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

Antibacterial agent produced Amycolatopsis (Nocardia) orientalis. It is bactericidal. The mechanism of action is due to the blocking of polymerization of cell wall glycopeptides, which leads to the destruction of the microbial cell. Also alters the permeability of the cytoplasmic membrane and inhibits selectively the synthesis of ribonucleic acid bacteria. Target action is different from that of vancomycin, which are penicillins and cephalosporins, so between vancomycin and other antibiotics have not been cross-resistance.

It is selectively active against gram-positive microorganisms: Staphylococcus aureus, Staphylococcus epidermidis (including strains resistant to methicillin / oxacillin); most streptococci, including Streptococcus pyogenes, Streptococcus pneumoniae (including strains resistant to penicillin), Streptococcus agalactiae, green streptococci, Streptococcus bovis; enterococci, incl. Enterococcus faecalis and Enterococcus faecium (most strains E.faecium have an intermediate sensitivity to Vankomycin); Corynebacterium spp.; Listeria monocytogenes, Bacillus spp. Clostridium spp., (including toxin-producing strains Clostridium difficile, causing pseudomembranous colitis); Peptococcus spp., Peptostreptococcus spp. and Actinomyces spp.

Vancomabol® is inactive against gram-negative microorganisms (the exception is significant activity against Flavobacterium meningosepticum), mycobacteria, intracellular pathogens, Bacteroides spp. and mushrooms.

Optimum action is observed at pH 8; With a decrease in pH to 6, the antimicrobial effect decreases dramatically.

Pharmacokinetics:

In patients with normal renal function, immediately after infusion at a dose of 15 mg / kg for a duration of about 1 hour, the plasma concentrations are 63 μg / ml, after two hours they decrease to 23 μg / ml, and after 11 hours - up to 8 μg / ml . Volume of distribution - 0.39-0.92 l / kg. After intravenous (iv) administration of 500 mg of vancomycin with a duration of 30 min, plasma concentrations are 49 μg / ml; after 1-2 hours they decrease to 20 mcg / kg. With repeated administration does not cumulate. The connection with plasma proteins is 55%.

Well penetrates into many organs and tissues. Bactericidal concentrations are determined in ascites, synovial, pleural and pericardial fluids, in urine, atrial auricle tissue. It does not penetrate intact blood-brain barrier, but with inflammation of the meninges it is found in the cerebrospinal fluid in therapeutic concentrations. Penetrates through the placenta. Excreted in breast milk.

Half-life (T_1/2) with normal kidney function varies depending on age: in adults - about 6 hours (4-11 hours), in newborns - 6-10 hours, in children up to a year - 4 hours, in older children 2-3 hours . T_1/2 with impaired renal function and kidney failure increases, reaching in severe and terminal renal failure (creatinine clearance less than 10 mL / min) 6-10 days. In the body is practically not metabolized. 75-90% of the drug is excreted by the kidneys by glomerular filtration in the first 24 hours. In small and moderate amounts can be excreted through the intestine. In small amounts, it is excreted in hemodialysis or peritoneal dialysis.

Indications:

Intravenously:

Moderate and severe infections caused by resistant to penicillins and cephalosporins, Gram-positive aerobic cocci and Gram-positive bacteria and gram-positive infection in severe allergy to penicillin and cephalosporins:

- infections of the central nervous system caused by staphylococci and streptococci (especially S. pneumoniae) with multiple resistance, infections caused by Flavobacterium meningosepticum, including meningitis;

- lower respiratory tract infections, including community acquired and nosocomial pneumonia, lung abscess and pleural empyema;

- bacterial endocarditis caused by Streptococcus viridaris or Streptococcus bovis, endocarditis caused by enterococci (for example, Enterococcus faecalis), vancomycin is effective only in combination with aminoglycosides;

- infections of bones and joints (including osteomyelitis);

- infections of the skin and soft tissues;

- sepsis.

Contraindications:

Hypersensitivity to vancomycin, other glycopeptides, I trimester of pregnancy, lactation period, neuritis of the auditory nerve.

Carefully:

Pregnancy (II, III trimester), with hearing impairment (including in history), severe renal failure (dose adjustment required).

Pregnancy and lactation:

Vancomabol® should be given to women during pregnancy only in the second and third trimesters.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Vancomabol® is administered only by intravenous drip; the recommended concentration of solution for infusions is 5 mg / ml, the rate of administration is less than 10 ml / min.

Adults: usual doses in adults with normal renal function - 0.5 g every 6 hours, or 1 g every 12 hours. To treat bacterial meningitis, 500-750 mg every 6 hours is administered. The recommended duration of intravenous infusion of a single dose is 60 minutes.

In patients with impaired renal function a correction of the dose of Vancomabol® is required taking into account the values of creatinine clearance.

Dosage of Vancomabol® in patients with impaired renal function

Creatinine clearance, ml / min
>80	80-50	50-10	< 10
1 g every 12 hours	1 g every 1-3 days	1 g every 3-7 days	1 g every 7-14 days
In patients on hemodialysis: 1 g every 7-10 days

Children - 10 mg / kg every 6 hours; a single dose is administered as an intravenous infusion of about 1 hour. The maximum daily dose is no more than 2 g. For the treatment of bacterial meningitis, the dose is increased to 15 mg / kg, which is administered every 6 hours.

Newborn children - at 15 mg / kg, followed by 10 mg / kg every 12 hours.

Rules for the preparation of solution

The lyophilizate is dissolved in water for injection: 500 mg 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% saline or 5% dextrose solution: for 500 mg - 100 ml and for 1000 mg - 200 ml.

A ready-made solution for infusions should be administered as a slow intravenous infusion lasting about 60 minutes.

Side effects:

Post-fusion reactions: (due to rapid administration) associated with the massive release of histamine from mast cells: anaphylactoid reactions (arterial hypotension, bronchospasm, dyspnoea, skin rash, itching),the syndrome of "red man" (tachycardia, hyperemia of the upper body and face), chills, painful spasm of the muscles of the chest and back. These reactions pass independently after 20 minutes or several hours. To prevent the development of postinfusion complications, only slow intravenous infusion of Vancomabol® with a duration of at least 1 hour is used.

Allergic reactions: fever, nausea, chills, eosinophilia, rash (including exfoliative dermatitis), malignant exudative erythema (Stevens-Johnson syndrome), vasculitis.

From the urinary system: nephrotoxicity (increase of serum creatine, urea nitrogen, very rarely - development of renal insufficiency); rarely interstitial nephritis.

From the side of the digestive system: nausea, very rarely - pseudomembranous colitis.

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

On the part of the organs of hematopoiesis: reversible neutropenia (especially with prolonged admission); rarely - transient thrombocytopenia, agranulocytosis.

Local Reactions: phlebitis, pain at the injection site, with subcutaneous or intramuscular injection - necrosis of soft tissues.

Overdose:

Symptoms: increased severity of side effects.

Treatment: supporting and symptomatic therapy aimed at maintaining glomerular filtration. Vancomycin poorly washed away during hemodialysis. There are data on the effectiveness of hemofiltration and hemoperfusion using polysulfone ion-exchange resins to reduce the concentration of vancomycin in plasma.

Interaction:

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

General anesthetics and vecuronium bromide - the risk of lowering blood pressure or developing a neuromuscular blockade. Infusion of Vancomabol® is possible at least 60 minutes before administration.

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

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

Vancomabol® solutions are pharmaceutically incompatible with solutions of other antibiotics.

Special instructions:

To reduce the risk of nephrotoxicity in patients with existing renal dysfunction (including in elderly patients), in patients with hypovolemia, and simultaneously taking other nephrotoxic drugs (aminoglycosides, polymyxin B, amphotericin B, furosemide, antitumor drugs), dynamic monitoring of renal function is required, including indicators of creatinine and urea nitrogen, urinalysis.

The risk of ototoxicity is higher in the group of patients with initial impairment of kidney and hearing function (functional or organic damage to the inner ear and auditory nerve) and / or taking other ototoxic drugs. To reduce the risk of ototoxicity, especially with prolonged therapy with Vancomabol®, periodic monitoring of the audiogram is necessary.

Vancomycin has a local irritant effect in contact with soft tissue, especially in high concentrations.Therefore, you should strictly follow the procedure for intravenous administration and avoid getting the solution outside the vessel.

In preterm infants, control of serum concentrations of vancomycin is sometimes required to correct dosage regimens.

It is desirable to determine the concentration of vancomycin serum (in renal failure, in patients older than 60 years) to correct dosages and administration regimens. The maximum concentrations should not exceed 40 μg / ml, and the minimum concentration should not exceed 10 μg / ml. Concentrations above 80 μg / ml are considered toxic.

Form release / dosage:

Lyophilizate for the preparation of a solution for infusions, 500 mg and 1000 mg.

Packaging:

500 mg or 1000 mg of active substance into glass bottles with a capacity of 10 ml and 20 ml.

1 The vial of the preparation and the instruction for use is placed in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000126/09

Date of registration:14.01.2009 / 13.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp21.01.2017

Illustrated instructions

Instructions

Vancomobol® (Vancomabol®)