Vancomycin Elfa solution powder for infusion 1000mg 20ml vials 1pc

Composition

1 bottle contains:

Active ingredient:

Vancomycin hydrochloride in terms of vancomycin 1000.0 mg

Pharmacological action

Pharmacotherapeutic group: Antibiotic-glycopeptid ATX:  

J. 01. X. A. 01 Vancomycin

J. 01. X. A Glycopeptide structure antibiotics

Pharmacodynamics :

An antibiotic of the tricyclic glycopeptide group, isolated from Amycolatopsis orientalis, is effective against many gram-positive microorganisms.

The bactericidal effect of vancomycin is manifested as a result of inhibition of cell wall biosynthesis. In addition, vancomycin can alter bacterial cell membrane permeability and RNA synthesis. There is no cross-resistance between vancomycin and other classes of antibiotics.

In vitro, vancomycin is active against gram-positive microorganisms, including Staphylococcus aureus, Staphylococcus epidermidis (including heterogeneous methicillin-resistant strains), Streptococcus pyogenes, Streptococcus pneumoniae (including penicillin-resistant strains), Streptococcus agalactiae, Streptococcus bovis, Streptococcus spp. of the viridians group, Clostridium difficile (including toxigenic strains involved in the development of pseudomembranous colitis) and Corynebacterium spp. It acts bacteriostatically on Enterococcus spp. (including Enterococcus faecalis). Optimum action – 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.

Other microorganisms that are sensitive to vancomycin in vitro include Listeria monocytogenes, Lactobacillus spp., Actinomyces spp., Clostridium spp., Bacillus spp.

In in vitro, some isolated strains of enterococci and staphylococci show resistance to vancomycin.

The combination of vancomycin and aminoglycosides shows synergism in vitro against many strains Staphylococcus aureus, Streptococcus spp. (not belonging to enterogroup D), Enterococcus spp., Streptococcus spp. of the viridians group.

Vancomycin is inactive in vitro against gram-negative microorganisms, mycobacteria, viruses, protozoa and fungi.

Pharmacokinetics:

Suction

Repeated intravenous use of 1 g of vancomycin (15 mg / kg; infused for 60 minutes) produces average plasma concentrations of about 63 mg/L immediately after completion of infusions. 2 hours after the infusion, the average plasma concentrations were about 23 mg/l, and 11 hours after the infusion, about 8 mg/l.

Multiple infusions of 500 mg (30 min infusion) produced average plasma concentrations of about 49 mg/l after completion of the infusions. 2 hours after the infusion, the average plasma concentrations were about 19 mg/l, and 6 hours after the infusion, about 10 mg/l. The plasma concentrations of vancomycin administered multiple times are similar to those of a single dose.

Distribution

The volume of distribution varies from 0.3 to 0.43 l / kg. Ultrafiltration has shown that when the serum concentration of vancomycin is between 10 mg / l and 100 mg / L,55% of vancomycin is found in the protein-bound state.

After intravenous use, vancomycin is detected in pleural, pericardial, ascitic, synovial fluids and atrial auricle tissue, as well as in urine and peritoneal fluid at concentrations that inhibit the growth of microorganisms. In meningitis, penetration of the drug into the cerebrospinal fluid in therapeutic concentrations is noted. Vancomycin penetrates the placental barrier and is excreted in breast milk.

Metabolism and elimination

Vancomycin is practically not metabolized. The mean plasma half-life (T 1/2) of vancomycin in patients with normal renal function is 4-6 hours. Approximately 75% of the vancomycin dose is excreted by the kidneys through glomerular filtration in the first 24 hours. The average plasma clearance is about 0.058 l / kg / h, and the average renal clearance is about 0.048 l/kg/h. The renal clearance of vancomycin is fairly constant and ensures its elimination by 70-80%.

Pharmacokinetics in special clinical cases

Impaired renal function slows down the elimination of vancomycin. In patients with anuria, the average T 1/2 is 7.5 days.

The overall systemic and renal clearance of vancomycin may be reduced in elderly patients as a result of a natural slowing of glomerular filtration.

Indications

For intravenous infusions

Vancomycin is used for serious or severe infections caused by sensitive microorganisms, including:  Staphylococcus spp. (including penicillin-forming and methicillin-resistant strains), Streptococcus spp. (including penicillin-resistant strains), with an allergic reaction to penicillin, with intolerance to other antimicrobial drugs.

Endocarditis

Endocarditis caused by Streptococcus viridans, Streptococcus bovis (monotherapy, combination therapy with aminoglycosides); endocarditis caused by enterococci (including Eterococcus faecalis; as a combination therapy with aminoglycosides for treatment); early endocarditis caused by Staphylococcus epidermidis, Corynebacterium spp. after valve replacement (in combination with rifampicin, aminoglycosides/both antibiotics); prevention of bacterial endocarditis in patients with penicillin resistance and heart valve diseases (regardless of their etiology) before oral surgery, tonsillectomy, removal of adenoids, before bladder catheterization, cystoscopy surgery on the rectum or colon (monotherapy or in combination with aminoglycosides).

– sepsis;

– bone and joint infections;

– central nervous system

infections; – lower respiratory tract

infections; – skin and soft tissue infections.

Use during pregnancy and lactation

Use of the drug during pregnancy – only for “vital” indications, if the intended benefit to the mother exceeds the potential risk to the fetus.

The use of the drug during breastfeeding is contraindicated.

Contraindications

-Breast-feeding period;

– hypersensitivity to vancomycin and other components of the drug;

– neuritis of the auditory nerve.

With caution: Hearing impairment (including a history), renal failure, pregnancy (I, II and III trimester), patients with teicoplanin allergy (possible cross-allergy).

Side effects

From the cardiovascular system:  cardiac arrest, “hot flashes”; low blood pressure, shock (symptoms are mainly associated with rapid infusion of the drug), vasculitis, thrombophlebitis.

From the digestive system:  nausea, pseudomembranous colitis, increased activity of “hepatic” transaminases.

From the hematopoietic system:  agranulocytosis, eosinophilia, neutropenia, thrombocytopenia, pancytopenia, anemia, leukopenia.

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

Sensory disorders: ototoxic effects (transient/permanent): tinnitus, dizziness, and hearing loss. In most cases, ototoxic effects were observed in patients receiving excessive doses of vancomycin, with a history of hearing loss, or in patients receiving concomitant treatment with other drugs with possible development of ototoxicity, for example, aminoglycosides.

Dermatological reactions:  exfoliative dermatitis, rash.

Allergic reactions:  urticaria, anaphylactoid reactions (associated with rapid infusion of the drug), Stevens-Johnson syndrome, toxic epidermal necrolysis, pruritic dermatosis, benign pemphigus dermatosis, diffuse exfoliative erythroderma (red man syndrome – redness of the upper body, pain and spasm of the chest and back muscles; after stopping the infusion, reactions usually pass within 20 minutes, but sometimes can last up to several hours), rash accompanied by eosinophilia and systemic manifestations.

Other services:  drug fever, phlebitis at the injection site, tissue necrosis at the injection site, pain at the injection sites, chills.

Interaction

Concomitant use of vancomycin with local anesthetics resulted in erythema, redness of the skin, and anaphylactoid reactions in children, and impaired intracardiac conduction in adults.

When used concomitantly with general anesthetics and vecuronium bromide, the frequency of side effects increases (the risk of lowering blood pressure, the development of neuromuscular blockade).

use of vancomycin at least 60 minutes before the anesthetic is administered may reduce the likelihood of these reactions.

When other potentially ototoxic and/or nephrotoxic drugs (aminoglycosides, amphotericin B, acetylsalicylic acid or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, cyclosporine, loop diuretics, polymyxin B, cisplatin, etacric acid) are used simultaneously and/or sequentially, careful monitoring is required for the possible development of ototoxicity symptoms (tinnitus, dizziness, and hearing loss) and nephrotoxicity (increased plasma creatinine and urea concentrations, hematuria, proteinuria, rash, eosinophilia, and eosinophiluria). Antihistamines, meclozin, phenothiazines, and thioxanthenes can mask symptoms of the ototoxic effect of vancomycin (tinnitus, vertigo).

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 pharmaceutically incompatible when mixed. The probability of precipitation increases with increasing concentration of vancomycin. It is necessary to thoroughly flush the intravenous system between the use 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

For intravenous infusion. It should not be administered intramuscularly or by intravenous bolus.

With intravenous use of vancomycin, the recommended concentration is not more than 5 mg / ml and the rate of use is not more than 10 mg / min.

For adults, the drug should be administered 2 g iv per day (500 mg every 6 hours/or 1 g every 12 hours). Each dose should be administered at a rate of no more than 10 mg / min and for at least 60 minutes. The maximum single dose is 1000 mg, the maximum daily dose is 2000 mg.

Children over 1 month of age should be given 10 mg / kg IV 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 one month. Each dose should be administered for at least 60 minutes. In such patients, it is advisable to carefully monitor the concentration of vancomycin in the blood plasma.

The maximum single dose for children is 15 mg / kg of body weight, the daily dose for a child should not be higher than the daily dose for an adult (2 g).

In obese patients, the drug is used in normal doses.

Patients with impaired renal function should be individually selected dose. Creatinine clearance (CC) can be used to select the dose of vancomycin for this group of patients.

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 / 24 hours. With anuria, it is recommended to enter 1 g every 7-10 days.

Correction by increasing the intervals between injections

In patients with severe renal insufficiency, it is advisable to adjust the dose by increasing the intervals between injections: with creatinine clearance of 10-50 ml / min-1 g every 3-7 days, with creatinine clearance

In premature children and elderly patients, a significant dose reduction may be required as a result of reduced renal function.

Preparation of the solution for intravenous use

The solution is prepared by adding 10 ml of water for injection to 500 mg and 20 ml to 1000 mg. Reconstituted 10 ml (or 20 ml) solution of Vancomycin Elf is added to 100 ml (or 200 ml) of 5% dextrose solution or 0.9% sodium chloride solution to obtain a 5 mg/ml solution of vancomycin for infusions.

Before infusion, the prepared solution for parenteral use should be visually checked for mechanical impurities and discoloration.

Overdose

Symptoms: increased severity of dose-dependent side effects.

Treatment: symptomatic therapy aimed at maintaining glomerular filtration. Vancomycin is poorly removed during dialysis. There is evidence that hemofiltration and hemoperfusion through polysulfone ion exchange resin leads to an increase in the clearance of vancomycin.

Special instructions

Rapid use of vancomycin (within a few minutes) can be accompanied by a marked decrease in blood pressure and, in rare cases, cardiac arrest. Vancomycin should be administered as a diluted solution for at least 60 minutes to avoid adverse reactions associated with rapid infusion. Patients receiving intravenous vancomycin should have their blood tested periodically and have their kidney function monitored.

When prescribing the drug to newborns (especially premature babies), monitoring the concentration of vancomycin in the blood serum is desirable.

Vancomycin is used for serious or severe infections caused by sensitive microorganisms, including: Staphylococcus spp. (including penicillin-forming and methicillin-resistant strains), Streptococcus spp. (including penicillin-resistant strains) with an allergic reaction to penicillin, intolerance to other antimicrobial drugs.

Vancomycin should be used with caution in patients with renal insufficiency and in patients over 60 years of age (it is advisable to determine the concentration of vancomycin in blood plasma), since high, long-term concentrations of the drug in the blood can increase the risk of toxic effects of the drug (maximum concentrations of vancomycin in blood serum (Cmax) should not exceed 40 mcg/ml, and the minimum – 10 mcg/ml, concentration >80 mcg/ml is considered toxic).

For patients with renal insufficiency, the dose of vancomycin should be selected individually.

When prescribing the drug, thrombophlebitis may occur; the likelihood of their development can be reduced by slow use of dilute solutions (2.5-5 g / l) and alternating sites of use of the drug.

There are reports of cases of ototoxicity in patients treated with vancomycin. Signs of ototoxicity may be temporary or permanent.

Ototoxicity has been reported to occur most frequently in patients who have received high doses of vancomycin, patients who have previously had hearing impairment, or patients who have received concomitant therapy with other ototoxic agents (for example, aminoglycosides).

When using the drug Vancomycin Elf, there may be signs of ototoxicity, both temporary and permanent. Usually, ototoxicity is observed in patients receiving high doses of the drug, as well as in patients with hearing impairment or with the simultaneous use of other ototoxic drugs.

With concomitant renal failure, the risk of ototoxicity of vancomycin increases.

Prolonged use of vancomycin can lead to the emergence of resistant bacterial strains and the development of superinfection. If superinfection develops during therapy, appropriate measures should be taken.

Pseudomembranous colitis associated with Clostridium difficile has been reported in rare cases in patients receiving intravenous vancomycin. Influence on the ability to drive vehicles and vehicles:During treatment with the drug, the ability to concentrate attention may decrease, which should be taken into account when driving vehicles or performing work that requires increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dry place, protected from light, at a temperature of 15 °C to 25 °C.

Keep out of the reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Vancomycin

Conditions of release from pharmacies

By prescription

Dosage form

infusion solution