The antibacterial agent, produced by Amycolatopsis orientalis, bactericidal effect on the majority of microorganisms (enterococci on -bakteriostaticheski). Blocks the synthesis of the bacterial cell wall in the area other than the one on which there are penicillins and cephalosporins (not compete with them for binding sites), firmly contacting the D-alanyl-D-alanine precursor part of the cell wall, which leads to cell lysis. Able also change the permeability of cell membranes of bacteria and selectively inhibit the synthesis of RNA. It is active against Gram-positive microorganisms: of Staphylococcus spp. (including methicillin-resistant strains and penitsillinazoobrazuyuschie), Streptococcus spp., Streptococcus pneumoniae ( including strains resistant to penicillin), Corynebacterium spp., Enterococcus spp., Clostridium spp., Actinomyces spp . Optimum action – at pH 8, by lowering the pH to 6 effect decreases sharply. It is active only on microorganisms which are in the stage of reproduction. Resistant almost all Gram-negative bacteria, Mycobacterium spp., Fungi, viruses, protozoa. It does not cross-resistant with other antibiotics.. Faumakokinetika maximum concentration (C max ) after intravenous infusion of 500 mg – 49 mg / ml at 30 min and 20 mg / kg every 1-2 hours; after intravenous infusion of 1 g – 63 ug / ml in 60 minutes and 23-30 ug / ml in; 1-2 hours. The connection to plasma proteins -. 55% Therapeutic concentrations are determined in the ascites, synovial, pleural, pericardial and peritoneal fluids, urine, tissue atrial appendage. It does not cross the intact blood-brain barrier (in meningitis is detected in the CSF in therapeutic concentrations). It crosses the placenta. Provided with breast milk. Practically not metabolized. The half-life (T ½ ) with normal renal function: Adults-about 6 hours (4-11 hours), newborns – 6-10 hours, infants -4 hours, older children – 2-3 hours; T ½ in chronic renal failure (oliguria or anuria) in adults – 6-10 days. Repeated administration of accumulation is possible, 75-90% of the drug is excreted by the kidneys by a passive filter in the first 24 hours; in patients with distant or absent kidneys remove slowly and removal mechanism is unknown. In small to moderate amounts can be excreted in bile. In small amounts appear in hemodialysis or peritoneal dialysis.
Sepsis; endocarditis; meningitis; infections of the lower respiratory tract (pneumonia, lung abscess); bone and joint infections (including osteomyelitis); pseudomembranous colitis (not associated with the use of antibiotics), caused by Clostridium difficile, enterocolitis; skin and soft tissue infections.
Hypersensitivity, pregnancy (I trimester), lactation, neuritis of the auditory nerve. Precautions: hearing loss (including history), renal failure, pregnancy (II-III trimesters).
Dosing and Administration
only intravenously, the recommended concentration is not more than 5 mg / ml with the introduction of a speed of no more than 10 mg / min; infusion duration should not be less than 60 minutes.
Adults – 0.5 g or 7.5 mg / kg every 6 hours or 1 g or 15 mg / kg every 12 hours.
newborns during the first week of life – an initial dose of 15 mg / kg followed by 10 mg / kg every 12 hours; starting from the 2nd week of life 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 of the initial dose -15 mg / kg, the dosing regimen further correcting considering creatinine clearance values (in anuria interval between injections – up to 10 days) in creatinine clearance greater than 80 mL / min – the usual dose when creatinine clearance of 50-80 ml / min – 1 g each 1-3 days, 10-50 ml / min – 1 g every 3-7 days, less than 10 ml / min – 1 g every 7-14 days (creatinine clearance can be calculated by the formula: for men: body weight (kg) × (140 – age (years) / 72 × serum creatinine concentration (mg / dL) women – the result is multiplied by 0.85).Preparation of solution: The powder is dissolved in water for injection: 500 mg – 10 ml 1 g -. 20 ml (solution concentration of 50 mg / mL) The resulting solution was subject to further dilution of 0.9% sodium chloride or 5% dextrose to a concentration of less than 5 mg / ml (for the 500 mg – 100 ml and 1 g – 200 mL). The prepared solution was used immediately. Preparation of the solution for the reception inside:winstrol results may be used orally for the treatment of pseudomembranous colitis caused by Clostridium difficile, and staphylococcal enterocolitis. The appropriate dose is prepared in 30 ml of water: adults – 0.5-2 g 3-4 times, children – 0.04 g / kg of 3 – 4 times. The duration of the treatment – 7 – 10 days.
Side effects Postinfuzionnye reaction (due to the rapid introduction): anaphylactoid reactions (lowering blood pressure, bronchospasm, dyspnea, skin rash, itching), the syndrome of “red man”, associated with the release of histamine (chills, fever, heart palpitations, flushing of the upper body and face, spasm of the muscles of the chest and back). from the urinary system: renal toxicity (up to the development of renal failure) usually when combined with aminoglycosides or the appointment of more than 3 weeks in high concentrations, is manifested by increased serum creatinine and urea nitrogen concentrations.Rarely, interstitial nephritis. From the side of gastrointestinal tract: nausea, pseudomembranous colitis. From the senses: ototoxicity – hearing loss, vertigo, ringing in the ears. From the side of hematopoiesis: reversible neytropenyya, transient thrombocytopenia, rarely – agranulocytosis. Allergic reactions : fever, nausea, chills, eosinophilia, rashes (including exfoliative dermatitis), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), vasculitis. Local reactions: phlebitis, pain and tissue necrosis at the injection site.
Overdosing Symptoms: increased severity of side effects. Treatment: symptomatic, in combination with hemoperfusion and hemofiltration.
Interaction with other drugs
When concomitant administration of winstrol results with local anesthetics in children may appear erythematous rash and flushing of the skin face, in adults – a violation of intracardiac conduction.
Co-administration with nephrotoxicity and ototoxic drugs (aminoglycosides, amphotericin B, or acetylsalicylic acid, etc. . salicylate, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, cyclosporine, “loop” diuretics, polymyxin B, cisplatin, ethacrynic acid) requires careful monitoring for possible development of these symptoms. Kolestiramin reduces efficiency. Antihistamine drugs meklozin, phenothiazines, thioxanthenes may mask symptoms Valium actions winstrol results (tinnitus, vertigo). General anesthetics and vecuronium bromide – the risk of reduction in blood pressure or development of neuromuscular blockade. Infusion of winstrol results can be at least 60 minutes before their introduction. A solution of winstrol results has a low pH, which may cause physical or chemical instability when mixed with other solutions. It should not be mixed with alkaline solutions.
Application in II-III trimester of pregnancy is possible only by “real life” testimony. In appointing premature and newborn desired control of the concentration in the blood serum of the drug.
In simultaneous reception with general anesthetics increase the frequency of side effects, so winstrol results is best administered before general anesthesia.
The treatment period is necessary to conduct the audiogram, the determination of renal function (urinalysis, creatinine, and urea nitrogen).
It is advisable to determine the concentration of winstrol results in the blood serum (in renal failure, in patients older than 60 years). The maximum concentration should not exceed 40 mg / mL, and the minimum – 10 mcg / mL. Concentrations above 80 mg / ml are considered toxic.
Likelihood of local reactions may be reduced due to the slow introduction of dilute solutions (2.5 – 5 g / l) and alternation injection sites.