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The antibiotic glycopeptide produced by Amycolatopsis orientalis has a bactericidal effect on most microorganisms (on Enterococcus spp. - bacteriostatic). Blocks the synthesis of the bacterial cell wall in a site different from that on which penicillins and cephalosporins act (does not compete with them for binding sites), firmly binding to D-alanyl-D-alanine residues of peptidoglycan subunits - the main component of the cell wall, which leads to cell lysis.
Active against gram-positive microorganisms: Staphylococcus spp. (including penicillinase-forming and methicillin-resistant strains), Streptococcus spp., Streptococcus pneumoniae (including penicillin-resistant strains), Corynebacterium spp., Enterococcus spp., Clostridium spp., Actinomyces spp.
The optimum effect is at pH 8, with a decrease in pH to 6, the effect decreases sharply. Actively acts only on microorganisms that are in the multiplying stage.
Almost all gram-negative bacteria, Mycobacterium spp., Fungi, viruses, protozoa are resistant. Has no cross-resistance with other antibiotics.
Poorly absorbed when taken orally. With intraperitoneal administration, systemic absorption of up to 60% is possible (when administered at a dose of 30 mg / kg, the plasma concentration is about 10 mg / kg). About 60% of the dose is absorbed after 6 hours. The connection with plasma proteins is 55%.
After intravenous administration, the volume of distribution is 0.39-0.92 l / kg. Cmax 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 μg / ml after 60 minutes and 23-30 μg / ml after 1-2 hours.
Therapeutic concentrations are determined in ascitic, synovial, pleural and pericardial fluids, in peritoneal dialysate fluid, in urine, and atrial appendage tissue. Does not penetrate the BBB (with meningitis, it is found in the cerebrospinal fluid in therapeutic concentrations).
Penetrates the placenta. Excreted in breast milk. Practically not metabolized.
T1 / 2 with normal renal function: adults - about 6 hours (4-11 hours), newborns - 6-10 hours, infants - 4 hours, older children - 2-3 hours; T1 / 2 with 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 removed or absent kidney, it is excreted slowly and the mechanism of excretion is unknown.
In small and moderate amounts, it can be excreted in the bile. In small quantities, it is excreted during hemodialysis or peritoneal dialysis.
Sepsis, endocarditis, pneumonia, lung abscess, infections of bones and joints (including osteomyelitis), meningitis, pseudomembranous colitis caused by Clostridium difficile, enterocolitis, skin infections.
Hypersensitivity, lactation, auditory neuritis.
Carefully. Hearing impairment (including history), renal failure, pregnancy.
Postinfusion reactions (due to rapid administration): anaphylactoid reactions (decreased blood pressure, bronchospasm, shortness of breath, skin rash, itching), red man syndrome associated with the release of histamine (chills, fever, heart palpitations, hyperemia of the upper half of the trunk and face, spasm muscles of the chest and back).
From the urinary system: nephrotoxicity (up to the development of renal failure) 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. Rarely - interstitial nephritis.
From the digestive system: nausea, pseudomembranous colitis.
From the senses: ototoxicity - hearing loss, vertigo, ringing in the ears.
From the side of hematopoiesis: reversible neutropenia, transient thrombocytopenia, rarely - agranulocytosis.
Local reactions (in case of violation of the rules of infusion): phlebitis, pain at the injection site, tissue necrosis at the injection site.
Allergic reactions: fever, nausea, chills, eosinophilia, rash (including exfoliative dermatitis), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), vasculitis.
With the simultaneous appointment with local anesthetics, children may experience erythematous rashes and hyperemia of the skin of the face, in adults - a violation of intracardiac conduction.
Simultaneous administration with nephro- and ototoxic drugs (aminoglycosides, amphotericin B, ASA or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, cyclosporin, "loop" diuretics, polymyxin B, cisplatin, ethacrynic acid) is not recommended.
Cholestyramine reduces efficacy.
Antihistamines, meclosine, phenothiazines, thioxanthenes can mask the symptoms of the ototoxic effect of vancomycin (tinnitus, vertigo).
General anesthetics and vecuronium bromide - the risk of lowering blood pressure or developing neuromuscular blockade. Vancomycin can be infused at least 60 minutes before administration.
Only i / v (i / m injections are painful) at a rate of no more than 10 mg / min; the duration of the 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 - 15 mg / kg, and then 10 mg / kg every 12 hours; in children aged 1 month, use 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, the initial dose is 15 mg / kg, then the dosage regimen is adjusted taking into account the CC values (with uremia, the interval between injections is up to 10 days): with CC more than 80 ml / min - the usual dose, CC 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.
The creatinine clearance can be calculated using 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.
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 diluted with 0.9% NaCl solution or 5% dextrose solution: for 500 mg - 100 ml and for 1 g - 200 ml.
With pseudomembranous colitis - inside, in the form of a solution in 30 ml of water: adults - 0.5-2 g divided into 3-4 doses, children - 0.04 g / kg divided into 3-4 doses, no more than 2 g per day. The duration of treatment is 7-10 days.
Symptoms: increased severity of side effects.
Treatment: symptomatic, in combination with hemoperfusion and hemofiltration.
Application in the II-III trimester of pregnancy is possible only for "vital" indications.
When administered to premature and normal infants, monitoring of serum concentrations is desirable.
When taken simultaneously with general anesthetics, the incidence of side effects increases, so vancomycin is best administered before general anesthesia.
During the treatment period, it is necessary to conduct an audiogram, determine the function of the kidneys (urinalysis, creatinine and urea nitrogen).
It is desirable to determine the concentration of vancomycin in the blood serum (with renal failure, in patients over 60 years of age).
The maximum concentration should not exceed 40 μg / ml, and the minimum - 10 μg / ml. Concentrations over 80 μg / ml are considered toxic.
The drug should be stored in a dry, dark place, out of the reach of children, at a temperature not exceeding 8 ° C.
|The purpose of the medication||Antibacterial|