Vancomycinum

General characteristics. Structure:

Active ingredient: 500 mg or 1000 mg of Vancomycinum of a hydrochloride.

Pharmacological properties:

Pharmacodynamics. Antibacterial agent, is produced by Amycolatopsis orientalis, affects bakteritsidno the majority of microorganisms (on enterococci - bacteriostatically). Blocks synthesis of a cell wall of bacteria in the site, other than what penicillin and cephalosporins affect (does not compete with them for binding sites), strongly contacting D - alanyl - a D-alanine part of the predecessor of a cell wall that leads to a lysis of a cell. It is also capable to change permeability of cellular membranes of bacteria and to selectively slow down RNA synthesis. It is active concerning gram-positive microorganisms: Staphylococcus spp. (including penitsillinazoobrazuyushchy and metitsillinorezistentny strains), Streptococcus spp., Streptococcus pneumoniae (including strains, resistant to penicillin), Corynebacterium spp., Enterococcus spp., Clostridium spp., Actinomyces spp. Shows the most expressed antibacterial action at pH 8, at decrease in pH to the 6th the effect sharply decreases. Actively affects only the microorganisms which are in a reproduction stage. Almost all gram-negative bacteria, Mycobacterium spp are steady., mushrooms, viruses, the elementary. Has no cross resistance with other antibiotics.

Indications to use:

Endocarditis. Vancomycinum is effective both at monotherapy, and in a combination with aminoglycosides for treatment of the endocarditis caused by Streptococcus viridans or S. bovis. At an endocarditis, caused by enterococci (for example, E. faecalis), Vancomycinum is effective only in combination with aminoglycosides. There are data that vankomition it is effective at treatment of a diphtheroid endocarditis. Vancomycinum is successfully applied in combination with rifampicin, aminoglycosides or with both antibiotics at the early endocarditis caused by S. epidermidis or diphtheroidis after prosthetics of the valve. In some cases Vancomycinum is shown for prevention of an endocarditis.

Sepsis.

Infections of bones and joints.

Infections of lower parts of respiratory tract.

Infections of skin and soft tissues.

Vancomycinum can be also applied at the infections caused by gram-positive microorganisms in cases:

- allergies to penicillin;

- intolerance or lack of the response to treatment by other antibiotics, including penicillin or cephalosporins;

- the infections caused by the microorganisms sensitive to Vancomycinum, but steady against other germicides.

Pseudomembranous colitis - as solution for intake (see the section "Route of Administration and Doses").

Route of administration and doses:

The drug is administered only intravenously (intramuscular injections are painful) with a speed no more than 10 mg/min.; duration of infusion has to be not less than 60 min.

Each 6 hours are the adult - on 0,5 g or 7,5 mg/kg, or on 1 g or 15 mg/kg there are each 12 hours.

To newborn children - on 15 mg/kg, and then 10 mg/kg there are each 12 hours; at children at the age of 1 month each 8 hours apply the same dose.

Children are more senior than 1 month - on 10 mg/kg each 6 hours or on 20 mg/kg each 12 hours.

Patients with an impaired renal function need to select a dose individually. For selection of a dose of Vancomycinum for this group of patients it is possible to use serum creatinine level. At elderly patients Vancomycinum has lower clearance and bigger volume of distribution. At this group it is reasonable to carry out selection of a dose on the basis of concentration of Vancomycinum in serum. At premature children and at elderly patients as a result of reduced function of kidneys the considerable dose decline can be required. It is regularly necessary to control concentration of Vancomycinum in serum.

Features of use:

Use in the II-III trimester of pregnancy is possible only according to "vital" indications. At appointment as the premature and normal newborn control of concentration in blood serum is desirable. At a concomitant use with the general anesthetics the frequency of side effects therefore it is better to enter Vancomycinum before the general anesthesia increases. During treatment carrying out an audiogramma, definition of function of kidneys (the analysis of urine, indicators of creatinine and an urea nitrogen) is necessary. It is desirable to define concentration of Vancomycinum in blood serum (at a renal failure, at patients 60 years are more senior). The maximum concentration should not exceed 40 mkg/ml, and minimum - 10 mkg/ml. Concentration over 80 mkg/ml are considered as toxic. For patients with a renal failure of a dose of Vancomycinum have to be selected individually.

Bystry introduction (for example, within several minutes) Vancomycinum can be followed by the expressed lowering of arterial pressure and in rare instances, a cardiac standstill. Vancomycinum should be entered in the form of divorced solution within not less than 60 minutes to avoid the side reactions connected with infusion. Patients should appoint Vancomycinum with care with an allergy on тейкопланин since cases of a cross allergy were registered.

Vancomycinum is "the irritating agent" therefore diffusion of the dissolved drug through a vascular wall can cause a necrosis of adjacent fabrics. Thrombophlebitises can be observed though the probability of their development can be reduced due to slow introduction of weak solutions (2,5-5 g/l) and alternations of injection sites of drug.

Side effects:

Post-infusional reactions (owing to bystry introduction): anaphylactoid reactions (decrease in the ABP, a bronchospasm, диспноэ, skin rash, an itch), the syndrome of "the red person" connected with release of a histamine (a fever, fever, tachycardia, a hyperemia of an upper half of a trunk and person, a spasm of muscles of a thorax and back).

From an urinary system: nephrotoxicity (up to development of a renal failure) is more often at a combination with aminoglycosides or at appointment more than 3 weeks in high concentration, shown increase in concentration of creatinine and an urea nitrogen. Seldom - intersticial nephrite.

From digestive organs: nausea, pseudomembranous colitis.

From sense bodys: ototoxicity - decrease in hearing, вертиго, a ring in ears.

From bodies of a hemopoiesis: a reversible neutropenia, passing thrombocytopenia, it is rare - an agranulocytosis.

Local reactions (at infusion violation of the rules): phlebitis, pain in an injection site, a necrosis of fabrics in an injection site.

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

Interaction with other medicines:

At co-administration with local anesthetics children can have erythematic rashes and a hyperemia of integuments of the person, adults have a disturbance of endocardiac conductivity.

Co-administration with nefro-and ototoksichny HP is not recommended (aminoglycosides, Amphotericinum of B, ACK or other salicylates, bacitracin, буметанид, капреомицин, кармустин, паромомицин, cyclosporine, "loopback" diuretics, polymyxin B, Cisplatinum, Acidum etacrynicum). Colestyraminum reduces efficiency.

Antihistaminic HP, меклозин, fenotiazina, thioxanthenes can mask symptoms of ototoksichesky action of Vancomycinum (a sonitus, вертиго). The general anesthetics and a vekuroniya bromide - risk of decrease in the ABP or development of neuromuscular blockade. Infusion of Vancomycinum is possible at least in 60 min. prior to their introduction.

Solution of Vancomycinum has low рН that can cause physical or chemical instability when mixing with other solutions.

It is necessary to avoid mixing with alkaline solutions. Solutions of Vancomycinum and beta лактамных antibiotics are physically incompatible when mixing.

The probability of precipitation increases with increase in concentration of Vancomycinum. It is necessary to wash out adequately intravenous system between uses of these antibiotics. Besides, it is recommended to reduce concentration of Vancomycinum to 5 mg/ml and less.

Contraindications:

Hypersensitivity, lactation period, neuritis of an acoustical nerve, pregnancy (1st trimester).

With care: A hearing disorder (including in the anamnesis), a renal failure, pregnancy (the 2nd and 3rd trimesters).

Overdose:

Symptoms: strengthening of expressiveness of by-effects.

Treatment: The corrective therapy directed to maintenance of glomerular filtering. Vancomycinum badly is removed when carrying out dialysis. There are data that haemo filtering and hemoperfusion through polysulfonic ion-exchange resin leads to increase in clearance of Vancomycinum.

Storage conditions:

To store in the place protected from children and light at a temperature from 2 °C to 8 °C. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

The lyophilized powder for preparation of solution for infusions on 500 mg or 1000 mg in bottles in packaging No. 1, No. 40.