Anadrol is a tricyclic glycopeptide antibiotic produced by Amycolatopsis orientalis, bactericidal effect on most of the microorganisms (in enterococci – bacteriostatic). 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. It is also able to modify the permeability of cell membranes of bacteria and selectively inhibit the synthesis of RNA.
It is active against gram-positive bacteria, including: Staphylococcus aureus and Staphylococcus epidermidis (including methicillin-resistant heterogeneous strains), Streptococcus spp, Enterococcus spp. . (including Enterococcus faecalis), Clostridium spp. (including Clostridium difficile). For in vitro anadrol sensitive Listeria monocytogenes, bacteria genera Lactobacillus, Actinomyces, Bacillus.
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. The oral route has no systemic action, acts locally on the sensitive microflora in the gastrointestinal tract (Staphylococcus aureus, Clostridium difficile).
The maximum concentration (Cmax) after intravenous infusion of 500 mg – 49 mg / ml at 30 min and 20 mg / ml in 1-2 hours; After intravenous infusion of 1 g -63 pg / ml after 60 minutes and 23-30 ug / ml in 1-2 hours Connection with the plasma protein -.. 55%
Therapeutic concentrations are determined in the ascites, synovial, pleural, pericardial and peritoneal fluids in urine, tissue atrial appendage. It does not cross the intact blood-brain barrier (in meningitis is detected in the CSF in therapeutic concentrations). anadrol crosses the placenta. Provided with breast milk.
The half-life (the T 1/2 ) with normal renal function: Adults – about 6 hours (4-11 hours), newborns – 6-10 hours, infants – 4 hours, older children – 2 3 h; The T l / 2 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.
Poor adsorbed by ingestion and typically does not penetrate into the systemic circulation.
Defined plasma concentrations of anadrol may be celebrated in some cases with repeated oral route in patients with acute pseudomembranous colitis caused by Cl. difficile.
Infectious-inflammatory diseases, caused by susceptible microorganisms:
• lower respiratory tract infections (pneumonia, lung abscess)
• bone and joint infections (including osteomyelitis)
• Skin and soft tissue infections For intake: • pseudomembranous colitis caused by difficile-of Clostridium • enterocolitis caused by Staphylococcus aureus
Hypersensitivity to anadrol, pregnancy (I trimester), lactation, neuritis of the auditory nerve.
Precautions: hearing loss (including history), renal failure, pregnancy (II and III trimesters).
Dosing and Administration
recommended concentration – no more than 5 mg / ml at a rate of administration is not more than 10 mg / min; infusion duration should not be less than 60 minutes. Adults 500 mg, or 7.5 mg / kg every 6 hours or 15 mg or 1000 mg / kg every 12 hours. Babies: newborns during the first week of life – an initial dose of 15 mg / kg, and then 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 h In patients with impaired renal excretory function requires correction dosing regimen based on the values of creatinine clearance (CC). Correction can be made by increasing the intervals between doses of anadrol Vero or by reducing single dose: Correction by increasing intervals between administrations: When QA 80 ml / min – a conventional dosing regimen in QA 50-80 ml / min – 1000 mg every . 1-3 days at 10-50 QC ml / min – 1000 mg every 3-7 days, CC than 10 ml / min – 1000 mg every 7-14 days correction unit dose:
|Creatinine clearance (ml / min)
|anadrol dose (mg / 24 hours)
Patients with anuria should appoint Vero anadrol in the initial dose of 15 mg / kg for the quick creation of a therapeutic serum concentration of the drug. The dose required to maintain stable concentrations is 1.9 mg / kg per day.
Patients with severe renal dysfunction is better administered by maintenance doses of 250-1000 mg I time in a few days than in the daily chart. At the anuria recommend 1000 mg administered every 7-14 days.
Once known only to the concentration of serum creatinine to calculate creatinine clearance can be used the following formula:
for men – [body weight (kg) x (140 – age (years)] . / [72 x concentration in serum creatinine (mg / dl)], for women – the result is multiplied by 0.85 . Preparation rastvoora lyophilizate 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 solution to the sodium concentration of less than 5 mg / ml (for the 500 mg – 100 ml for 1 g – 200 mL). . solutions were prepared on the basis of 0.9% sodium chloride or 5% dextrose may be stored in a refrigerator (2-8 ° C) for 14 days without significant loss of activity.
Application inside with pseudomembranous colitis, staphylococcal enterocolitis:
A daily dose for adults – 500-2000 mg divided by 3-4 hours; for children – 40 mg / kg, divided into 3-4 hours. The maximum daily dose for adults and children -. 2000 mg
. Duration of treatment is 7-10 days
Oral solution is prepared by dissolving the appropriate dose of the lyophilizate in 30 ml of water.
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, muscle spasm 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 concentration; . 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 neutropenia, transient thrombocytopenia, agranulocytosis. Allergic reactions: fever, 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 sites.
Symptoms: increased severity of side effects.
Treatment: symptoms, coupled with and hemoperfusion hemofiltration.
Interaction with other drugs
In an intravenous administration of anadrol 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, acetylsalicylic acid or other salicylates, bacitracin, bumetanide, capreomycin, carmustine, paromomycin, cyclosporine, loop diuretics, polymyxin B, cisplatin, ethacrynic acid) requires careful monitoring of the possible development of these symptoms.
Kolestiramin reduces activity (oral).
General anesthetics and vecuronium bromide – the risk of lowering blood pressure or development of neuro – muscular blockade. Infusion of anadrol can be at least 60 minutes prior to their introduction.
Antihistamines, meklozin, phenothiazines, thioxanthenes may mask symptoms Valium actions anadrol (tinnitus, vertigo).
The solution anadrol has a low pH that 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 anadrol should be administered prior to general anesthesia.
It is advisable to determine the serum concentrations of anadrol (in renal failure, in patients older than 60 years). The maximum concentration should not exceed 40 mg / mL, and the minimum – 10 pg / ml; concentration above 80 ug / ml are considered toxic. For patients with renal insufficiency dose of anadrol should be individualized.
The likelihood of local reactions may be reduced due to the slow introduction of the diluted solution (2.5-5 g / l) and the alternation of the injection site.