - peritonitis, which occurred with continuous ambulatory peritoneal dialysis (AHTD).

    Prevention of infectious complications in dental and orthopedic operations with the risk of developing infections caused by Gram-positive microorganisms.

    For oral administration: pseudomembranous colitis caused by Clostridium difficile (associated with the use of antibacterial drugs).

    Contraindications:

    - Hypersensitivity to teicoplanin and other components of the drug.

    Carefully:

    - In patients with increased sensitivity to vancomycin (risk of "cross-over" hypersensitivity).

    - In patients with renal insufficiency (correction of the dosing regimen is required, see the section "Dosing and Administration", and monitoring of the hearing, hematological parameters, kidney and liver function).

    - Patients undergoing long-term treatment (monitoring of the hearing, hematological parameters, kidney and liver function).

    - With simultaneous treatment with other ototoxic and nephrotoxic drugs: aminoglycosides, colistin, amphoteric B, cyclosporin, cisplatinum, furosemide and ethacrynic acid.

    Pregnancy and lactation:

    Do not use Targosis® during pregnancy or if it is suspected, except when the potential benefit to the mother prevails over the possible harm to the fetus.

    Studies in animals have not revealed teratogenic effects in teicoplanin.

    Breastfeeding period

    Information on the excretion of teicoplanin in breast milk is absent. If it is necessary to use the drug during lactation, the question of temporary discontinuation of breastfeeding should be resolved.

    Dosing and Administration:

    Teicoplanin is administered parenterally (intravenously or intramuscularly). Intravenous (IV) administration can be performed by either intravenous injection for 3-5 minutes, or - IV infusion for 30 minutes. In newborns, the drug should be administered only as an intravenous infusion.

    Dosing regimen in adults and adolescents 16-18 years with normal renal function

    Treatment of infections caused by drug-sensitive gram-positive bacteria (endocarditis, septicemia, bone and joint infections, lower respiratory tract infections, skin and soft tissue infections, urinary tract infections) For moderately severe infections of the skin and soft tissues, urinary tracts, lower respiratory tract infections, the initial dose of teicoplanin is 400 mg once iv on the first day, followed by a maintenance dose of 200 mg once daily in / in or intramuscularly (IM).

    For treatment of severe infections of bones and joints, septicemia, endocarditis, the initial dose is 400 mg IV every 12 hours for the first three doses followed by a maintenance dose of 400 mg IV or IM once daily. In severe infections, the minimum concentration in serum should not be less than 10 mg / L. Maximum concentrations, determined 1 hour after iv injection of 400 mg, are usually in the range of 20 to 50 mg / l.

    In some cases (in burn patients or in patients with endocarditis), the maintenance dose may be up to 12 mg / kg of body weight per day. Standard doses of 200 mg and 400 mg correspond to doses of 3 mg / kg and 6 mg / kg of body weight. In patients with a body weight of more than 85 kg, it is recommended to adjust the dose of the drug taking into account the body weight, adhering to the same therapeutic regimen: moderately severe infections of 3 mg / kg, severe infections of 6 mg / kg.

    Patients with peritonitis developed as a complication of continuous ambulatory peritoneal dialysis

    After a single loading dose of 400 mg intravenously, in the first week, 20 mg / l is injected into each tank with peritoneal dialysis solution, in the second week, 20 mg / l is administered per each second peritoneal dialysis solution reservoir in The third week is administered at a dose of 20 mg / l to a tank with peritoneal dialysis solution for night dialysis.

    Antimicrobial prophylaxis in surgical operations in orthopedics, dental operations (for example, endocarditis prophylaxis in patients with artificial heart valves): 400 mg teicoplanin (or 6 mg / kg with a patient weight of more than 85 kg) as an IV injection once during anesthesia. Pseudomembranous colitis caused by C. difficile: 200 mg of teicoplanin orally two times a day.

    Dosage regimen in children

    Children over 2 months to 16 years of age: for most Gram-positive infections, the recommended initial dose is 10 mg / kg body weight IV with an interval of 12 hours for the first three doses, with the transition to a maintenance dose of 6 mg / kg body weight given in / m or / once a day.

    In severe infections and neutropenia, the recommended initial dose is 10 mg / kg body weight IV with an interval of 12 hours for the first three doses with the transition to a maintenance dose of 10 mg / kg body weight administered / once a day.

    Children younger than 2 months, including newborns: the recommended initial dose is 16 mg / kg body weight IV on the first day with the transition to a maintenance dose of 8 mg / kg body weight IV once a day. IV administration should be carried out by iv infusion for 30 minutes.

    Dosage regimen in elderly patients

    With normal kidney function, dosage adjustment is not required.

    Dosing regimen in adults with renal insufficiency

    Until the 4th day of treatment with teicoplanin, correction of the dosing regimen is not required. Beginning on the fourth day, the administered dose should maintain the teicoplanin concentration in the serum at a level of 10 mg / L.

    With moderate renal failure (creatinine clearance 40-60 ml / min): the maintenance dose should be reduced by half, either by introducing the previous dose once every two days, or by administering a half dose once a day.

    In severe renal failure (creatinine clearance less than 40 ml / min) and in patients on hemodialysis: the maintenance dose should be reduced threefold,either by administering the previous dose every third day, or introducing 1/3 of the previous dose once a day.

    Teikoplanin is not excreted by hemodialysis.

    Duration of treatment

    The response therapeutic response in most patients with infections caused by susceptible antibiotics is observed within 48-72 hours after the start of the drug administration. The total duration of treatment is determined individually and depends on the type and severity of the infection and the clinical response of the individual patient. With endocarditis and osteomyelitis, treatment is recommended for 3 weeks or more; while Targotsid® should not be administered for more than 4 months. Preparation of the solution

    All contents of the ampoule with sterile water should be slowly introduced into the tare of the Targotsid® preparation, gently shaking the bottle until the powder completely dissolves, while avoiding the formation of foam. It is very important that the whole preparation is dissolved, even the part that is near the cork.

    When the solution is shaken, a foam is formed, which makes it difficult to extract the required volume of the solution. However, if teicoplanin the foam does not change the concentration of the remaining solution of 200 mg / 3 ml in the bottle of the drug Targosid® 200 mg and 400 mg / 3 ml in the Targocid® 400 mg bottle. If the solution turns frothy, then leave it to stand for about 15 minutes to reduce the amount of foam.

    It is necessary to slowly extract the teicoplanin solution from the vial, trying to extract it completely, piercing the middle of the rubber cork with a needle.

    The resulting solution will contain 200 mg of teicoplanin in 3 ml in a 200 mg Targogid® and 400 mg in 3 ml bottle of Targogid® 400 mg.

    It is important that the preparation of the solution is carried out correctly, and the solution is carefully removed from the vial; improper preparation of the solution can lead to a lower dose than required.

    The prepared solution is isotonic and has a pH of 7.2-7.8.

    The prepared solution can be directly injected or further diluted with 0.9% sodium chloride solution, Ringer's solution, Hartman's solution, 5 % dextrose solution, peritoneal dialysis solution containing 1.36 % or 3.86 % dextrose.

    Side effects:

    Typically, Targotsid® is well tolerated. Undesirable reactions rarely require withdrawal of treatment and in most cases are moderate and transient: severe unwanted reactions are rare. The undesirable reactions listed below were recorded.

    Local Reactions

    Erythema, pain at the injection site, thrombophlebitis, abscess in place of the / m injection. Allergic reactions

    Rash, itching, fever, chills, bronchospasm, anaphylactic reactions, anaphylactic shock, hives, angioedema, rare reports of exfoliative dermatitis, toxic epidermal necrolysis, erythema multiforme, including Stevens-Johnson syndrome.

    In addition, there have been reports of infusion-related reactions, such as erythema or blood tides to the upper body, with no history of prior treatment with teicoplanin, and they did not repeat with subsequent administration of the drug at a reduced rate or concentration of the drug. These cases were not specific for any specific concentration of the infusion solution and the rate of infusion.

    From the gastrointestinal tract Nausea, vomiting, diarrhea.

    From the side of the blood

    Agranulocytosis, leukopenia, neutropenia, thrombocytopenia, eosinophilia.

    From the liver and biliary tract

    Increased activity of "liver" transaminases and (or) alkaline phosphatase in the blood serum.

    From the side of the kidneys

    Increased serum creatinine concentrations, renal failure.

    From the central nervous system

    Dizziness; headache, convulsions with intravenous administration.

    Hearing disorders and labyrinthine disorders Hearing loss, ringing in the ears and vestibular disorders.

    Other

    Superinfection (excessive reproduction of microorganisms insensitive to the drug).
    Overdose:

    Experience of overdose in humans

    There have been reports of cases of excessive doses administered by mistake to children of childhood. In one report, excitation was observed in a 29-day newborn who received 400 mg of teicoplanin IV (95 mg / kg body weight). In all other cases, there were no symptoms or abnormalities of laboratory indicators associated with an overdose of teicoplanin. The age of patients with an overdose ranged from 1 month to 8 years. By mistake, doses from 35.7 mg / kg to 104 mg / kg were administered.

    Treatment of overdose

    Teikoplanin is not excreted by hemodialysis. Treatment of an overdose should be symptomatic.

    Interaction:

    FROM pefrotoksicheskimi and ototoxic drugs (streptomycin, neomycin, kanamycin, gentamycin, amikacin, tobramycin, tsefaloridinom, colistin, amphotericin B, cyclosporine, cystatin, furosemide, ethacrynic acid) When combined with the above drugs, the risk of side effects may increase with simultaneous or sequential application of teicoplanin with these drugs.

    Teicoplanin is pharmaceutically incompatible with aminoglycosides.

    Special instructions:

    Targotsid® be administered with caution in case of known hypersensitivity to vancomycin as possible to develop "cross" allergy. A toxic effect on the organ of hearing, hematologic, hepatic and renal toxicity of teicoplanin has been reported. Therefore it is necessary to monitor the status of hearing, haematological indices, functional state of the liver and kidney, especially in patients with renal failure patients, patients in which the treatment is carried out long and teicoplanin patientssimultaneously receiving treatment with other oto- and nephrotoxic drugs (aminoglycosides, colistin, amphotericin B, cyclosporin, cisplatinum, furosemide and ethacrynic acid).

    Superinfection: as in the case of other antibiotics, the use of teicoplanin. especially if it is prolonged, can lead to excessive reproduction of microorganisms insensitive to the preparation (bacteria or fungi); In case of development of superinfection during treatment with the drug, it is necessary to take appropriate measures.

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

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.

    Form release / dosage:

    Lyophilizate for the preparation of a solution for intravenous and intramuscular injection 200 mg, 400 mg (complete with a solvent).

    Packaging:

    For 200 mg or 400 mg of the active substance in a vial of colorless glass (type I). The bottle is sealed with a rubber stopper, crimped with an aluminum cap and covered with a protective plastic lid type "flip-off" yellow (for a dosage of 200 mg) or green (for a dosage of 400 mg).

    To 3 ml of solvent in ampoule of colorless glass (type I) with a break point 1 bottle and 1 ampoule together with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    3 years Thinner: 5 years

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001940
    Date of registration:18.12.2012
    Date of cancellation:2017-02-10
    The owner of the registration certificate:Aventis Pharma LimitedAventis Pharma Limited United Kingdom
    Manufacturer: & nbsp
    Representation: & nbspAventis Pharma Co., Ltd.Aventis Pharma Co., Ltd.India
    Information update date: & nbsp10.02.2017
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