VANKORUS

Active material: Vancomycin
When ATH: J01XA01
CCF: Antibiotic group glycopeptides
ICD-10 codes (testimony): A 04.7, A40, A41, i33, J15, J20, J42, J85, J86, J90, L01, L02, L03, L08.0, M00, M86
At KFU: 06.11
Manufacturer: Synthesis of (Russia)

Pharmaceutical form, composition and packaging

Valium for solution for infusion powder from white to white with pink or light brown tint.

Excipients: mannyt.

Vials 10 ml (1) – packs cardboard.

Valium for solution for infusion powder from white to white with pink or light brown tint.

Excipients: mannyt.

Vials 20 ml (1) – packs cardboard.

Pharmacological action

Antibiotics from the Group glikopeptidov. Vancomycin is a tricyclic glikopeptidnym antibiotic, derived from Amycolatopsis orientalis. Vancomycin bactericidal activity manifests itself as a result of inhibition of the biosynthesis of cell wall. Besides, Vancomycin may alter the permeability of cell membrane of bacteria and modify RNA synthesis. Cross resistance between vankomitinom and other classes of antibiotics is missing.

In vitro vancomycin active against grampolaugitionah microorganisms: Staphylococcus aureus and Staphylococcus epidermidis (including their heterogeneous Methicillin-resistant strains), Streptococcus pyogenes, Streptococcus pneumoniae (including penicillin-resistant strains), Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis and enterococci (incl. Enterococcus faecalis); Clostridium difficile (incl. toksigennye strains, participating in the development of psevdomembranoznogo enterocolitis) and difteroidov. To Vancomycin in vitro also other sensitive organisms: Listeria monocytogenes, Genera of bacteria Lactobacillus, Actinomyces, Clostridium and Bacillus.

In vitro some isolated strains of enterococci and staphylococci are resistant to Vancomycin. With a combination of Vancomycin and aminoglycosides synergies action is observed in vitro against many strains of Staphylococcus aureus, streptococci, not belonging to Group D, enterococci bacteria Streptococcus viridans group.

Vancomycin is not active in vitro against gramotricationah microorganisms, Mycobacteria and fungi.

Pharmacokinetics

Absorption

In patients with normal renal function with repeated on/in the introduction of Vancomycin dose 1 g (15 mg / kg, infusion over 60 m) creates average plasma concentrations of approximately 63 mg/l immediately after the infusion; through 2 h after infusion concentration in plasma is about 23 mg / l, and through 11 no – about 8 mg / l. When multiple infuziah in dose 500 mg for 30 m, creates average plasma concentrations of approximately 49 mg/l after completion of infusion; through 2 hours after infusion of mean concentrations in the plasma make up about 19 mg / l, through 6 no – about 10 mg / l. Plasma concentrations after repeated introduction of similar concentrations in the plasma of the one-time introduction.

Distribution

V_d ranging from 0.3 to 0.43 l / kg.

As demonstrated by ultrafiltration, When serum concentrations of 10 mg/l to 100 mg / l, linking plasma protein is Vancomycin 55%.

After the on/in the introduction of Vancomycin hydrochloride is detected in the blood, pericardial, ascitic, synovial fluids and tissue abalone Atrium, as well as in urine and peritoneal fluid at concentrations, inhibiting the growth of microorganisms. Vancomycin slowly penetrates cerebrospinal fluid. When meningitis drug penetration is observed in cerebrospinal fluid. Vancomycin penetrates through the placental barrier and is excreted in breast milk.

Metabolism

The drug is metabolized almost no.

Deduction

T_1/2 vankomitina from plasma in the average 4-6 hours in patients with normal renal function. About 75% Vancomycin administered dose appears in the urine due to clubockova filtering in the first 24 no. The average plasma clearance is about 0.058 L / kg / h, the average kidney klirens – about 0.048 L / kg / h. Kidney klirens vankomitina is fairly constant and ensures its launching 70-80%.

Pharmacokinetics in special clinical situations

Violation of kidney function slows the excretion of Vancomycin. In patients with a remote or a missing kidney average T_1/2 is 7.5 d.

The overall system and kidney klirens Vancomycin may be reduced in elderly patients as a result of a natural slowdown clubockova filtering.

Testimony

Infection, caused by susceptible pathogens to vancomycin, including:

— endocarditis, caused by Streptococcus viridans or Streptococcus bovis (as monotherapy or in combination with aminoglikozidami);

— endocarditis, caused by jenterokokkami, eg, Enterococcus faecalis (only in combination with aminoglikozidami);

— treatment difteroidnogo endocarditis (There is evidence of the effectiveness of Vancomycin);

— early endocarditis, caused by Staphylococcus epidermidis or difteroidami, After prosthetic valve (in combination with rifampicin, aminoglycoside antibiotics or both);

-Prevention of endocarditis (in some cases);

- Sepsis;

- Bone and joint infections;

- Infections of the lower respiratory tract;

- Infections of the skin and soft tissues;

- Infections, caused by grampolaugitionami microorganisms, in cases of allergic reactions to penicillin;

— with intolerance or lack of response to treatment with other antibiotics, including the Penicillins or cephalosporins;

- Infections, caused by microorganisms, sensitive to Vancomycin, but resistant to other antimicrobial drugs;

- Psevdomembranoznыy colitis (as a solution for the reception inside).

Dosage regimen

Only in/in the drip. Vankorus^® You cannot enter in/m or/in bolusno (spray)!

The on/in a solution of the drug recommended concentration of Vancomycin is not more 5 mg/ml and speed of not more than 10 mg / min. Patients, which restricts fluid intake, the drug can be used in concentrations up to 10 mg / ml, introduction rate – no more 10 mg / min. However, in the case of such concentrations increases the likelihood of side effects, Infusion-related.

Adults with normal renal function drug appoint daily dose 2 g / in (by 500 mg every 6 or h 1 g every 12 no). Each dose should be entered with a speed of no more than 10 mg/min and at least 60 m. Age and the presence of obesity in patient may require changes in normal doses based on determination of concentration of Vancomycin in serum.

To children dose, usually, is 10 mg/kg/every 6 no. Each dose should be at least 60 m.

To Newborn starting dose is 15 mg / kg, and then 10 mg / kg every 12 no during the first week of life. Starting from the second week of life – every 8 h to achieve age 1 Months. Each dose should be at least 60 m.

Patients with impaired renal function You must individually select dose. Selection of doses of Vancomycin for this group of patients can be performed under the supervision of the content of serum creatinine.

In elderly patients Vancomycin is the ground below, V_d better. This category of patients, selection of doses should be based on concentrations of Vancomycin in serum. In premature babies and elderly patients the deterioration of kidney function may require considerable dose reduction. Should regularly monitor the concentration of Vancomycin in plasma. The following table shows the dose Vancomycin given depending on QC .

At anurii This table cannot be used to determine dosage. When anurii drug should be appointed in the initial dose of 15 mg/kg body weight for fast creation of therapeutic concentrations of Vancomycin in serum. Dose, required to maintain stable concentrations of the drug, is 1.9 mg / kg / day. Patients with severe renal insufficiency It is advisable to enter maintenance doses 250-1000 mg 1 every few days: at CC 10-50 ml / min – 1 g every 3-7 days, at CC < 10 ml / min – 1 g every 7-14 days. At anurii recommended dose 1 g every 7-10 days.

Rules for solution for the on/in the introduction

Injection solution is prepared immediately before administration. To do this in a bottle with dry, sterile lyophilisate vancomycin add the necessary amount of water for injection, to get a solution with concentration 50 mg / ml. Further breeding prepared solution.

Cooked solutions of Vancomycin before entering are subject to further breeding to concentration of not more than 5 mg / ml. The required dose diluted as above vankomitina should be by fractional/in infusions for at least 60 m. As solvents can be used 5% Dextrose (Glucose) for injection or 0.9% sodium chloride solution for injection. Prior to injection, the prepared solution for parenteral administration must be checked visually, if possible, the presence of mechanical impurities and discoloration.

Preparation of solution for oral administration and its application

To the treatment of pseudomembranous colitis, caused Slostridium difficile, due to the use of antibiotics, as well as for the treatment of Staphylococcal enterocolitis Vankorus^® appointed interior. Adults appoint 0.5-2 g 3-4 times / day, children -daily dose 40 mg / kg, the multiplicity of reception 3-4 times / day. The appropriate dose dissolved in 30 ml of water and give it to the patient to drink or inject through the probe. To improve the flavor solution may be added thereto usual edible syrups. Duration of treatment – 7-10 days.

B / in the introduction of vancomycin has no advantage in the treatment of these diseases.

Vancomycin is not effective when administered in the case of other types of infections.

Side effect

Cardio-vascular system: cardiac arrest, tides, decrease in blood pressure, shock (These symptoms generally associated with rapid infusion of the drug).

From the digestive system: nausea, psevdomembranoznыy colitis.

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

From the urinary system: interstitial nephritis, renal function tests change, impairment of renal function.

On the part ofrganov senses: vertigo, tinnitus, ototoxic effects. A number of patients, treated with Vancomycin, ototoxic effect was observed. It can be transient or be permanent. Reported, that the majority of these cases were observed among patients, which received excess dose of vancomycin, with a history of hearing loss, or in patients, receiving concomitant treatment with other drugs with possible development of ototoxicity, eg, aminoglikozidami.

Dermatological reactions: exfoliative dermatitis, good (IgA) vesicular dermatosis, itching dermatosis, rash.

Allergic reactions: Stevens-Johnson syndrome, toxic epidermal necrolysis, hives, vasculitis. During or shortly after too rapid infusion vancomycin possible anaphylactoid reaction.

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

Rapid introduction of the drug may also cause syndrome “red man”, redness of the upper body or the pain and spasm of the muscles of the chest and back. After stopping the infusion of these reactions are usually tested for 20 m, but sometimes can last up to several hours.

Contraindications

-Neuritis of the auditory nerve;

- Renal failure;

- I trimester of pregnancy;

- Lactation (breast-feeding);

- hypersensitivity to vancomycin.

FROM caution use in patients with hearing impairment (incl. history), in the II and III trimesters of pregnancy.

Pregnancy and lactation

The drug is contraindicated for use in the I trimester of pregnancy. Application in II and III trimester of pregnancy is possible only for health reasons in the case of, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

If necessary, the use of the drug during lactation should stop breast-feeding at the time of treatment.

Cautions

Caution should be used vancomycin in patients with renal insufficiency (vancomycin is recommended to monitor plasma concentrations in patients with renal insufficiency in patients over 60 years), because at high, stored for a long time, the drug concentrations in the blood may increase the risk of toxic manifestations of the drug; the maximum concentration should not exceed 40 ug / ml, minimal – 10 ug / ml, concentration above 80 ug / ml are considered toxic. For patients with renal insufficiency, the dose of vancomycin should be installed individually.

rapid introduction (eg, for several minutes) 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 m, in order to avoid adverse reactions, Infusion-related.

Vancomycin should be used with caution in patients allergic to teicoplanin, tk. cases of cross-allergies have been reported.

Patients, receiving vancomycin in /, It is necessary to periodically conduct blood tests and monitoring of renal function.

Vancomycin is an irritant, therefore, the diffusion of the dissolved drug through the vessel wall can cause necrosis of surrounding tissue. Thrombophlebitis may occur, although the probability of their development can be reduced by slowly introducing dilute solutions (with concentration 2.5-5 mg / ml) and the alternation of the injection site.

Use in Pediatrics

When newborn assignment control plasma concentration is recommended.

Overdose

Symptoms: increased severity of side effects.

Treatment: corrective therapy, It aims to maintain glomerular filtration. Vancomycin is poorly removed during dialysis. There is evidence, that hemoperfusion hemofiltration, and polysulfone through an ion exchange resin leads to an increase in clearance of vancomycin.

Drug Interactions

At the same time / in the introduction of vancomycin and local anesthetics marked erythema, skin redness and anaphylactoid reaction, possible risk of reduction in blood pressure or development of neuromuscular blockade. Introduction of vancomycin as a 60-minute infusion before administration of the anesthetic can reduce the likelihood of these reactions.

With simultaneous and / or sequential systemic or local application of other potentially ototoxic and / or nephrotoxic agents (aminoglikozidy, Amphotericin B, aminosalicylic acid or other salicylates, bacitracin, capreomycin, karmustin, paromomycin, cyclosporine, “loop” Diuretic, polymyxin b, cisplatin, ethacrynic acid) It requires a careful monitoring of the possible development of these symptoms.

Cholestyramine reduces the activity of vancomycin (ingestion).

antihistamines, meklozin, fenotiazinы, thioxanthenes may mask the symptoms of vancomycin Valium actions (noise in ears, vertigo).

Pharmaceutical interaction

Vancomycin solution has a low pH, which may cause physical or chemical instability when mixed with other solutions. Should not be mixed with alkaline solutions.

Solutions of vancomycin and beta-lactam antibiotics are physically incompatible when mixed. The probability of precipitation increases with the concentration of vancomycin. Need to be adequately rinsed in / in between the application of these antibiotics. Besides, it is recommended to reduce the concentration of vancomycin solution to 5 mg / ml or less.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 2 year.