Vancorus lyophilisate for solution for infusion 1g vial 1pc

Composition

1 bottle of lyophilizate for preparation of infusion solution contains:

Active ingredient:

vancomycin (in the form of hydrochloride) 1 g

Pharmacological action

Pharmacodynamics

Vancomycin is a tricyclic glycopeptide antibiotic, produced by Amycolatopsisorientalis, acts bactericidal on most microorganisms (on Enterococcus spp. – bacteriostatically). Blocks bacterial cell wall synthesis in a region other than that affected by penicillins and cephalosporins (does not compete with them for binding sites), strongly binding to the D-alanyl-D-alanine part of the cell wall precursor, which leads to cell lysis.

Active against gram-positive microorganisms, including: Staphylococcus aureus and staphylococcus epidermidis(including heterogeneous methicillin-resistant strains), Streptococcusspp., Enterococcusspp. (wh. Enterococcus faecalis), Clostridium spp. (wh. Clostridium difficile). Listeria monocytogenes, genera of bacteria Lactobacillus spp., Actinomyces spp., and Bacillus spp. are sensitive to vancomycin in vitro.

The optimum action is at pH 8, with a decrease in pH to 6, the effect decreases sharply.

It is active only on microorganisms that are in the breeding stage.

Almost all gram-negative bacteria, Mycobacterium spp., fungi, viruses, and protozoa are resistant. It has no cross-resistance with other antibiotics.

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

Pharmacokinetics

The maximum concentration (Cmax) after an intravenous infusion of 500 mg is 49 mcg / ml after 30 minutes and 20 mcg / ml after 1-2 hours; after an intravenous infusion of 1 g-63 mcg/ml after 60 minutes and 23-30 mcg/ml after 1-2 hours. Plasma protein binding is 55%.

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

Vancomycin passes through the placenta. It is excreted in breast milk.

Half-life (T 1/2) for normal renal function: adults-about 6 hours (4-11 hours), newborns – 6-10 hours, children – 4 hours, older children – 2-3 hours; T 1/2 for chronic renal failure (oliguria or anuria) in adults – 6-10 days. With repeated use, cumulation is possible. 75-90% of the drug is excreted by the kidneys by passive filtration in the first 24 hours. In patients with only one kidney, it is excreted slowly and the mechanism of elimination is unknown.

In small and moderate amounts, vancomycin can be excreted in the bile. It is excreted in small amounts during hemodialysis or peritoneal dialysis. It is poorly absorbed when taken orally and usually does not enter the systemic circulation. Detectable plasma concentrations of vancomycin may be observed in some cases with repeated oral use in patients with acute pseudomembranous colitis caused by C. difficile.

Indications

Infectious and inflammatory diseases caused by vancomycin-sensitive microorganisms:

• endocarditis;
• sepsis;
• meningitis;
• lower respiratory tract infections (pneumonia, lung abscess);
• bone and joint infections (including osteomyelitis);
• skin and soft tissue infections;

As an oral solution: pseudomembranous colitis caused by Clostridium difficile; enterocolitis caused by Staphylococcus aureus.

Use during pregnancy and lactation

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

Vancomycin is excreted in breast milk. During the period of taking the drug, you should stop breastfeeding.

Contraindications

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

Side effects

Post-infusion reactions (due to rapid use): anaphylactoid reactions (decreased blood pressure, cardiac arrest, bronchospasm, dyspnoea, skin rash, pruritus); red man syndrome associated with histamine release (chills, fever, rapid heartbeat, hyperemia of the upper half of the trunk and face, spasm of the muscles of the chest and back).

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

From the digestive system: nausea, pseudomembranous colitis.

From the sensory organs: ototoxicity – hearing loss, vertigo, tinnitus.

Hematopoietic disorders: 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 the rules of infusion): pain and tissue necrosis at injection sites, phlebitis.

Interaction

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

When other potentially ototoxic and/or nephrotoxic drugs (aminoglycosides, amphotericin B, aminosalicylic acid or other salicylates, capreomycin, carmustine, cyclosporine, loop diuretics, including ethacric acid, polymyxin B, cisplatin) are used simultaneously and/or sequentially systemically or topically, careful monitoring of the possible development of these symptoms is required. Colestyramine reduces the activity of vancomycin when taken orally.

Antihistamines, meclozin, phenothiazines, and thioxanthenes can mask symptoms of the ototoxic effect of vancomycin (tinnitus, vertigo).

Pharmaceutical interaction

The vancomycin solution has a low pH, which can cause physical or chemical 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 concentration of vancomycin. It is necessary to flush the intravenous system adequately between applications of these antibiotics. In addition, it is recommended to reduce the concentration of vancomycin to 5 mg / ml or less.

How to take, course of use and dosage

Vancomycin is administered as a slow intravenous infusion at a rate of no more than 10 mg / minute for at least 60 minutes. The concentration of the prepared vancomycin solution 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.

For children:  newborn children under 7 days of life-an initial dose of 15 mg / kg of 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 excretory function of the kidneys need to adjust the dosage regimen taking into account the values of creatinine clearance (CC). Correction can be carried out by increasing the intervals between injections, or by reducing the single dose of the drug. :

Correction by increasing the intervals between injections:

Single dose adjustment:

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

For anuria, a dose of 1 g every 7-14 days is recommended. When only the serum creatinine concentration is known, the formula below can be used to calculate creatinine clearance:for men:  body weight (kg) x (140 – age (years)),72 x serum creatinine concentration (mg/dl)for women: the result obtained is multiplied by 0.85. Preparation of the solution for intravenous use The solution for injection is prepared immediately before use of the drug. To do this,10 ml is added to the vial with a dry, sterile preparation with a dosage of 0.5 g, and 20 ml of sterile water for injection with a dosage of 1 g (the solution concentration is 50 mg / ml).

FURTHER DILUTION of the prepared solution is REQUIRED. The prepared solutions of vancomycin before use should be further diluted to a concentration of no more than 5 mg / ml. The required dose of vancomycin diluted in the above manner should be administered by intravenous infusion for at least 60 minutes. As solvents, you can use 5% dextrose (glucose) solution for injection or 0.9% sodium chloride solution for injection: for 0.5 g-100 ml and for 1 g-200 ml.

Before injection, the prepared solution for parenteral use should be visually checked, if possible, for the presence of mechanical impurities and discoloration. Solutions prepared on the basis of 5% dextrose (glucose) solution or 0.9% sodium chloride solution can be stored in the refrigerator (2-8 about C) for 14 days without significant loss of activity.

Preparation of the oral solution and its applicationfor 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 prescribed 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 dose for adults and children is 2 g. The corresponding dose is dissolved in 30 ml of water and given to the patient to drink it or administered through a probe. To improve the taste of the solution, you can add ordinary food syrups to it. The duration of treatment is 7-10 days.

Overdose

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

Treatment: perform symptomatic therapy. Fluid use and monitoring of vancomycin plasma concentrations are recommended. To quickly remove excess vancomycin from the body, hemofiltration is more effective than hemodialysis.

Special instructions

The drug is intended for use only in a hospital setting.

When using the drug in children and premature newborns, the concentration of vancomycin in blood plasma should be regularly monitored.

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

The frequency and severity of thrombophlebitis can be reduced by properly diluting the initial solution and alternating the sites of use of the drug.

With prolonged use of vancomycin, it is necessary to conduct an audiogram, monitor the picture of peripheral blood, kidney function (general urinalysis, indicators of creatinine and blood urea nitrogen).

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

Form of production

Lyophilizate for infusion solution preparation

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Vancomycin

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

From pneumonia, From osteomyelitis, From infectious diseases