“Vancomycin” from the group of glycopeptide antibiotics. It is capable of exerting a bactericidal effect, deforms the synthesis of cell walls and bacterial RNA, and the permeability of the membrane of the cytoplasm. It is active against gram-positive bacteria: Staphylococcus spp. (including strains that produce penicillinase, as well as methicillin-resistant strains), Enterococcus spp., Listeria spp., Streptococcus spp., Actinomyces spp., Corynebacterium spp, Clostridium spp. (including Clostridium difficile). No cross-resistance was detected with antibiotics of other groups.
Structure
The composition of “Vancomycin” from the group of glycopeptide antibiotics contains vancomycin proper, which is present here in hydrochloride form, as well as excipients.
Effect from the standpoint of pharmacokinetics
After Vancomycin is taken orally, it is absorbed in very small amounts. A slight increase in the absorption of the drug is observed with inflammation of the intestinal mucosa. In this case, after using the drug in an amount of 500 milligrams every six hours in the blood plasma, the active substance reaches a maximum concentration in the range from 2.4 to 3 mg / l.
If the same amount of the drug is administered intravenously, then in patients with normal kidney function, the highest content will be approximately 7.3 mg / L. With the intravenous administration of “Vancomycin” in the amount of 1000 milligrams, its concentration in the blood plasma doubles. Immediately after infusion, this indicator will range from 20 to 50 mg / l, and after twelve hours - from 5 to 10. After intravenous administration of 500 milligrams per hour, the average plasma concentration at the end of the infusion is approximately 33 mg / l, after an hour - 7.3 mg / l, after four hours, this figure is 5.7 mg / l.
If you enter repeatedly “Vancomycin” from the group of glycopeptide antibiotics repeatedly, then its content will be similar to a single use. Distribution volume varies from 0.2 to 1.25 l / kg. If we talk about children, including also newborns, then this indicator is slightly lower in comparison with adults: 0.53 - 0.82.
According to the results of ultrafiltration, it can be seen that when the content of “Vancomycin” in the blood serum is in an amount of 10 to 100 mg / l, it binds to plasma proteins by 30-55%. With intravenous administration, the active substance is found in various tissues of the body (kidneys, vascular walls, liver, abscess walls, heart, atrial ear tissue, lungs), in fluids (pleural, ascitic, pericardial, synovial, peritoneal), in urine (in inhibitory increased sensitivity of microorganisms concentration).
It has been noticed that Vancomycin, from the group of glycopeptide antibiotics, slowly penetrates into the fluid of the spinal cord, but with inflammation of its membranes, a directly proportional increase in the speed of the drug through the blood-brain barrier is recorded.
The antibiotic crosses the placental barrier and, accordingly, passes into breast milk.
Means “Vancomycin” (photo) from the group of glycopeptide antibiotics are almost not metabolized. If the functioning of the kidneys is normal, then on average the half-life of it from plasma ranges from 4 to 6 hours. About 75 percent of the dose in the first 24 hours is excreted by the kidneys through glomerular filtration. But excretion with bile is observed in a small amount. The same thing with hemodialysis or peritoneal dialysis.
The average plasma clearance is approximately 0.058 l / kg / h, and the kidney clearance is 0.048. After permanent renal clearance, Vancomycin is excreted by 70 - 80 percent. If impaired renal activity is observed, this process slows down. During anuria, the average half-life is 7.5 days. Due to glomerular filtration, slowed down by natural causes in elderly patients, in general, the systemic and renal clearance of Vancomycin may decrease.
Indications
As indications for the use of “Vancomycin” from the group of glycopeptide antibiotics are infectious and inflammatory diseases characterized by a severe course and caused by pathogens sensitive to the active substance of the drug (with intolerance or treatment failure with other antibiotics, which also include cephalosporins or penicillins):
- endocarditis (as monotherapy or part of a combination type of antibiotic therapy);
- sepsis;
- lung abscess;
- skin infections;
- pneumonia;
- soft tissue infections;
- pseudomembranous colitis provoked by Clostridium difficile ;
- meningitis.
The main forms of release
Vancomycin has the following forms:
- the powder from which the solution for infusion is prepared (i.e. injections in the form of ampoules for injection) in an amount of 500 milligrams and 1 gram;
- lyophilisate for the manufacture of a solution in the same volume.
Other dosage forms, including also suspensions or tablets, do not exist.
This is confirmed by the instructions for use of “Vancomycin” from the group of glycopeptide antibiotics.
Dosage
The drug is administered intravenously through a dropper. For adults, the dosage is 500 milligrams, applied every six hours, or 1 gram every 12 hours. To avoid collaptoid reactions, the infusion should last at least 60 minutes. The dose for children is 40 milligrams per kilogram per day, each administered over an hour. In patients with impaired renal function of excretion, it, accordingly, decreases based on the indicators of QC.
Also, depending on the etiology of the disease, Vancomycin is allowed to be ingested. The daily norm for adults varies from 500 milligrams to 2 grams in three to four doses, the dose for children is 40 milligrams per kilogram with the same number of doses. With intravenous administration to adult patients, 3-4 grams are maximally acceptable.
Side effect
Side effects from the use of “Vancomycin” from the group of glycopeptide antibiotics are:
- heart failure;
- decrease in blood pressure;
- tides;
- shock (these symptoms are mainly due to the rapid infusion of the drug);
- eosinophilia;
- neutropenia;
- nausea;
- agranulocytosis;
- thrombocytopenia;
- deformation of functional tests of the kidneys;
- interstitial nephritis;
- impaired renal activity;
- tinnitus;
- vertigo;
- exfoliative dermatitis;
- itchy dermatosis;
- ototoxic effects;
- Stevens-Johnson syndrome;
- bubbly benign dermatosis;
- vasculitis;
- hives;
- rash;
- epidermal necrolysis of a toxic nature;
- anaphylactoid type reactions;
- drug fever;
- chills;
- tissue necrosis in the places where the injection was injected, and pain in these areas;
- thrombophlebitis;
- erythema;
- the appearance of red neck syndrome, which is due to the release of histamine;
- skin rash;
- redness of the neck, face, hands and upper body;
- palpitations;
- vomiting
- nausea;
- temperature rise;
- chills;
- fainting.
Contraindications
Among the contraindications to the use of Vancomycin are:
- apparent impaired renal function;
- auditory nerve neuritis;
- first trimester of pregnancy;
- lactation period;
- hypersensitivity of the patient to vancomycin - the active substance of the drug.
What is the use of Vancomycin from the group of glycopeptide antibiotics by pregnant women and nursing mothers?
Due to the fact that ototoxicity and nephrotoxicity may develop, it is forbidden to use the drug in the first trimester of pregnancy. In the second and third trimester, “Vanzomycin” can be used only if there are vital indications. If necessary, you should complete breastfeeding.
Treatment for children and the elderly
If you use the drug for newborns, you need to carefully monitor the concentration of "Vancomycin" in the blood plasma. The same applies to elderly patients.
note
"Vancomycin" must be used carefully for impaired renal activity of mild to moderate degrees, hearing impairment (including a history of). During the therapeutic period, patients with kidney disease and / or defects in the eighth pair of cranial nerves require monitoring of renal function and hearing. Intramuscular administration of the drug is prohibited due to the high risk of tissue necrosis.
Drug interaction
The use of “Vancomycin” along with some drugs can cause a number of negative reactions:
- when combined with cisplatin, polymyxins, amphotericin and diuretics, kidneys and hearing organs are at risk;
- with simultaneous use with phenobarbital, a group of corticosteroids and heparin;
- when taken with anesthetics in children, cutaneous erythema with dilated capillaries in the face area was detected; in adults, the appearance of heart rhythm defects and blockade;
- colestyramine reduces effectiveness.
- it is necessary to avoid the combination of the drug with antibiotics related to the beta-lactam type.
In the treatment of premature babies, it is necessary to monitor the concentration of the drug in the blood serum. During the treatment period, the doctor prescribes a kidney diagnosis and a hearing examination.
Reviews on "Vancomycin" from the group of glycopeptide antibiotics
The patient reviews say that this drug is a powerful antibiotic, as a result of which it can only be used under strict medical supervision. In addition, many note the development of serious side effects, such as difficulty breathing, low blood pressure, ear pain and redness of the skin.
Analogs of Vancomycin from the group of glycopeptide antibiotics should be selected by a doctor.
Analogs
Structural analogues of the active substance can be identified as follows:
- "Vancoled";
- Vancomabol;
- Vancomycin J;
- “Vancomycin Teva”;
- “Vancomycin hydrochloride”;
- "Vankorus";
- "Vankotsin";
- Vanmixan
- Vero Vancomycin;
- Edicin.
We provided information on the Vancomycin preparation from the group of glycopeptide antibiotics. But remember that the appointment of any medication should be done by a specialist! Be healthy!