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omnadren cycle

Pharmacodynamics: omnadren cycle is a synthetic monocyclic beta-lactam antibiotic for parenteral use. Structurally different from other beta-lactam antibiotics (such as penicillins, cephalosporins); core molecule is alpha-methyl-3-amino-mono-baktamnaya acid. Effective bactericidal: binds to transpeptidase and violates the final stages of bacterial cell wall synthesis. It has high affinity for penicillin-binding protein 3. High stability to beta-lactamases (including penicillinases and cephalosporinase) Gram-negative bacteria. A potent and specific activity in vitro against gram-negative aerobic pathogens includingPseudomonas aeruginosa . The bactericidal effect is manifested in a wide pH range and under anaerobic conditions. It is active against the following microorganisms, both in vitro , and in vivo : Citrobacter spp. , Including S. freundii, Enterobacter spp. , including E. cloacae, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant and others. penitsillinazoprodutsiruyuschie strains), Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia spr., including S. marcescens. The following strains were susceptible in vitro , however, the clinical implications of these findings is unknown: the Aeromonas hydrophila, Morganella morganii, of Neisseria gonorrhoeae (including penitsillinazoprodutsiruyuschie strains), of Pasteurella multocida, the Proteus vulgaris, Providencia stuartii, Providencia rettgeri, of Yersinia enterocolitica . Resistant to Aztreabolu ® : aerobic gram-positive cocci and bacteria, of Acinetobacter spp. , Anaerobic bacteria, Mycoplasma and other intracellular pathogens, of Mycobacterium spp. Is possible to use Aztreabola ® if you are allergic to penicillins, cephalosporins and carbapenems. Rarely causes goiter.

Pharmacokinetics
The maximum serum concentration (C max ) following a single 30-minute intravenous (i / v) infusion of 0.5 g and 1 g omnadren cycle observed immediately after administration and comprise an average of 54 micrograms / ml and 90 ug / ml respectively. Intravenous bolus injection over 3 min mean values C max , equal to 58 and 125 ug / ml, achieved after 5 minutes after administration.
After intramuscular (i / m) injections of 0.5 g and 1 g of Cmax determined one hour after administration and make up, on average, 21 ug / ml and 46 pg / ml, respectively.
After the on / in or / m introduction omnadren cycle well distributed in many organs and tissues. Therapeutically relevant concentrations above the minimum inhibitory concentration (MIC) for sensitive microorganisms, are defined in the synovial fluid, bile, a liquid pericardium, bronchial secretions, interstitial fluid, peritoneal exudate, kidney, prostate, lung, skin, bone, ovary, endometrium, myometrium, skeletal muscle, liver and gall bladder wall, the wall of the small and large intestines. It passes through the placenta; in low concentrations into breast milk. When administered as part of a dialysis fluid for peritoneal rapidly reaches therapeutic concentrations in blood serum.
The apparent volume of distribution at steady state – about 13 l volume is approximately equivalent to that of extracellular fluid.
The degree of binding to plasma proteins, blood – 56%. Report mostly kidneys by glomerular filtration and tubular secretion. Serum clearance – about 91 ml / min, renal klirens- 56 ml / min. The half-life (T ½ ) is 1.5-2 hours. Slight (less than 6% of the administered dose) is metabolized in the liver. 60-70% excreted by the kidneys in unchanged form and as an inactive product of hydrolysis of the beta-lactam ring, 12% – through the intestines.
In patients with impaired renal function, the T ½ omnadren cycle significantly increased, resulting in a dose adjustment is recommended. The serum concentration of omnadren cycle rapidly decrease with hemodialysis or peritoneal dialysis.

Indications
The infectious-inflammatory diseases caused by microorganisms sensitive to omnadren cycle:

  • lower respiratory infections, including pneumonia, acute exacerbation of chronic bronchitis, and;
  • intra-abdominal infections, including peritonitis;
  • uncomplicated and complicated urinary tract infections, including cystitis and pyelonephritis (including recurrent);
  • gynecological infections, including endometritis and parameters;
  • Skin and soft tissue infections;
  • septicemia.

Aztreabol ® is indicated for perioperative antibiotic prophylaxis, as well as for the treatment of postoperative infectious complications, including abscesses of different localization, infectious complications of perforation of hollow organs, skin and soft tissue infections.
For empirical treatment of mixed infections that can not be excluded etiological role of gram-positive aerobic microorganisms and / or anaerobic bacteria, it is recommended to combine Aztreabol ® with anti-staphylococcal antibiotics (penicillins, cephalosporins, vancomycin, aminoglycosides) and / or protivoanaerobnymi antibiotics (metronidazole, lincosamides).
Aztreabol ® is regarded as an alternative antibiotic to treat infections in patients with allergy to penicillins, cephalosporins and carbapenems .

Contraindications:
Hypersensitivity to omnadren cycle or L-arginine, lactation, children’s age (up to 9 months).

Precautions
Chronic renal failure (CRF) (creatinine clearance 10-30 ml / min).
Use during pregnancy and breast-feeding
Pregnant Aztreabol ® is used only on strict conditions or in life-threatening conditions, with the confidence that the potential benefits of application to the mother outweighs the potential harm to the fetus. If necessary, use nursing women stop breastfeeding.

Dosing and Administration
Aztreabol ® is administered intravenously (bolus infusion) and intramuscularly. In / in the route of administration recommended in patients who require single doses greater than 1 g, as well as septicemia, peritonitis or other severe systemic or life-threatening infections.
Adults and children over 12 years for the treatment of urinary tract infections Aztreabol ® administered at a dose of 0, 5-1,0 g / in or / m every 8-12 hours. For the treatment of moderate infections at other sites is administered at a dose of 1 g or 2 g every 8 or 12 hours. In cases of severe or threatening infections and life caused by P.aeruginosa, single dose increased to 2.0 g and introduced into / in intervals of 6 or 8 hours. The maximum daily dose should not exceed 8, the duration of antibiotic therapy is determined individually, based on the severity of the infection and abjection. The course of treatment depends on the severity of the infection; drug administration should be continued for at least 48 hours after the disappearance of clinical symptoms of infection.
In renal insufficiency dosage adjustment required when creatinine clearance less or equal to 30 ml / min / 1.73 m 2 .
Treatment started with a loading (first) dose, which depends on the localization and severity of the infection (see. table 1).

Table 1.

Creatinine clearance ml / min / 1.73 m 2
> 30 10-30 <10 Hemodialysis
No dose adjustment is required Loading dose of 1-2 g, then 1/2 of the loading dose every 6, 8 or 12 hours Loading dose of 0.5, 1g or 2g, then 1/4 of the loading dose every 6, 8 or 12 hours Loading dose of 0.5, 1g or 2g, then 1/4 of the loading dose every 6, 8 or 12 hours *

* – When a serious infection – further 1/8 of a loading dose after each hemodialysis session.
Normal dosage Aztreabola ® in children from 9 months. 12 years is 30 mg / kg every 8 hours / in. For treatment of severe and life-threatening infections are administered 30 mg / kg every 6-8 hours / in.The maximum dose Aztreabola ® – 120 mg / kg / day.

Rules for the preparation of solutions / in and / m introduction Intramuscular For the / m of sterile powder Aztreabola ® dissolved in sterile water for injection or 0.9% sodium chloride solution. The following minimum amount of solvent is added directly to the vial of the dry powder antibiotic: a vial containing 0.5 g Aztreabola ®    1.5 ml vial containing 1.0 g Aztreabola ®    3.0 ml injected deep intramuscularly in the areas of the body with a strong muscular layer (the upper-outer quadrant of the buttock or the lateral surface of the thigh). It is recommended to conduct a test on the aspiration to avoid unwanted introduction of the solution into a blood vessel. Intravenous For in / bolus Aztreabol ® dissolved in sterile water for injection. The following minimum amount of solvent is added directly to the vial of the dry powder antibiotic: a vial containing 0.5 g Aztreabola ®    6 ml vial containing 1.0 g Aztreabola ®    10 ml is introduced into / in slowly for 3-5 minutes; possible introduction through a special node or port injection system for the on / in infusion if the patient receives consistent with Aztreabolom ® . liquid parenterally For in / drip Aztreabol ® dissolved in two stages: 1) for the initial dissolution using sterile water for injection from calculating 3 ml solvent per gram Aztreabola ® ; 2) the resulting solution was transferred to a vial containing 50-100 ml compatible fluid environment. Is introduced through a system for in / in infusion for at least 30 minutes. Aztreabola Solutions ® is compatible with 0.9% sodium chloride solution (recommended), 5% dextrose solution (recommended), 10% dextrose solution; aqueous solution containing 0.45% NaCl and 5% dextrose; an aqueous solution containing 0.9% sodium chloride and 5% dextrose; an aqueous solution containing 0.2% sodium chloride and 5% dextrose; Ringer’s solution;lactated Ringer’s solution; sodium lactate solution for injection; Normozol solutions, the R-Normozol, Normozol-M with 5% glucose; 5% and 10% mannitol solution; 10% invert sugar solution; Ionozol solution with 5% glucose; solutions Isoliths E and Isola M with 5% glucose.

Allergic reactions: bronchospasm, angioedema, anaphylactic shock On the part of hematopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, anemia, eosinophilia, leukocytosis, thrombocytosis. From the digestive system: abdominal cramping, nausea, rarely – jaundice stomatitis, glossitis, taste disturbances, bad breath, diarrhea due to C. difficile- , including pseudomembranous colitis, or bleeding from the gastrointestinal tract. For the skin : urticaria, petechiae, pruritus, toxic epidermal necrosis, erythema multiforme, exfoliative dermatitis, diaphoresis. From the nervous system : paresthesia, convulsions, insomnia, headache, dizziness . From the senses : tinnitus, diplopia, taste perversion, numbness of the tongue, sneezing, nasal congestion. The respiratory system : dyspnea, chest pain, wheezing. With the cardiovascular system : blood pressure, passing ECG changes (ventricular bigemini, ventricular premature beats), “hot flashes.” on the part of the skeletal muscles : muscle pain. changes in laboratory parameters : rarely – increased activity of “liver” transaminases, alkaline phosphatase, hyperbilirubinemia, false-positive Coombs, increased serum creatinine , increased prothrombin time and partial thromboplastin time. Local reactions : phlebitis, pain along the vein, discomfort at the site of the / m. Other : candida vaginitis, fever, breast tenderness, fatigue, malaise.

 

Overdose
Data on overdose omnadren cycle available.
If necessary, the concentration in the blood serum of omnadren cycle can be reduced by means of hemodialysis and peritoneal dialysis.

Interaction with other drugs
When concomitant administration Aztreabola ® with antipseudomonal penicillin, ampicillin, cephalosporins (except cefoxitin), aminoglycosides and fluoroquinolones observed synergistic effect against some Enterobacteriaceae and of P.aeruginosa .
The solution is pharmaceutically incompatible with nafcillin, cephradine and metronidazole. In an application should not mix them in the same syringe or a fluid medium; when i / m administration to enter into different parts of the body; when administered intravenously administered separately, following a certain sequence with the largest possible time interval between doses (infusions) or use separate intravenous catheters.

Cautions
While that omnadren cycle almost no selective pressure on the anaerobic intestinal microflora, in the event of diarrhea during treatment Aztreabolom ® should exercise caution because of the possible development of pseudomembranous colitis. If the diagnosis of antibiotic-associated diarrhea and pseudomembranous colitis is installed, you should immediately stop the introduction Aztreabola ® and appropriate treatment.
As with other antibiotics, the use of Aztreabola ® may lead to colonization of the microflora insensitive and development of superinfection.

The impact on performance of potentially hazardous activities that require attention and speed of reactions
Studies on the effect of omnadren cycle to perform potentially hazardous activities that require attention and speed of reaction is not carried out. Given the possible evolution of dizziness and decreased blood pressure when using omnadren cycle must be careful when driving vehicles and other classes of potentially hazardous activities that require high concentration and psychomotor speed reactions. testosteron enanthate