Expiration date: 07/2025

Release form and composition:

Lyophilizate for the preparation of solutions for infusion in the form of a powder from white to white with a pink or light brown hue.

Auxiliary substances: mannitol.

Bottles of 10 ml (1) - packs cardboard.

Lyophilizate for the preparation of solutions for infusion in the form of a powder from white to white with a pink or light brown hue.

1 FL.

vancomycin (hydrochloride) 500 mg

Auxiliary substances: mannitol.

Bottles of 20 ml (1) - packs cardboard.

Pharmacological action:

Antibiotic from the group of glycopeptides. Vancomycin is a tricyclic glycopeptide antibiotic isolated from Amycatpsis rientais. The bactericidal action of vancomycin is manifested in the result of inhibition of biosynthesis of cell wall. In addition, vancomycin may alter the permeability of the cell membrane of bacteria and modify RNA synthesis. Cross-resistance between vancomycin and other antibiotics classes.

In all vitr vancomycin is active against gram-positive microorganisms: Staphycccus Staphycccus aureus and epidermidis (including heterogeneous methicillin-resistant strains), Streptcccus pygenes, Streptcccus pneumniae (including penicillin-resistant strains), Streptcccus agaactiae, Streptcccus viridans, Streptcccus bvis and enterococci (including Entercccus faecais) Cstridium difficie (including toxigenic strains involved in the development of pseudomembranous enterocolitis) and diptheroids. To vancomycin in all vitr is also sensitive to other micro-organisms: Listeria mncytgenes, childbirth bacteria Lactbacius, Actinmyces, Cstridium and Bacius.

All vitr In some isolated strains of enterococci and staphylococci are resistant to vancomycin. In a combination of vankomycin and aminoglycosides, there is a synergy of action in vitr against many strains of Staphycccus aureus, streptococci not belonging to group D, enterococci and bacteria of the Streptcccus viridans group.

Vancomycin is not active in all vitr against gram-negative organisms, mycobacteria and fungi.

Pharmacokinetics:

Suction

In persons with normal kidney function with repeated on/in the introduction of vancomycin at a dose of 1 g (15 mg/kg infusion for 60 min) are the average plasma concentrations of approximately 63 mg/l immediately after completion of infusion 2 hours after the infusion the average plasma concentration is approximately 23 mg/l, and after 11 hours to about 8 mg/L. in case of multiple infusions in a dose of 500 mg within 30 min, created average plasma concentrations of about 49 mg/l after completion of infusion 2 hours after the infusion the average plasma concentration be about 19 mg/l, after 6 h, about 10 mg/L. Concentrations in plasma during repeated administration are similar to concentrations in plasma after a single dose.

Distribution

Vd ranges from 0.3 to 0.43 l/kg.

As shown by ultrafiltration, at serum concentrations from 10 mg/l to 100 mg / l, the binding of Vancouver with plasma proteins is 55%.

After the on/in the introduction of vancomycin hydrochloride is found in the pleural, pericardial, ascitic, synovial fluids and tissues of the atrial appendage, as well as in urine and peritoneal fluid at concentrations, inhibiting the growth of microorganisms. Vancomycin slowly penetrates into cerebrospinal fluid. When meningitis marked penetration of the drug into the cerebrospinal fluid. Vancomycin crosses the placental barrier and is excreted in breast milk.

Metabolism

The drug is practically not metabolized.

Breeding

T1/2 of vancomycin from plasma is on average 4-6 hours in patients with normal renal function. About 75% of the administered dose of vancomycin is excreted in the urine by glomerular filtration in the first 24 h the Average plasma clearance is about 0.058 l/kg/h, the average renal clearance is about 0.048 l/kg/h Renal clearance of vancomycin is fairly constant and ensures its excretion by 70-80%.

Pharmacokinetics in special clinical cases

The impairment of renal function slows excretion of vancomycin. In patients with a remote or a missing kidney the average T1/2 is 7.5 days.

The total systemic and renal clearance of vancomycin may be reduced in elderly patients due to a natural slowing of glomerular filtration.

Indications:

Infections caused by vancomycin-sensitive pathogens, including:

• endocarditis caused by Streptcccus viridans or Streptcccus bvis (as monotherapy or in combination with aminoglycosides)
  
• endocarditis caused by enterococci, for example, Entercccus faecais (only in combination with aminoglycosides)
  
• treatment difterence endocarditis (there is evidence of the effectiveness of vancomycin)
  
• early endocarditis, caused Staphycccus epidermidis or diphtheroids, after a prosthetic valve (in combination with rifampicin, an aminoglycoside, or both antibiotics)
  
• prevention of endocarditis (in some cases)
  
• sepsis
  
• infections of bones and joints
  
• infections of the lower respiratory tract
  
• infections of the skin and soft tissues
  
• infection caused by gram-positive organisms, in cases of allergic reactions to penicillin
  
• in case of intolerance or lack of response to treatment with other antibiotics, including penicillins or cephalosporins
  
• infections caused by microorganisms sensitive to vancomycin, but resistant to other antimicrobial drugs
  
• pseudomembranous colitis (as a solution for oral administration).
  

Dosage regimen:

Entered only in / in drip. Vankorus® cannot be administered in/m or in / in bolusno (jet)!

When in / in the administration of the drug solution the recommended concentration of Vancouver is no more than 5 mg/ml and the rate of administration is no more than 10 mg/min.in patients who are shown to limit fluid consumption, the drug can be used in concentrations up to 10 mg/ml, the rate of administration - no more than 10 mg/min. However, in the case of such concentrations, the likelihood of side effects associated with infusion increases.

Adults with normal renal function, the drug is prescribed in a daily dose of 2 g/in (500 mg every 6 h or 1 g every 12 h). Each dose should be administered at a speed of not more than 10 mg/min and for at least 60 minutes of age and the presence of obesity, patients may require changes to the usual dose on the basis of determination of concentration of vancomycin in serum.

For children, the dose is usually 10 mg / kg / every 6 hours. Each dose should be administered for at least 60 minutes.

For newborns, the initial dose is 15 mg/kg, followed by 10 mg / kg every 12 hours during the first week of life. Starting from the second week of life-every 8 hours until the age of 1 month. Each dose should be administered for at least 60 minutes.

Patients with impaired renal function should be individually selected dose. The selection of doses of vancomycin for this group of patients can be carried out under the monitoring of serum creatinine.

In elderly patients the clearance of vancomycin is lower Vd more. In this category of patients, it is advisable to carry out dose selection based on serum concentrations of Vancouver. In premature infants and elderly patients due to deterioration of kidney function may require a significant reduction in dose. Should regularly monitor the concentration of vancomycin in blood plasma. The following table shows the dose of Vancouver depending on CC.

1 FL.

Vancomycin (in the form of hydrochloride) 1 g

In anuria, this table can not be used to determine the dose. In anuria, the drug should be prescribed at an initial dose of 15 mg/kg body weight for the rapid creation of therapeutic concentrations of Vancouver serum. The dose required to maintain a stable concentration of the drug is 1.9 mg/kg/day. Patients with severe renal insufficiency, it is advisable to introduce maintenance doses of 250-1000 mg 1 every few days: with CC 10-50 ml/min - 1 g every 3-7 days, with CC t 10 ml/min - 1 g every 7-14 days. When anuria is the recommended dose of 1 g every 7-10 days.

Rules for the preparation of solution for on / in the introduction

The solution for injection is prepared immediately before administration of the drug. For this into the vial of dry, sterile lyophilisate of vancomycin add the required volume of water for injection to obtain a solution with a concentration of 50 mg/ml, further dilution of the prepared solution.

The prepared solutions of vancomycin before the introduction of the subject to further dilution to a concentration of not more than 5 mg/ml the Required dose, diluted as above vancomycin should be administered by the fractional on/in infusions for at least 60 min. as solvent use 5% solution of dextrose (glucose) for injection or 0.9% sodium chloride solution for injection. Before injecting the prepared solution for parenteral administration should be inspected visually, if possible, the presence of mechanical impurities and color change.

Preparation of solution for oral administration and its application

For the treatment of pseudomembranous colitis caused by Sstridium difficulty, due to the use of antibiotics, as well as for the treatment of staphylococcal enterocolitis Vankorus® prescribed inside. Adults are prescribed 0.5-2 g 3-4 times/day, children – in a daily dose of 40 mg/kg, the multiplicity of 3-4 times / day. 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 it is possible to add conventional food syrups. The duration of treatment is 7-10 days.

In/in the introduction of vancomycin has no advantages for the treatment of these diseases.

Vancomycin is ineffective when administered in the case of other types of infections.

Side effect:

From the cardiovascular system: cardiac arrest, hot flashes, decrease in blood PRESSURE, shock (these symptoms are mainly associated with rapid infusion of the drug).

From the digestive system: nausea, pseudomembranous colitis.

From the hematopoietic system: agranulocytosis, eosinophilia, neutropenia, thrombocytopenia.

From the urinary system: interstitial nephritis, changes in functional renal tests, impaired renal function.

From the senses: vertigo, tinnitus, ototoxic effects. A number of patients who received vancomycin was observed ototoxic effects. It may be transient or permanent. It is reported that most of these cases were observed in patients who received excessive doses of vankomycin, with a history of hearing loss or in patients receiving simultaneous treatment with other drugs with the possible development of ototoxicity, for example, aminoglycosides.

Dermatological reactions: exfoliative dermatitis, benign (IgA) vesicular dermatosis, itchy dermatosis, rash.

Allergic reactions: Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, vasculitis. Anaphylactoid reactions are possible during or shortly after a very rapid infusion of Vancouver.

Other: chills, drug fever, tissue necrosis at injection sites, pain at injection sites, thrombophlebitis.

Rapid administration of the drug can also cause red man syndrome, redness of the upper body or pain and spasm of the chest and back muscles. After the termination of infusion, these reactions usually take place within 20 minutes, but sometimes can last up to several hours.

Contraindications:

• neuritis of the auditory nerve
  
• renal failure
  
• I trimester of pregnancy
  
• lactation (breastfeeding) period)
  
• hypersensitivity to vancomycin.
  

With caution the drug should be used during the hearing (including in history), in II and III trimestrah pregnancy.

Pregnancy and lactation:

The drug is contraindicated for use in the first trimester of pregnancy. Application in the II and III trimesters of pregnancy is possible only for life indications in the case when the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

If necessary, the use of the drug during lactation should stop breastfeeding for the duration of treatment with the drug.

Special instruction:

With caution should use vancomycin in patients with renal insufficiency (it is recommended to monitor the concentration of vancomycin in blood plasma of renal insufficiency in patients older than 60 years), because the high long-lasting concentrations of a drug in the blood may increase the risk of manifestations of toxic action of the drug the maximum concentration should not exceed 40 mcg/ml, minimum 10 µg/ml, concentrations above 80 µg/ml are considered toxic. For patients with renal insufficiency dose of Vancouver should be set individually.

A quick introduction (for example, within several minutes) of vancomycin may be accompanied by a pronounced decrease in blood pressure and in rare cases - cardiac arrest. Vancomycin should be administered in a diluted solution for at least 60 min to avoid side reactions associated with the infusion.

Vancomycin should be administered with caution to patients with Allergy-teicoplanin, because there have been cases of cross-Allergy.

In patients, receiving V/V Vancouver, it is necessary to periodically conduct a blood test and control kidney function.

Vancomycin is an irritant substance, so the diffusion of dissolved drug through the vascular wall may cause necrosis of adjacent tissues. Thrombophlebitis can be observed, although the probability of their development can be reduced by the slow introduction of dilute solutions (with a concentration of 2.5-5 mg/ml) and alternating places of administration.

Use in Pediatrics

In the appointment of the newborn is recommended to control the concentration in the blood plasma.

Overdose:

Symptoms: increased severity of side effects.

Treatment: corrective therapy, aimed at maintaining the clubockova filtering. Vancomycin is poorly removed by dialysis. There is evidence that hemofiltration and hemoperfusion through polysulfonic ion exchange resin leads to an increase in the clearance of Vancouver.

Drug interaction:

Simultaneous in/in the introduction of vancomycin and local anesthetics was observed erythema, redness of the skin and anaphylactoid reactions, possible risk reducing actions or the development of neuromuscular blockade. The introduction of Vancomycin in the form of 60-minute infusion before the introduction of anesthetic can reduce the likelihood arise these reactions.

With simultaneous and/or sequential systemic or local use of other potentially ototoxic and/or nephrotoxic drugs (aminoglycosides, amphotericin b, aminosalicylic acid or other salicylates, bacitracin, capreomycin, carmustine, paromomycin, cyclosporine, loop diuretics, polymyxin, cisplatin, ethacrynic acid) requires careful monitoring of possible development of these symptoms.

Cholestyramine reduces the activity of vancomycin (the ingestion).

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

Pharmaceutical interaction

Vancomycin solution has a low pH that may cause chemical or physical instability when mixed with other solutions. Mixing with alkaline solutions should be avoided.

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

Storage conditions and terms:

List B. the Drug should be stored out of reach of children, dry, protected from light place at temperature not exceeding 25°C. shelf Life - 2 years.