medicalmeds.eu Medicines Antibiotic of group of glycopeptides. Vankorus

Vankorus

Producer: JSC Sintez Russia

Code of automatic telephone exchange: J01XA01

Release form: Liquid dosage forms. Lyophilisate for preparation of solution for infusions.

Indications to use: Endocarditis. Sepsis. Meningitis. Lower respiratory tract infections. Pneumonia. Abscess of lungs. Osteomyelitis. Colitis. Coloenteritis.

General characteristics. Structure:

Lyophilisate for preparation of solution for infusions in the form of powder from color, white to white with a pink or light brown shade.

Active ingredient: 1 фл.
Vancomycinum (in the form of a hydrochloride) 500 mg

Excipients: Mannitolum - 0.02 g.

Lyophilisate for preparation of solution for infusions in the form of powder from color, white to white with a pink or light brown shade.

Active ingredient: 1 фл.
Vancomycinum (in the form of a hydrochloride) 1 g

Excipients: Mannitolum - 0.04 g.

Pharmacological properties:

Antibiotic - glycopeptide. Amycolatopsis orientalis is produced.

Affects bakteritsidno the majority of microorganisms, sensitive to it (on Enterococcus spp. - 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 bacterial cell.

It is active concerning gram-positive microorganisms, including: Staphylococcus aureus and Staphylococcus epidermidis (including heterogeneous Methicillinum - resistant strains), Streptococcus spp., Enterococcus spp. (including Enterococcus faecalis), Clostridium spp. (including Clostridium difficile).

Listeria monocytogenes, Lactobacillus spp are sensitive to Vancomycinum of in vitro., Actinomyces spp., Bacillus spp.

Optimal effect – at рН 8, at decrease рН to the 6th effect of Vancomycinum sharply decreases.

Actively affects only the microorganisms which are in a reproduction stage.

Almost all gram-negative bacteria, Mycobacterium spp are steady against Vancomycinum., mushrooms, viruses, the elementary.

Has no cross resistance with antibiotics of other groups.

At use inside has no systemic action, affects locally sensitive microflora in a GIT (Staphylococcus aureus, Clostridium difficile).

Pharmacokinetics. Absorption and distribution

Cmax later in/in infusion of 500 mg – 49 mkg/ml in 30 min. and 20 mkg/ml in 1-2 h; later in/in infusion of 1 g – 63 mkg/ml in 60 min. and 23-30 mkg/ml in 1-2 h.

Linkng with proteins of plasma – 55%.

It is widely distributed in the majority of fabrics and liquids of an organism. Therapeutic concentration are defined in ascitic, synovial, pleural, pericardiac and peritoneal liquids, in urine, auricula atrii fabric. Does not get through the unimpaired GEB (at meningitis it is found in liquor in therapeutic concentration).

Vancomycinum gets through a placenta. It is allocated with breast milk.

At repeated introduction cumulation is possible.

At intake it is badly absorbed and usually does not get into a system blood stream. The defined plasma concentration of Vancomycinum can be noted in some cases at multiple dose inside at patients with the acute pseudomembranous colitis caused by Clostridium difficile.

Metabolism

Vancomycinum is practically not metabolized in an organism.

Removal

T1/2 at normal function of kidneys: adults are about 6 h (4-11 h), newborns are 6-10 h, babies are 4 h, children of more advanced age are 2-3 h.

75-90% of drug are removed by kidneys by passive filtering in the first 24 h.

In small and moderate amounts Vancomycinum can be removed with bile. In insignificant quantities it is removed at a hemodialysis or peritoneal dialysis.

Pharmacokinetics in special clinical cases

T1/2 at a chronic renal failure (an oliguria or an anury) at adults – 6-10 days.

At patients with one kidney it is removed slowly and the mechanism of removal is unknown.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to Vancomycinum:

— endocarditis;

— sepsis;

— meningitis;

— lower respiratory tract infections (pneumonia, lung abscess);

— infections of bones and joints (including osteomyelitis);

— infections of skin and soft tissues.

In the form of solution for intake:

— the pseudomembranous colitis caused by Clostridium difficile;

— the coloenteritis caused by Staphylococcus aureus.

Route of administration and doses:

Vancomycinum is entered in the form of slow into infusions with a speed no more than 10 mg/min. within not less than 60 min.

The drug cannot be administered in oil or in/in struyno.

Concentration of the prepared solution of Vancomycinum should not exceed 5 mg/ml.

The adult – on 0.5 g (7.5 mg/kg) each 6 h or on 1 g (15 mg/kg) each 12 h.

To children: to newborn children up to 7 days of life – an initial dose of 15 mg/kg of body weight, then - 10 mg/kg each 12 h; since 2nd week of life – on 10 mg/kg each 8 h; to children of 1 month is also more senior – on 10 mg/kg each 6 h.

Patients with disturbance of secretory function of kidneys need correction of the mode of dosing taking into account values of the clearance of creatinine (CC).

Correction can be carried out by increase in intervals between introductions, or by reduction of a single dose of drug:

Correction by increase in intervals between introductions

KK (ml/min.)                Vancomycinum Dose                 Interval between introductions
more than 80                                  1 g                                                  of 12 h
80-50                                       1                                                g 1-3 days
50-10                                       1                                                g 3-7 days
less than 10                                 1 g                                                of 7-14 days

Correction of a single dose
KK (ml/min.)                         Vancomycinum Dose (mg/)
                                                    100 1545
                                                      90 1390
                                                      80 1235
                                                      70 1080
                                                        60 925
                                                        50 770
                                                        40 620
                                                        30 465
                                                        20 310
                                                        10 155

This table cannot be applied to definition of a dose of drug at an anury. Such patients should appoint an initial dose of 15 mg/kg of body weight for bystry creation of therapeutic concentration of drug in serum. The dose necessary for maintenance of stable concentration of drug makes 1.9 mg/kg /

With the expressed renal failure it is reasonable to patient to enter maintenance doses of 250-1000 mg of 1 times in several days.

At an anury the dose of 1 g is recommended each 7-14 days.

When only concentration of creatinine in blood serum is known, for calculation of clearance of creatinine it is possible to use the formula given below:

For men:

KK = the body weight (kg) × (140 – age (years))/72 × concentration of creatinine in blood serum (mg/dl).

For women: the received result is multiplied on 0.85.

Preparation of solution for in/in introductions

Solution for injections is prepared just before administration of drug. For this purpose with dry, sterile drug a dosage of 0.5 g add 10 ml to a bottle, a dosage of 1 g – 20 ml of sterile water for injections (concentration of solution makes 50 mg/ml).

The prepared Vancomycinum solutions before introduction are subject to further cultivation to concentration no more than 5 mg/ml. The required dose of Vancomycinum divorced in the above-stated way should be entered in the way in/in infusions within not less than 60 min. As solvents it is possible to use 5% solution of a dextrose (glucose) for injections or 0.9% chloride sodium solution for injections: for 0.5 g – 100 ml and for 1 g – 200 ml.

Before an injection the prepared solution for parenteral administration should be checked visually if it is possible, for presence of mechanical impurities and discoloration.

The solutions prepared on the basis of 5% of solution of a dextrose (glucose) or 0.9% of solution of sodium of chloride can be stored in the refrigerator (2-8 °C) within 14 days without considerable loss of activity.

Preparation of solution for intake and its use

For treatment of the pseudomembranous colitis caused by Clostridium difficile owing to use of antibiotics, and also for treatment of a staphylococcal coloenteritis the drug Vankorus® is appointed inside.

Daily dose for adults – 0.5-2 g, divided into 3-4 receptions.

Daily dose for children – 40 mg/kg, divided into 3-4 receptions.

The maximum daily dose for adults and children – 2 g.

The corresponding single dose is dissolved in 30 ml of water and allowed the patient it to drink or entered via the probe. For improvement of taste of solution it is possible to add usual food syrups to it. Treatment duration - 7-10 days.

Features of use:

Drug is intended to use only in the conditions of a hospital.

At use of drug for babies and premature newborns it is regularly necessary to control concentration of Vancomycinum in a blood plasma.

It is necessary to administer the drug infusionally slowly (not less than 60 min.). Bystry introduction (for example, within several minutes) Vancomycinum can be followed by the expressed decrease in the ABP and in rare instances - a cardiac standstill.

Frequency of emergence and weight of thrombophlebitises can be reduced due to the correct cultivation of initial solution and alternation of injection sites of drug.

At prolonged use of Vancomycinum carrying out an audiogramma is necessary, to control a pattern of peripheral blood, function of kidneys (the general analysis of urine, indicators of creatinine and an urea nitrogen of blood).

It is desirable to define concentration of Vancomycinum in blood serum at a renal failure at patients 60 years as the high, remaining a long time concentration of Vancomycinum in blood can increase danger of manifestation of toxic effect of drug 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.

Side effects:

Post-infusional reactions (owing to bystry introduction): anaphylactoid reactions (decrease in the ABP, cardiac standstill, bronchospasm, диспноэ, skin rash, 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 in blood; intersticial nephrite.

From the alimentary system: nausea, pseudomembranous colitis.

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

From bodies of a hemopoiesis: reversible neutropenia, passing thrombocytopenia, agranulocytosis.

Allergic reactions: fever, 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.

Local reactions (at infusion violation of the rules): pain and a necrosis of fabrics in places of injections, phlebitis.

Interaction with other medicines:

At simultaneous in introduction of Vancomycinum and local anesthetics erythematic rashes and a hyperemia of integuments of the person can develop, adults have a disturbance of endocardiac conductivity.

At simultaneous and/or consecutive system or topical administration of other potentially ototoksichny and/or nefrotoksichny drugs (aminoglycosides, Amphotericinum In, aminosalicylic acid or other salicylates, капреомицин, кармустин, cyclosporine, "loopback" diuretics, including Acidum etacrynicum, polymyxin B, Cisplatinum) carrying out careful control of possible development of these symptoms is required.

Colestyraminum reduces activity of Vancomycinum at its intake.

Antihistamines, меклозин, fenotiazina, thioxanthenes can mask symptoms of ototoksichesky action of Vancomycinum (a sonitus, вертиго).

Pharmaceutical interaction

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 in/in system between uses of these antibiotics. Besides, it is recommended to reduce concentration of Vancomycinum to 5 mg/ml and less.

Contraindications:

— neuritis of an acoustical nerve;

— I trimester of pregnancy;

— period of a lactation (breastfeeding);

— hypersensitivity to Vancomycinum.

With care patients should use drug with the weakened hearing, a renal failure in view of possible development of ototoksichesky and nephrotoxic effects, to patients with an allergy on тейкопланин (a possibility of a cross allergy), pregnancy (II and the III trimester).

Use of the drug VANKORUS® at pregnancy and feeding by a breast

At pregnancy (II and the III trimester) drug is appointed only if the estimated advantage for mother surpasses potential risk for a fruit and only to lifelong indications.

Vancomycinum is allocated with breast milk. For treatment by drug it is necessary to stop breastfeeding.

Use at renal failures

Patients with disturbance of secretory function of kidneys need correction of the mode of dosing taking into account values of the clearance of creatinine (CC).

Correction can be carried out by increase in intervals between introductions, or by reduction of a single dose of drug:

Correction by increase in intervals between introductions

With the expressed renal failure it is reasonable to patient to enter maintenance doses of 250-1000 mg of 1 times in several days.

At an anury the dose of 1 g is recommended each 7-14 days.

When only concentration of creatinine in blood serum is known, for calculation of clearance of creatinine it is possible to use the formula given below:

For men:

KK = the body weight (kg) x (140 – age (years)),
72 x a kontsenration of creatinine in blood serum (mg/dl).

For women: the received result is multiplied on 0.85.

Use for elderly patients

It is desirable to define concentration of Vancomycinum in blood serum at a renal failure at patients 60 years as the high, remaining a long time concentration of drug in blood can increase danger of manifestation of toxic effect of drug 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.

Use for children

At use of drug for babies and premature newborns it is regularly necessary to control concentration of Vancomycinum in a blood plasma.

Overdose:

Symptoms: strengthening of expressiveness of by-effects from an urinary system and sense bodys.

Treatment: carry out symptomatic therapy. Administration of liquid and control of plasma concentration of Vancomycinum is recommended. For bystry removal of surplus of Vancomycinum from an organism haemo filtering is more effective, than a hemodialysis.

Storage conditions:

List B. Drug should be stored in the unavailable to children, dry, protected from light place at a temperature not above 25 °C. A period of validity - 2 years.