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.

The optimum action is when 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.

Almost all Gram-negative bacteria are resistant, Mycobacterium spp., Fungi, viruses, protozoa.

Has no cross-resistance with other antibiotics.

Pharmacokinetics:

The maximum concentration (C_mOh) after intravenous infusion of 500 mg - 49 μg / ml after 30 minutes and 20 μg / kg after 1-2 hours; after intravenous infusion of 1 g - 63 mcg / ml after 60 min and 23-30 mcg / ml after 1-2 h.

Connection with plasma proteins - 55%.

Therapeutic concentrations are determined in ascites, synovial, pleural, pericardial and peritoneal fluids, in the urine, atrial auricle tissue. It does not penetrate the intact blood-brain barrier (with meningitis found in the cerebrospinal fluid at therapeutic concentrations). Penetrates through the placenta. Excreted in breast milk.

Virtually not metabolized.

The half-life (T_1/2) with normal kidney function: adults - about 6 hours (4-11 hours), newborns - 6-10 hours, infants - 4 hours, children of older age - 2-3 hours; T_1/2with 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by the kidneys by passive filtration in the first 24 hours; in patients with a deleted or missing kidney is slowly withdrawn and the removal mechanism is unknown.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; meningitis; infection of the lower respiratory tract (pneumonia, lung abscess); infection of bones and joints (incl.osteomyelitis); pseudomembranous colitis (not associated with the use of antibiotics), caused by Clostridium difficile, enterocolitis; infections of the skin and soft tissues.

Contraindications:

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

Carefully:

Hearing impairment (including in anamnesis), renal failure, pregnancy (II-III trimesters).

Pregnancy and lactation:Application in II-III trimester of pregnancy is possible only according to "vital" indications.

Dosing and Administration:

Only intravenously, the recommended concentration is not more than 5 mg / ml with a rate of administration 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 during the first week of life - an initial dose of 15 mg / kg, followed by 10 mg / kg every 12 hours; beginning with the second week of life, apply the the same dose 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 initial dose - 15 mg / kg, more dosing regime taking into account correcting the creatinine clearance values (in anuria interval between injections - up to 10 days): the creatinine clearance greater than 80 mL / min - the usual dose,with a 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 calculate according to 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).

Preparation of the solution

The powder 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 subject to further dilution with 0.9% sodium chloride solution or 5% dextrose solution to a concentration of not more than 5 mg / ml (for 500 mg - 100 ml and for 1 g - 200 ml). The prepared solution is used immediately.

Preparation of solution for oral administration

Vancomycin can be used orally to treat pseudomembranous colitis caused by Clostridium difficile, and staphylococcal enterocolitis.

Appropriate dose is prepared in 30 ml of water: for adults - for 0,5-2 g 3-4 times, children - 0.04 g / kg 3-4 times. 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 person" syndrome, associated with the release of histamine (chills, fever,heart palpitations, hyperemia of the upper half of the trunk and face, spasm of muscles of the chest and back).

From the urinary system: nephrotoxicity (up to the development of renal insufficiency), more often when combined with aminoglycosides or when administered for more than 3 weeks in high concentrations, manifested by an increase in the concentration of creatinine and urea nitrogen. Rare interstitial nephritis.

On the part of the organs of the gastrointestinal tract: nausea, pseudomembranous colitis.

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

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

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

Local Reactions: phlebitis, pain and necrosis of tissues at the site of administration.

Overdose:

Symptoms: increased severity of side effects.

Treatment: symptomatic, in combination with hemoperfusion and hemofiltration.

Interaction:

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

Simultaneous administration with nephro- and ototoxic drugs (aminoglycosides, amphotericin B, acetylsalicylic acid or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, ciclosporin, "loop" diuretics, polymyxin AT, cisplatin, ethacrynic acid) requires careful monitoring of the possible development of these symptoms.

Kolestyramin reduces effectiveness.

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

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

The solution of vancomycin has a low pH, which can cause physical or chemical instability when mixed with other solutions. Avoid mixing with alkaline solutions.

Special instructions:

When prescribing preterm and newborns, control over the concentration of the drug in the blood serum is desirable.

With simultaneous administration with general anesthetics, the incidence of side effects increases, so vancomycin it is better to administer before general anesthesia.

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

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

The likelihood of developing local reactions can be reduced by slowly introducing dilute solutions (2.5-5 g / l) and alternating injection sites.

Form release / dosage:

Powder for solution for infusion, 0.5 g and 1.0 g.

Packaging:

0.5 g or 1.0 g of active substance is placed in a vial.

Solvent - "Water for Injection", 2 ml or 5 ml produced by JSC "Pharmasintez", Russia (RU No. LP-001844)

One bottle with 0.5 g of the drug, together with instructions for use, is placed in a cardboard pack.

One bottle with 1.0 g of the drug, together with the instruction for use, is placed in a cardboard pack.

One bottle with 0.5 g of the drug and one ampoule with 10 ml of solvent together with the instruction for use are placed in a cardboard box with septa.

One bottle with 1.0 g of preparation and two (2) ampoules of 10 ml of solvent together with instructions for use are placed in a cardboard box with septa.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005916/08

Date of registration:28.07.2008 / 29.01.2016

Expiration Date:Unlimited

The owner of the registration certificate:FARMGID CJSCFARMGID CJSC Russia

Manufacturer: & nbsp

Laika Labs Limited India

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp22.01.2017

Illustrated instructions

Instructions

Vancomycin (Vancomycin)