Vancomycin - instructions for use, dose, side effects, contraindications

Antibacterial agent, produced Amycolatopsis orientalis, acts bactericidal against most microorganisms (on enterococci - bacteriostatic).It blocks the synthesis of the bacterial cell wall in a region different from that of penicillins and cephalosporins (does not compete with them for binding sites), firmly linking to D-alanyl-D-alanine part of the precursor of the cell wall, which leads to cell lysis. It is also able to change the permeability of bacterial cell membranes and selectively inhibit the synthesis of RNA. It is active against gram-positive microorganisms: Staphylococcus spp. (including penicillinase-forming and methicillin-resistant strains), Streptococcus spp., Streptococcus pneumoniae (including strains resistant to penicillin), Corynebacterium spp., Enterococcus spp., Clostridium spp., Actinomyces spp.

Maximum active with pH 8, when the pH is reduced to 6, the effect decreases sharply. Actively acts only on microorganisms, which are in the stage of reproduction.

Vancomycin is resistant to almost all gram-negative bacteria, Mycobacterium spp., fungi, viruses, protozoa. Has no cross-resistance with other antibiotics.

Pharmacokinetics:

After intravenous administration, the volume of distribution is 0.39-0.92 l / kg. The maximum concentration in blood plasma (FROM_mOh) after intravenous administration of 0.5 g of vancomycin is 49 μg / ml after 30 minutes and 20 μg / kg after 1-2 hours; after administration of 1 g - 63 mcg / ml after 60 min and 23-30 mcg / ml after 1-2 h. The connection with plasma proteins is 55%.

Achieves therapeutic concentrations in body tissues and fluids: in ascites, synovial, pleural and pericardial fluids, peritoneal dialysate fluid, in urine, atrial auricle tissue. Does not penetrate the blood-brain barrier (with meningitis detected in the cerebrospinal fluid in therapeutic concentrations). Penetrates through the placental barrier. Excreted in breast milk.

Virtually not metabolized. Half-life with normal renal function: adults - about 6 hours (4-11 hours), newborns 6-10 hours, infants 4 hours, older children 2-3 hours. In chronic renal failure (oliguria or anuria), the elimination half-life increases to 6-10 days.

With repeated introduction, cumulation is possible.

75-90% of the drug is excreted by the kidneys by passive filtration in the first 24 hours; in patients with a deleted or missing kidney is slowly withdrawn and the removal mechanism is unknown. In small and moderate amounts can be excreted with bile. In small amounts, it is excreted in hemodialysis or peritoneal dialysis.

Indications:

Sepsis, endocarditis, pneumonia, lung abscess, infections of bones and joints (incl.osteomyelitis), meningitis, skin and soft tissue infections.

For oral administration: pseudomembranous colitis caused by Clostridium difficile; enterocolitis caused by Staphylococcus aureus.

Contraindications:

Hypersensitivity, pregnancy (I trimester), lactation period, neuritis of the auditory nerve.

Carefully:

Hearing impairment (including in history), renal failure.

Pregnancy and lactation:

Application in pregnancy (II and III trimester) is possible only on "vital" indications.

Stop breastfeeding.

Dosing and Administration:

Introduced only intravenously (intramuscular injections are painful) at a rate of not more than 10 mg / min; duration of 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 up to 7 days of life - 15 mg / kg, then 10 mg / kg every 12 hours.

Children up to 1 month old: apply the same dose every 8 hours.

Children over 1 month old - 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 corrected taking into account the values of creatinine clearance (CC): with CC above 80 ml / min - usual dose, KK 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.

Preparation of Vancomycin Solution: the powder is dissolved in water for injection: 0.5 g in 10 ml, 1 g in 20 ml (the concentration of the solution is 50 mg / ml). The resulting solution is diluted with 0.9% sodium chloride solution or 5% dextrose solution, or Ringer's solution: for 0.5 g - 100 ml and for 1 g - 200 ml.

Solutions prepared on the basis of 0.9% sodium chloride or 5% dextrose can be stored in the refrigerator (2-8) ° C for 14 days without significant loss of activity. Solutions prepared on the basis of Ringer's solution can be stored in the refrigerator for 4 days (96 hours).

With pseudomembranous colitis and enterocolitis - Inside, in the form of a solution in 30 ml of water: for adults - 0.5-2 g divided into 3-4 doses; children - 0.04 g / kg divided into 3-4 doses, not more than 2 grams a day. The duration of treatment is 7-10 days.

Side effects:

Post-fusion reactions (due to rapid administration): anaphylactoid reactions - (lowering blood pressure, bronchospasm, dyspnoea, skin rash, itching), red man syndrome associated with histamine release (chills, fever, heart palpitations, hyperemia of the upper body and face, spasm 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 the appointment of more than 3 weeks in high doses, manifested by an increase in the concentration of creatinine and urea nitrogen. Rarely - interstitial nephritis.

On the part of the digestive system: nausea, pseudomembranous colitis.

From the sense organs: ototoxicity - hearing loss, vertigo, ringing in the ears.

From the hematopoiesis: reversible neutropenia, transient thrombocytopenia; rarely - agranulocytosis.

Local reactions (in violation of infusion rules): phlebitis, pain at the injection site, tissue necrosis at the site of administration.

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

Overdose:

Symptoms: increased severity of side effects.

Treatment: symptomatic, in combination with hemoperfusion and hemofiltration.

Interaction:

With simultaneous appointment with local anesthetics, children may experience erythematous rashes and hyperemia of the skin of the face, in adults - violation of intracardiac conduction.

It is not recommended simultaneous administration with nephrotoxic and ototoxic drugs (aminoglycosides, amphotericin B, acetylsalicylic acid or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, ciclosporin, "loop" diuretics, polymyxin AT, cisplatin, ethacrynic acid).

Kolestyramin reduces the effectiveness of vancomycin.

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

When used simultaneously with common anesthetics and vecuronium bromide, the frequency of side effects increases (risk of lowering blood pressure, development of neuromuscular blockade), so infusion of vancomycin is possible at least 60 minutes before administration.

Special instructions:

When appointing newborn children (especially - premature), it is desirable to monitor the concentration of the drug in the blood serum.

During the treatment it is necessary to conduct an audiogram, monitoring the kidney function (urine analysis, creatinine and urea nitrogen).

It is desirable to monitor the concentration of vancomycin in the serum with renal failure,and also in patients older than 60 years. The maximum concentration is not should exceed 40 μg / ml, and the minimum - 10 μg / ml. Concentration above 80 mcg / ml is considered toxic.

Form release / dosage:Powder for solution for infusion, 0.5 g and 1.0 g of active substance.

Packaging:

In bottles with a capacity of 10 ml, 20 ml.

1 bottle with instructions for use in a pack of cardboard.

10 bottles with instructions for use in a cardboard box.

For hospital:

- 50 bottles and 5 instructions for use in a cardboard box;

- 1 bottle with instructions for use (from 1 to 50 bottles with an equal number of instructions for use) in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

At the expiration date of the drug unused bottles carefully dissolve, dissolve the contents a large amount of water and drain into sewerage.

Shelf life:

2 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003482/10

Date of registration:27.04.2010 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp21.01.2017

Illustrated instructions

Instructions

Vancomycin (Vancomycin)