Vancorus, powder and oral intake 1 g

Pharmacodynamics

Vancomycin is a tricyclic glycopeptide antibiotic, produced by Amycolatopsisorientalis, acts bactericidally on most microorganisms (on Enterococcus spp. – bacteriostatically). It blocks the synthesis of the bacterial cell wall at a site different from that of penicillins and cephalosporins (it does not compete with them for binding sites), firmly binding to the D-alanyl-D-alanine part of the cell wall precursor, which leads to cell lysis.

Active against Gram-positive microorganisms, including: Staphylococcusaureus andStaphylococcusepidermidis(including heterogeneous methicillin-resistant strains),Streptococcusspp.,Enterococcusspp. (including Enterococcus faecalis), Clostridium spp. (including Clostridium difficile). Listeria monocytogenes, bacterial genera Lactobacillus spp., Actinomyces spp., Bacillus spp. are sensitive to vancomycin in vitro.

The maximum effect is at pH 8, at lowering pH to 6 the effect sharply decreases.

It is active only against microorganisms in the reproduction stage.

Resistant to almost all Gram-negative bacteria, Mycobacterium spp., fungi, viruses, protozoa. It does not have cross-resistance with other antibiotics.

When administered orally it has no systemic action, it acts locally on sensitive microflora in the gastrointestinal tract (Staphylococcus aureus, Clostridium difficile).

Pharmacokinetics

The maximum concentration (Cmax) after intravenous infusion of 500 mg is 49 µg/ml after 30 minutes and 20 µg/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. The binding to plasma proteins is 55%.

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

Vancomycin penetrates through the placenta. It is excreted with breast milk.

Half-life (T1/2) in normal renal function: adults – about 6 hours (4-11 hours), newborns – 6-10 hours, infants – 4 hours, older children – 2-3 hours; T1/2 in chronic renal failure (oliguria or anuria) in adults – 6-10 days. Cumulation is possible when administered repeatedly. 75-90% of the drug is excreted by the kidneys by passive filtration in the first 24 hours. In patients with one kidney it is excreted slowly and the excretion mechanism is unknown.

In small and moderate amounts vancomycin may be excreted with bile. It is excreted in small amounts by hemodialysis or peritoneal dialysis. It is poorly adsorbed by ingestion and usually does not penetrate into the systemic bloodstream. Detectable plasma concentrations of vancomycin may be observed in isolated cases with repeated oral administration in patients with acute pseudomembranous colitis caused by C. difficile.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to vancomycin:

endocarditis;
sepsis;
meningitis;
lower respiratory tract infections (pneumonia, lung abscess);
infections of bones and joints (including osteomyelitis);
skin and soft tissue infections;

In the form of an oral solution: pseudomembranous colitis caused by Clostridium difficile; enterocolitis caused by Staphylococcus aureus.

Pharmacological effect

Pharmacodynamics

Vancomycin is a tricyclic glycopeptide antibiotic produced by Amycolatopsis orientalis and has a bactericidal effect on most microorganisms (bacteriostatic on Enterococcus spp.). Blocks the synthesis of the bacterial cell wall in a site different from 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), Streptococcus spp., Enterococcus spp. (including Enterococcus faecalis), Clostridium spp. (including Clostridium difficile). Listeria monocytogenes, bacterial genera Lactobacillus spp., Actinomyces spp., Bacillus spp. are sensitive to vancomycin in vitro.

The optimum action is at pH 8; when the pH decreases to 6, the effect decreases sharply.

Actively affects only microorganisms that are in the stage of reproduction.

Almost all gram-negative bacteria, Mycobacterium spp., fungi, viruses, and protozoa are resistant. Does not have cross-resistance with other antibiotics.

When used orally, it has no systemic effect; it acts locally on sensitive microflora in the gastrointestinal tract (Staphylococcus aureus, Clostridium difficile).

Pharmacokinetics

The maximum concentration (Cmax) after intravenous infusion of 500 mg is 49 mcg/ml after 30 minutes and 20 mcg/ml after 1-2 hours; after intravenous infusion of 1 g – 63 mcg/ml after 60 minutes and 23-30 mcg/ml after 1-2 hours. Connection with plasma proteins – 55%.

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

Vancomycin crosses the placenta. Excreted in breast milk.

Half-life (T1/2) with normal renal function: adults – about 6 hours (4-11 hours), newborns – 6-10 hours, infants – 4 hours, older children – 2-3 hours; T1/2 for 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 by passive filtration in the first 24 hours. In patients with one kidney, excretion is slow and the mechanism of elimination is unknown.

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

Special instructions

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

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

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

The incidence and severity of thrombophlebitis can be reduced by properly diluting the original solution and alternating the sites of drug administration.

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

It is advisable to determine the concentrations of vancomycin in the blood serum in patients over 60 years of age with renal failure, since high, long-lasting concentrations of vancomycin in the blood can increase the risk of toxic effects of the drug (maximum concentrations should not exceed 40 mcg/ml, and minimum concentrations should not exceed 10 mcg/ml; concentrations above 80 mcg/ml are considered toxic). For patients with renal failure, doses of vancomycin should be individualized.

Active ingredient

Vancomycin

Composition

1 bottle of lyophilisate for preparing a solution for infusion contains:

active ingredient:

vancomycin (in the form of hydrochloride) 1 g.

Pregnancy

During pregnancy (II-III trimester), the drug Vancorus is prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus.

Vancomycin is excreted in breast milk. Breastfeeding should be stopped while taking the drug.

Contraindications

Hypersensitivity to vancomycin,
acoustic neuritis,
pregnancy (first trimester),
lactation period.

Side Effects

Post-infusion reactions (due to rapid administration): anaphylactoid reactions (decrease in blood pressure, cardiac arrest, bronchospasm, dyspnea, skin rash, itching); “red man” syndrome associated with the release of histamine (chills, fever, rapid heartbeat, flushing of the upper half of the body and face, spasm of the chest and back muscles).

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 senses: ototoxicity – hearing loss, vertigo, tinnitus.

From the hematopoietic organs: reversible neutropenia, transient thrombocytopenia, agranulocytosis.

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

Local reactions (if the infusion rules are violated): pain and tissue necrosis at the injection sites, phlebitis.

Interaction

With simultaneous intravenous administration of vancomycin and local anesthetics, erythematous rashes and hyperemia of the skin of the face may appear, and in adults, intracardiac conduction disturbances may occur.

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, capreomycin, carmustine, cyclosporine, loop diuretics, including ethacrynic acid, polymyxin B, cisplatin), careful monitoring of the possible development of data is required symptoms.

Cholestyramine reduces the activity of vancomycin when taken orally.

Antihistamines, meclozine, phenothiazines, thioxanthenes can mask the symptoms of vancomycin ototoxicity (tinnitus, vertigo).

Pharmaceutical interactions

Vancomycin solution has a low pH, which may 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 likelihood of precipitation increases with increasing concentrations of vancomycin. The intravenous system should be adequately flushed between uses of these antibiotics. In addition, it is recommended to reduce vancomycin concentrations to 5 mg/ml or less.

Overdose

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

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

Storage conditions

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

Shelf life

2 years

Manufacturer

Sintez, Russia