Active substanceVancomycinVancomycin
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  • Dosage form: & nbsplyophilizate for solution for infusion
    Composition:

    Per one vial:

    Active substance: vancomycin hydrochloride (in terms of vancomycin) 0.5 g and 1.0 g containing mannitol (mannitol).

    Description:Powder from white to white with a pink or light brown color.
    Pharmacotherapeutic group:Antibiotic glycopeptide
    ATX: & nbsp

    J.01.X.A.01   Vancomycin

    J.01.X.A   Antibiotics of the glycopeptide structure

    Pharmacodynamics:

    Vancomycin is a tricyclic glycopeptide antibiotic, produced Amycolatopsis orientalis, bactericidal effect on most microorganisms (on Enterococcus spp. - bacteriostatically). It blocks the synthesis of the bacterial cell wall in a region different from that of penicillins and cephalosporins (does not compete with them for binding sites), firmly linking to D-alanyl-D-alanine part of the precursor of the cell wall, which leads to cell lysis.

    It is active against Gram-positive microorganisms, including: Staphylococcus aureus and Staphylococcus epidermidis (including heterogeneous methicillin-resistant strains), Streptococcus spp., Enterococcus spp. (in t.h. Enterococcus faecalis), Clostridium spp. (in t.h. Clostridium difficile).

    To vancomycin in vitro sensitive Listeria monocytogenes, genera of bacteria Lactobacillus spp., Actinomyces spp., Bacillus spp.

    The optimum action is when pH 8, when the pH is reduced to 6, the effect decreases sharply.

    Actively acts only on microorganisms, which are in the stage of reproduction.

    Almost all Gram-negative bacteria are stable, Mycobacterium spp., fungi, viruses, protozoa. Has no cross-resistance with other antibiotics.

    When administered orally, it has no systemic effect, acts locally on the sensitive microflora in the gastrointestinal tract (Staphylococcus aureus, Clostridium difficile).

    Pharmacokinetics:

    Maximum concentration (Cmax) after intravenous infusion of 500 mg - 49 μg / ml after 30 minutes and 20 μg / ml after 1-2 hours; after intravenous infusion of 1 g - 63 mcg / ml after 60 min and 23-30 mcg / ml after 1-2 h. The connection with plasma proteins is 55%.

    Therapeutic concentrations are determined in ascites, synovial, pleural, pericardial and peritoneal fluids, in the urine, atrial auricle tissue. It does not penetrate the intact blood-brain barrier (with meningitis found in the cerebrospinal fluid at therapeutic concentrations).

    Vancomycin penetrates the placenta. Excreted in breast milk.

    The half-life (T1/2) with normal kidney function: adults - about 6 hours (4-11 hours), newborns - 6-10 hours, infants - 4 hours, children of older age - 2-3 hours; T1/2 with chronic renal failure (oliguria or anuria) in adults - 6-10 days: With repeated administration, cumulation is possible. 75-90% of the drug is excreted by the kidneys by passive filtration in the first 24 hours. Patients with one kidney are slowly withdrawn and the removal mechanism is unknown.

    In small and moderate amounts vancomycin can be excreted with bile. In small amounts, it is excreted in hemodialysis or peritoneal dialysis.

    Poorly absorbed when ingested and usually does not enter the systemic circulation.Determined plasma concentrations of vancomycin may be noted in individual cases with repeated use of the inside of patients with acute pseudomembranous colitis caused by FROM. difficile.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to vancomycin:

    - endocarditis;

    - sepsis;

    - meningitis;

    - infections of the lower respiratory tract (pneumonia, lung abscess);

    - infection of bones and joints (including osteomyelitis);

    - infections of the skin and soft tissues.

    In the form of a solution for oral administration:

    - pseudomembranous colitis caused by Clostridium difficile;

    - enterocolitis caused by Staphylococcus aureus.

    Contraindications:

    Hypersensitivity to vancomycin, neuritis of the auditory nerve, pregnancy (I trimester), lactation.

    Carefully:

    Patients with impaired hearing, renal failure due to the possible development of ototoxic and nephrotoxic effects, patients with allergies to teicoplanin (the possibility of cross-allergy), pregnancy (II and III trimester).

    Pregnancy and lactation:

    When pregnant (II-III trimester), the drug is prescribed only if the intended benefit to the mother exceeds the potential risk to the fetus.

    Vancomycin is excreted in breast milk.For the period of taking the drug should stop breastfeeding.

    Dosing and Administration:

    Vancomycin is administered as a slow intravenous infusion at a rate of no more than 10 mg / min for at least 60 minutes. The concentration of the prepared solution of vancomycin should not exceed 5 mg / ml.

    Adults: 0.5 g or 7.5 mg / kg every 6 hours or 1 g or 15 mg / kg every 12 hours.

    Children: Newborn children up to 7 days of life - the initial dose of 15 mg / kg body weight, then - 10 mg / kg every 12 hours; starting from the second week of life - 10 mg / kg every 8 hours; children from 1 month and older - 10 mg / kg every 6 hours.

    Patients with impaired renal excretory function require correction of the dosing regimen taking into account the values ​​of creatinine clearance (CK).

    Correction can be carried out by increasing the intervals between administrations, or by reducing the single dose of the drug:

    Correction by increasing the intervals between the administrations:

    Creatinine clearance (ml / min)

    Vancomycin Dose

    Interval between administrations

    more than 80

    1 g

    12 h

    80-50

    1 g

    1-3 days

    50-10

    1 g

    3-7 days

    less than 10

    1 g

    7-14 days

    Correction of a single dose:

    Creatinine clearance (ml / min)

    Dose of vancomycin (mg / day)

    100

    1545

    90

    1390

    80

    1235

    70

    1080

    60

    925

    50

    770

    40

    620

    30

    465

    20

    310

    10

    155

    This table can not be used to determine the dose of the drug in anuria.Such patients should be given an initial dose of 15 mg / kg body weight to quickly create therapeutic concentrations of the drug in the serum. The dose required to maintain a stable drug concentration is 1.9 mg / kg / day. Patients with severe renal failure should be administered maintenance doses of 250-1000 mg once every few days.

    With anuria, a dose of 1 g is recommended every 7-14 days.

    When only the concentration of serum creatinine is known, the following formula can be used to calculate the creatinine clearance:

    for men: body weight (kg) x (140 - age (years)) / 72 x serum creatinine concentration (mg / dL)

    for women: the result is multiplied by 0.85.

    Preparation of a solution for intravenous administration

    Solution for injection is prepared immediately before the administration of the drug. To do this, 10 ml are added to the bottle with a dry, sterile preparation of 0.5 g dosage, with a dosage of 1 g - 20 ml of sterile water for injection (concentration of the solution is 50 mg / ml).

    REQUIRED FURTHER DILUTION of the prepared solution.

    Prepared solutions of vancomycin before administration are subject to further dilution to a concentration of not more than 5 mg / ml.The required dose, diluted in the above manner, vancomycin, should be administered by intravenous infusion for at least 60 minutes.

    As solvents, a 5% solution of dextrose (glucose) for injection or 0.9% solution of sodium chloride for injection can be used: for 0.5 g - 100 ml and for 1 g - 200 ml.

    Before injection, the prepared parenteral solution should be visually inspected, if possible, for mechanical impurities and discoloration.

    Solutions prepared on the basis of a 5% solution of dextrose (glucose) or 0.9% solution of sodium chloride, can be stored in the refrigerator (2-8 ° C) for 14 days without significant loss of activity.

    Preparation of a solution for ingestion and its use

    For the treatment of pseudomembranous colitis caused by Clostridium difficile, due to the use of antibiotics, as well as for the treatment of staphylococcal enterocolitis, the drug is administered orally.

    The daily dose for adults is 0.5-2 g, divided into 3-4 doses, for children - 40 mg / kg, divided into 3-4 doses. The maximum daily intake for adults and children is 2 g.

    The appropriate dose is dissolved in 30 ml of water and the patient is given a drink or injected through a probe. To improve the taste of the solution, ordinary food syrups can be added to it.The duration of treatment is 7-10 days.

    Side effects:

    Post-fusion reactions (due to rapid administration): anaphylactoid reactions (blood pressure lowering, cardiac arrest, bronchospasm, dyspnoea, skin rash, itching), red man syndrome associated with histamine release (chills, fever, heart palpitations, hyperemia of the upper half of the trunk and face, spasm of the chest muscles and backs).

    From the urinary system: nephrotoxicity (up to the development of renal insufficiency) of the bowl when combined with aminoglycosides or when administered for more than 3 weeks in high concentrations, manifested by an increase in the concentration of creatinine and urea nitrogen; interstitial nephritis.

    From the side gastrointestinal tract: nausea, pseudomembranous colitis.

    From the sense organs: ototoxicity - hearing loss, vertigo, ringing in the ears.

    From the hematopoiesis: reversible neutropenia, transient thrombocytopenia, agranulocytosis.

    Allergic reactions: fever, chills, eosinophilia, rash (including exfoliative dermatitis), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), vasculitis.

    Local reactions (in case of violation of infusion rules): pain and necrosis of tissues at injection sites, phlebitis.

    Overdose:

    Symptoms: increased severity of side effects from the urinary and sensory systems.

    Treatment: Conduct symptomatic therapy. It is recommended to administer the liquid and monitor the plasma concentrations of vancomycin. To quickly remove excess vancomycin from the body, hemofiltration is more effective than hemodialysis.

    Interaction:

    With simultaneous intravenous administration of vancomycin and local anesthetics, erythematous rashes and hyperemia of the skin of the face may appear, in adults - violation of intracardiac conduction.

    With simultaneous and / or sequential systemic or topical application of other potentially ototoxic and / or nephrotoxic drugs (aminoglycosides, amphotericin B, aminosalicylic acid or other salicylates, capreomycin, carmustine, ciclosporin, "loop" diuretics, incl. ethacrynic acid, polymyxin AT, cisplatin) requires careful monitoring of the possible development of these symptoms.

    Kolestyramin reduces the activity of vancomycin when it is ingested.

    Antihistamines, meclozine, phenothiazines, thioxanthenes can mask the symptoms of the ototoxic action of vancomycin (tinnitus, vertigo).

    The solution of vancomycin has a low pH, which can cause physical or chemical instability when mixed with other solutions. Avoid mixing with alkaline solutions.

    Solutions of vancomycin and beta-lactam antibiotics are physically incompatible when mixed. The probability of precipitation increases with increasing concentration of vancomycin. It is necessary to adequately rinse the intravenous system between the applications of these antibiotics. In addition, it is recommended to reduce the concentration of vancomycin to 5 mg / ml or less.

    Special instructions:

    Application in II-III trimester of pregnancy is only possible "for life indications."

    The drug is intended for use only in a hospital.

    When using the drug in infants and preterm infants, the concentration of vancomycin in the blood plasma should be monitored regularly.

    The drug should be infusion slowly (at least 60 minutes). Rapid administration (eg, within a few minutes) of vancomycin may be accompanied by a marked decrease in blood pressure and, in rare cases, cardiac arrest.

    The incidence and severity of thrombophlebitis can be reduced by properly diluting the original solution and alternating the injection site.

    With prolonged use of vancomycin, an audiogram should be performed, the peripheral blood picture should be monitored, the kidney function (general urinalysis, creatinine and urea nitrogen).

    It is desirable to determine the concentrations of vancomycin in the serum in patients with renal insufficiency in patients older than 60 years, since high, persistent concentrations of the drug in the blood can increase the risk of toxic effects of the drug (maximum concentrations should not exceed 40 μg / ml, and minimum -10 μg / ml, concentrations above 80 μg / ml are considered toxic). For patients with renal insufficiency, doses of vancomycin should be selected individually.

    Form release / dosage:

    Lyophilizate for the preparation of a solution for infusions, 0.5 g and 1 g.

    Packaging:

    For 0.5 g of active substance in bottles with a capacity of 10 ml, 1 g of active substance in bottles with a capacity of 20 ml.

    1, 5 or 10 bottles with instructions for use are placed in a pack of cardboard.

    50 bottles are placed in a box of cardboard with 5 instructions for use for delivery to hospitals.

    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 shown on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000602
    Date of registration:11.02.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia
    Information update date: & nbsp03.02.2017
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