Vancorus

Vancorus is an antimicrobial systemic drug. It belongs to the category of glycopeptide antibiotics.

Indications Vancorus

It is used for bacterial infections that occur in a severe form and are caused by microbes that are sensitive to the drug (also in case of bacterial resistance to cephalosporins with penicillins or in case of patient hypersensitivity to these drugs):

• sepsis with endocarditis;
• pneumonia and pulmonary abscess;
• osteomyelitis or enterocolitis with meningitis.

Release form

Released as a lyophilisate used in the manufacture of infusion solutions, in vials of 500 or 1000 mg. Inside the pack is 1 vial with powder.

Pharmacodynamics

Vancomycin is an antibiotic produced by Amycolatopisorientalis. It has a bactericidal effect and prevents the binding of drug-sensitive microbial cell walls.

It has an effective effect on gram-positive bacteria: staphylococci (including penicillinase-producing and methicillin-resistant microbial strains), streptococci (including penicillin-resistant strains), and also clostridia and corynebacteria.

Almost all gram-negative microbes, as well as viruses, fungi and protozoa, are resistant to the drug. The drug does not have cross-resistance with other antibiotics.

Pharmacokinetics

The peak value with intravenous infusion of 500 mg of the drug is 49 mcg/ml half an hour after administration and 20 mcg/kg after 1-2 hours. With intravenous infusion of 1 g of the drug, this value reaches 63 mcg/ml after 1 hour, and also up to 23-30 mcg/ml after 1-2 hours. The synthesis rate with plasma protein is 55%.

The medicinal level of the substance is observed in the pericardial, pleural, peritoneal and serous fluid, as well as in the synovium, atrial appendage tissues and urine. The component does not pass through intact BBB (but in meningitis it can penetrate into the cerebrospinal fluid in medicinal concentrations). In addition, the component is able to pass through the placental barrier. It is excreted into mother's milk. It is almost not metabolized.

The half-life with healthy kidney function is:

• approximately 6 hours (range 4-11 hours) in adults;
• 6-10 hours in newborns;
• 4 hours for infants;
• 2-3 hours for older children.

The same indicator for chronic kidney failure is 6-10 days in an adult.

In case of repeated use of the solution, cumulation may occur.

About 75-90% of the substance is excreted via the kidneys by powerful filtration during the first 24 hours. In people with missing or removed kidneys, excretion is slow, and the mechanism of this process is not determined. Moderate or small amounts of the substance may be excreted in bile. A small part of the component is excreted by peritoneal dialysis or hemodialysis.

Dosing and administration

The solution is administered exclusively by the intravenous method. The optimal concentration is a maximum of 5 mg/ml (the infusion rate of the solution is a maximum of 10 mg/minute). The duration of the procedure should not exceed 1 hour.

The adult dose is 0.5 g or 7.5 mg/kg every 6 hours or 1 g or 15 mg/kg every 12 hours.

For newborns in the first week of life, the initial dosage is 15 mg/kg, and then 10 mg/kg every 12 hours. Starting from the second week, the same dosage must be administered every 8 hours. Children from the age of 1 month should be administered 10 mg/kg of the drug every 6 hours or 20 mg/kg every 12 hours.

For individuals with renal excretory function disorders, the initial dose is 15 mg/kg, after which the regimen is adjusted depending on the CC indicators (in case of anuria, the intervals between procedures are up to 10 days):

• the CC level is more than 80 ml/minute – a standard dose is administered;
• the CC indicator is within 50-80 ml/minute – 1 g at intervals of 1-3 days;
• the CC rate is within 10-50 ml/minute – administer 1 g at intervals of 3-7 days;
• CC level less than 10 ml/minute – 1 g at intervals of 1-2 weeks.

Preparation of infusion solution:

The powder must be dissolved in injection water in the following proportion: 10 ml of water is required for 500 mg of the drug; 20 ml of water for 1 g of the drug (the solution concentration is 50 mg/ml). This mixture is then diluted with a solution of sodium chloride (0.9%) or dextrose (5%) until a maximum concentration of 5 mg/ml is obtained (proportions: 100 ml for 500 mg, 200 ml for 1 g). The prepared solution must be used immediately.

Preparation of oral solution:

Vancomycin is allowed to be used orally (to eliminate pseudomembranous colitis caused by Clostridium difficile, as well as staphylococcal food poisoning). The required dose should be prepared in 30 ml of water. Adults should take 0.5-2 g of the substance 3-4 times a day, and children - 0.04 g / kg in the same frequency.

The duration of the therapeutic course is within 7-10 days.

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Use Vancorus during pregnancy

In the 1st trimester the drug is prohibited, but in the 2nd and 3rd it can be used with caution.

Contraindications

Contraindications include hypersensitivity to the drug, breastfeeding, and cochlear neuritis.

Caution is required in case of renal failure and hearing disorders (also if present in the anamnesis).

Side effects Vancorus

The following side effects may develop due to the use of the drug:

• post-infusion manifestations (due to rapid administration of the infusion): anaphylactoid symptoms (such as bronchospasms, decreased blood pressure, itching, skin rashes and shortness of breath) and red neck syndrome, which occurs due to the release of the substance histamine. It manifests itself in the form of a state of fever, chills, muscle spasms in the back and chest area, as well as increased heart rate and hyperemia in the face and upper body;
• disorders in the urinary system: development of nephrotoxicity (reaching renal failure), which occurs mainly when combining drugs with aminoglycoside antibiotics or as a result of the administration of large doses for a period of more than 3 weeks. The disorder manifests itself as an increase in the level of urea nitrogen, as well as creatinine. Occasionally, tubulointerstitial nephritis appears;
• gastrointestinal disorders: development of pseudomembranous colitis or nausea;
• reactions of the senses: the appearance of ototoxicity - hearing loss, tinnitus and vertigo;
• disorders of the hematopoietic system: treatable neutropenia or temporary thrombocytopenia; agranulocytosis occasionally occurs;
• allergic manifestations: the appearance of nausea, fever and chills, and along with this, rashes (this includes the exfoliative form of dermatitis), eosinophilia, Stevens-Johnson syndrome, as well as Lyell's syndrome, and in addition, vasculitis;
• local disturbances: phlebitis, pain or tissue death at the injection site.

Overdose

In case of overdose, side effects develop to a more severe degree.

To eliminate the disorders, symptomatic therapy is necessary together with hemofiltration and hemoperfusion procedures.

Interactions with other drugs

In case of combined use of the drug and local anesthetics in children, erythematous rash or hyperemia of the skin on the face may occur. In adults, intracardiac conduction block develops.

Combination with ototoxic or nephrotoxic drugs (such as carmustine with aminoglycosides, aspirin and other salicylates, as well as amphotericin B and capreomycin with bumetanide and bacitracin, cisplatin with cyclosporine, paromomycin, loop diuretics and polymyxin B with ethacrynic acid) requires constant monitoring for possible occurrence of symptoms of the disorder.

Cholestyramine weakens the effect of vancomycin.

Meclizine and thioxanthenes with antihistamines and phenothiazines can mask the signs of ototoxic effects of the drug (vertigo and tinnitus).

Systemic anesthetics with vecuronium bromide may cause a decrease in blood pressure or blockade of neuromuscular transmission. The infusion may be administered at least 1 hour before the use of the above drugs.

The drug solution has a weak pH value, which may cause chemical or physical instability when mixed with other drug solutions. Do not combine with alkaline solutions.

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Storage conditions

Vancorus should be stored in a dark place, protected from moisture. Keep away from small children. Temperature level – no more than 25°C.

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Shelf life

Vancorus is suitable for use for a period of 2 years from the date of production of the powder.