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

    1 bottle contains:

    active substance: vancomycin hydrochloride (in terms of anhydrous substance) 500 mg or 1000 mg.

    Description:

    Lyophilized mass from white to white with a yellowish or pinkish hue.

    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, acts bactericidal against most microorganisms (on enterococci - bacteriostatic). 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 also able to change the permeability of bacterial cell membranes and selectively inhibit the synthesis of RNA.

    It is active against Gram-positive microorganisms, including: Staphylococcus aureus and Staphylococcus epidermidis (including heterogeneous methicillin-resistant strains), Streptococcus spp., Enterococcus spp. (incl. Enterococcus faecalis), Clostridium spp. (incl. Clostridium difficile). To vancomycin in vitro sensitive Listeria monocytogenes, genera of bacteria Lactobacillus, Actinomyces, Bacillus.

    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 applied orally does not have a systemic effect, acts locally on the sensitive microflora in the gastrointestinal tract (Staphylococcus aureus, Clostridium difficile).

    Pharmacokinetics:

    The 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 passive filtration in the first 24 hours; in patients with a deleted or missing kidney is slowly withdrawn and the removal mechanism is unknown. In small and moderate amounts 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 Cl. difficile.

    Indications:

    Infectious-inflammatory diseases caused by sensitive microorganisms:

    - sepsis;

    - endocarditis;

    - meningitis;

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

    - infection of bones and joints (including osteomyelitis);

    - infections of the skin and soft tissues.

    For oral administration:

    - pseudomembranous colitis caused by Clostridium difficile;

    - Enterocolitis caused by Staphylococcus aureus.
    Contraindications:

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

    Carefully:

    Hearing impairment (including in history), renal failure, pregnancy (II and III trimesters).

    Dosing and Administration:

    Intravenously.

    The recommended concentration is no more than 5 mg / ml with a rate of administration of not more than 10 mg / min; the duration of the infusion should be at least 60 minutes.

    Adults: 500 mg or 7.5 mg / kg every 6 hours or 1000 mg or 15 mg / kg every 12 hours.

    For children: Newborn children during the first week of life - an initial dose of 15 mg / kg, followed by 10 mg / kg every 12 hours; beginning with the second week of life, apply the same dose every 8 hours; for children older than 1 month - 10 mg / kg every 6 hours or 20 mg / kg every 12 hours.

    Patients with impaired renal excretory function correction of the dosing regimen is required taking into account the values ​​of creatinine clearance (CK). Correction can be carried out by increasing the intervals between injections of Vero-Vancomycin, or by reducing the single dose of the drug.

    Correction by increasing the intervals between the administrations:

    At CC more than 80 ml / min - the usual dosing regimen, with KK 50-80 ml / min - 1000 mg every 1-3 days, with KK 10-50 ml / min - 1000 mg every 3-7 days, with QC less than 10 ml / min - 1000 mg every 7-14 days.

    Correction of a single dose:

    Creatinine clearance

    (ml / min)

    Vancomycin Dose

    (mg / 24 hours)

    100

    1545

    90

    1390

    80

    1235

    70

    1080

    60

    925

    50

    770

    40

    620

    30

    465

    20

    310

    10

    155

    Patients with anuria Vero-vancomycin should be given at an initial dose of 15 mg / kg to quickly create a therapeutic concentration of the drug in the blood serum. The dose required to maintain a stable concentration is 1.9 mg / kg per day. Patients with severe renal dysfunction should be given maintenance doses of 250-1000 mg once every few days than on a daily schedule. When anuria is recommended to administer 1000 mg 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 the solution: The lyophilizate is dissolved in water for injection: 500 mg in 10 ml, 1 g in 20 ml (the concentration of the solution is 50 mg / ml). The resulting solution is subject to further dilution with 0.9% sodium chloride solution or 5% dextrose solution to a concentration of not more than 5 mg / ml (for 500 mg - 100 ml and for 1 g - 200 ml). Solutions prepared on the basis of 0.9% sodium chloride or 5% dextrose can be stored in a refrigerator (2-8 ° C) for 14 days without significant loss of activity.

    Application inside with pseudomembranous colitis, staphylococcal enterocolitis: daily dose for of adults - 500-2000 mg, divided into 3-4 doses; for children - 40 mg / kg, divided into 3-4 admission. The maximum daily dose for adults and children is 2000 mg. Duration of treatment is 7-10 days.

    The solution for oral ingestion is prepared by dissolving the appropriate dose of lyophilizate in 30 ml of water.

    Side effects:

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

    From the urinary system: nephrotoxicity (up to the development of renal insufficiency), more often 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.

    On the part of the organs of the gastrointestinal tract: nausea, pseudomembranous colitis.

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

    On the part of the organs of hematopoiesis: reversible neutropenia, transient thrombocytopenia, agranulocytosis.

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

    Local reactions: phlebitis, pain and necrosis of tissues at injection sites.

    Overdose:

    Symptoms: increased severity of side effects.

    Treatment: symptomatic, in combination with hemoperfusion and hemofiltration.
    Interaction:

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

    Simultaneous administration with nephro- and ototoxic drugs (aminoglycosides, amphotericin B, acetylsalicylic acid or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, ciclosporin, loop diuretics, polymyxin AT, cisplatin, ethacrynic acid) requires careful monitoring of the possible development of these symptoms.

    Kolestyramin reduces activity (for oral administration).

    General anesthetics and vecuronium bromide - risk of lowering blood pressure or developing a neuromuscular blockade. Infusion of vancomycin is possible at least 60 minutes before their administration.

    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.

    Special instructions:

    Application in II-III trimester of pregnancy is possible only according to "vital" indications. When prescribing preterm and newborns, control over the concentration of the drug in the blood serum is desirable.

    With simultaneous administration with general anesthetics, the incidence of side effects increases, so vancomycin should be administered before general anesthesia.

    It is desirable to determine the concentration of vancomycin in the blood serum (with renal failure, in patients older than 60 years). The maximum concentrations should not exceed 40 μg / ml, and the minimum concentration should not exceed 10 μg / ml; concentrations above 80 μg / ml are considered toxic. For patients with renal insufficiency, doses of vancomycin should be selected individually.

    The likelihood of developing local reactions can be reduced by slowly introducing dilute solutions (2.5-5 g / L) and alternating injection sites.

    Form release / dosage:Lyophilizate for the preparation of a solution for infusions, 500 mg and 1000 mg.
    Packaging:

    For 500 mg and 1000 mg in vials.

    1 bottle with instructions for use in a pack of cardboard.
    For 10 or 25 bottles with an equal number of instructions for use in a cardboard box (for hospitals).
    Storage conditions:

    At a temperature not exceeding 25 FROM. Prepared solution of the drug stored in the refrigerator at a temperature of 2-8 FROM not more than 14 days.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N001886 / 01
    Date of registration:31.03.2008 / 12.08.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp30.01.2017
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