Vancomycin lyophilizate for solution for infusion 1g vial 1pc

Composition

>of 1 fl. contains vancomycin (in the form of hydrochloride) 1000 mg

Pharmacological action

The antibiotic glycopeptide produced by Amycolatopsis orientalis acts bactericidally 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 D-alanyl-D-alanine residues of peptidoglycan subunits – the main component of the cell wall, which leads to cell lysis.

Active against gram-positive microorganisms: Staphylococcus spp. (including penicillinase-forming and methicillin-resistant strains), Streptococcus spp., Streptococcus pneumoniae (including penicillin-resistant strains), Corynebacterium spp., Enterococcus spp., Clostridium spp., Actinomyces spp.

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.

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

Pharmacokinetics:

Poorly absorbed when taken orally. With intraperitoneal use, systemic absorption of up to 60% is possible (when administered at a dose of 30 mg/kg, the plasma concentration is about 10 mg/kg). About 60% of the dose is absorbed after 6 h. Plasma protein binding is 55%. After I/V use the volume of distribution of 0.39-0.92 l/kg Cmax after the on/in infusion 500 mg – 49 µg/ml after 30 min and 20 µg/kg in 1-2 h; after the on/in infusion 1 g – 63 µg/ml after 60 min and 23 to 30 µg/ml in 1-2 hours

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

Penetrates through the placenta. It is excreted in breast milk. It is practically not metabolized.

T1 / 2 for normal renal function: adults-about 6 hours (4-11 hours), newborns – 6-10 hours, children – 4 hours, older children – 2-3 hours; T1/2 for CRF (oliguria or anuria) in adults – 6-10 days. With repeated use, accumulation is possible,75-90% of the drug is excreted by the kidneys by passive filtration in the first 24 hours; in patients with a removed or absent kidney, it is excreted slowly and the mechanism of elimination is unknown.

In small and moderate amounts, it can be excreted with bile. It is excreted in small amounts during hemodialysis or peritoneal dialysis.

Indications

Sepsis, endocarditis, pneumonia, lung abscess, bone and joint infections (including osteomyelitis), meningitis, pseudomembranous colitis caused by Clostridium difficile, enterocolitis, skin infections.

Contraindications

Hypersensitivity, lactation, neuritis of the auditory nerve.

With caution. Hearing impairment (including a history), kidney failure, pregnancy.

Side effects

Post-infusion reactions (due to rapid use): anaphylactoid reactions (decreased blood pressure, bronchospasm, shortness of breath, 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) is more common 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. Rarely-interstitial nephritis.

From the digestive system: nausea, pseudomembranous colitis.

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

Hematopoietic disorders: reversible neutropenia, transient thrombocytopenia, rarely-agranulocytosis.

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

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

Interaction

When administered concomitantly with local anesthetics, children may develop erythematous rashes and hyperemia of the skin of the face, while adults may have a violation of intracardiac conduction.

Concomitant use with nephrotoxic and ototoxic drugs (aminoglycosides, amphotericin B, ASA or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, cyclosporine, loop diuretics, polymyxin B, cisplatin, etacric acid) is not recommended.

Colestyramine reduces its effectiveness.

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

General anesthetics and vecuronium bromide – risk of lowering blood pressure or developing neuromuscular blockade. Infusion of vancomycin is possible at least 60 minutes before their introduction.

How to take, course of use and dosage

I/O only (iv injections are painful) at a rate of no more than 10 mg / min; the duration of the infusion should be at least 60 minutes. Adults-0.5 g or 7.5 mg / kg every 6 hours or 1 g or 15 mg/kg every 12 hours.

Newborn children – 15 mg / kg, and then 10 mg / kg every 12 hours; in children aged 1 month, the same dose is used every 8 hours. For children older than 1 month – 10 mg/kg every 6 hours or 20 mg/kg every 12 hours.

In patients with impaired renal excretory function, the initial dose is 15 mg / kg, then the dosage regimen is adjusted taking into account the values of creatinine clearance (with uremia, the interval between injections is up to 10 days): with creatinine clearance of more than 80 ml / min-the usual dose, creatinine clearance of 50-80 ml / min-1 g every 1-3 days,10-50 ml / min-1 g every 3-7 days, less than 10 ml / min-1 g every 7-14 days.

Creatinine clearance can be calculated by the formula For men: body weight (kg) * (140 – age (years)/72 * serum creatinine concentration (mg / dl), for women – the result is multiplied by 0.85.

The powder is dissolved in water for injection: 500 mg – in 10 ml,1 g-in 20 ml (the solution concentration is 50 mg / ml). The resulting solution is diluted with 0.9% NaCl solution or 5% dextrose solution: for 500 mg-100 ml and for 1 g-200 ml.

With pseudomembranous colitis-inside, in the form of a solution in 30 ml of water: adults-0.5-2 g divided into 3-4 doses, children-0.04 g / kg divided into 3-4 doses, no more than 2 g per day. The duration of treatment is 7-10 days.

Overdose

Symptoms: increased severity of side effects.

Treatment: symptomatic, combined with hemoperfusion and hemofiltration.

Special instructions

Use in the II-III trimester of pregnancy is possible only for “vital” indications.

When prescribing to preterm and normal newborns, monitoring of serum concentrations is desirable.

Concomitant use with general anesthetics increases the frequency of side effects, so it is better to administer vancomycin before general anesthesia.

During treatment, it is necessary to conduct an audiogram, determine kidney function (urinalysis, creatinine and urea nitrogen).

It is advisable to determine the concentration of vancomycin in the blood serum (in patients with renal insufficiency, in patients older than 60 years).

Maximum concentrations should not exceed 40 micrograms/ml, and minimum concentrations should not exceed 10 micrograms / ml. Concentrations above 80 micrograms / ml are considered toxic.

Storage conditions

The drug should be stored in a dry place, protected from light, inaccessible to children at a temperature not exceeding 8°C.

Shelf

life is 2 years. Do not use after the expiration date.

Active ingredient

Vancomycin

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

For adults as prescribed by a doctor, for children as prescribed by a doctor

Indications

Infectious Diseases, Osteomyelitis, Pneumonia