Active substanceAzrethonAzrethon
Similar drugsTo uncover
  • Aznam J
    powder w / m in / in 
  • Azrerebol®
    powder w / m in / in 
    PREBAND PFC, LLC     Russia
  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:1 bottle contains as active substance - aztreonam 0.5 g or 1.0 g and as an auxiliary - L-arginine 0.4 g and 0.8 g respectively.
    Description:White or white with a yellowish tint powder.
    Pharmacotherapeutic group:Antibiotic monobactam
    ATX: & nbsp

    J.01.D.F   Monobactams

    J.01.D.F.01   Azrethon

    Pharmacodynamics:

    Azrethra is a synthetic monocyclic beta-lactam antibiotic for parenteral use. Structurally different from other beta-lactam antibiotics (such as penicillins, cephalosporins); The nucleus of the molecule is alpha-methyl-3-amino mono-baccamic acid. It is bactericidal: it binds to transpeptidases and breaks the final stages of bacterial cell wall synthesis. Has a high affinity for penicillin-binding protein 3. Highly resistant to beta-lactamases (including penicillinases and cephalosporinases) of gram-negative bacteria. Has a strong and specific activity in vitro for gram-negative aerobic pathogens, including Pseudomonas aeruginosa. The bactericidal action is manifested in a wide range of pH values ​​and under anaerobic conditions.

    Is active against the following microorganisms as in vitro, and in vivo: Citrobacter spp., including S. freundii, Enterobacter spp., including E. cloacae, Escherichia coli, Haemophilus influenzae (including ampicillin-resistant and other penicillinase-producing strains), Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia spp., including S. marcescens. The following strains were sensitive in vitro, however, the clinical significance of these data is not known: Aeromonas hydrophila, Morganella morganii, Neisseria gonorrhoeae (including penicillinase-producing strains), Pasteurella multocida, Proteus vulgaris, Providencia stuartii, Providencia rettgeri, Yersinia enterocolitica. Resistant to Azrethabol®: Gram-positive aerobic cocci and bacteria, Acinetobacter spp., anaerobic microorganisms, mycoplasmas and other intracellular pathogens, Mycobacterium spp.

    It is possible to use Azreaabol® for allergies to penicillins, cephalosporins and carbapenems. Rarely causes dysbacteriosis.
    Pharmacokinetics:

    Maximum serum concentrations (Cms) after a single 30-minute intravenous (i / v) infusion of 0.5 g and 1 g aztreonam observed immediately after administration and comprise, on average 54 mg / ml and 90 ug / ml, respectively. With an intravenous bolus injection for 3 min, the mean Cmah, equal to 58 and 125 μg / ml, are achieved 5 minutes after administration.

    After intramuscular (in / m) injection, 0.5 g and 1 g of Cmah are determined one hour after administration and are, on average, 21 μg / ml and 46 μg / ml, respectively.

    After IV or IM injections aztreonam well distributed in many organs and tissues. Therapeutically significant concentrations, exceeding the minimum inhibitory concentrations (MICs) for sensitive microorganisms, are defined in the synovial fluid, bile, pericardial fluid, secret, liquid, peritoneal exudate, kidney, prostate, lungs, skin, bones, ovaries, endometrium, myometrium, skeletal muscles, liver tissue and gallbladder wall, the wall of the small and large intestine. Passes through the placenta; in low concentrations penetrates into breast milk. With the introduction of the liquid for peritoneal dialysis quickly reaches therapeutic concentrations in blood serum.

    The apparent volume of distribution in the equilibrium state is about 13 liters, which is approximately equivalent to the volume of the extracellular fluid. The degree of binding to plasma proteins is 56%.

    Displayed mainly by kidneys through glomerular filtration and tubular secretion.Whey clearance - about 91 ml / min, renal clearance -

    (T1/2) is 1.5-2 hours. Slightly (less than 6% of the administered dose) is metabolized in the liver. 60-70% is excreted by the kidneys in unchanged form and as an inactive product of the hydrolysis of the beta-lactam ring, 12% through intestines.

    In patients with reduced renal function T1/2 Aztreonam is markedly increased, as a result of which a dose adjustment is recommended. Serum concentrations Aztreonam rapidly decrease with hemo- or peritoneal dialysis.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to aztreonam: infections of the lower respiratory tract, including pneumonia, acute and exacerbation of chronic bronchitis; Intra-abdominal infections, including peritonitis; uncomplicated and complicated urinary tract infections, including pyelonephritis and cystitis (including recurrent); gynecological infections, including endometritis and parametritis; infections of the skin and soft tissues; septicemia.

    Azrerebol® is indicated for perioperative antibiotic prophylaxis, as well as for the treatment of postoperative infectious complications, including abscesses of various localizations,infectious complications with perforation of hollow organs, skin and soft tissue infections. For empirical therapy of mixed infections when it is impossible to exclude etiological role aerobic Gram-positive microorganisms and / or anaerobes, it is recommended to combine with Aztreabol® protivostafilokokkovymi antibiotics (penicillins, cephalosporins, vancomycin, aminoglycosides) and / or protivoanaerobnymi antibiotics (metronidazole, lincosamides). Aztreabol® considered as an alternative antibiotic to treat infections in patients allergic to penicillin, cephalosporins and carbapenems.
    Contraindications:

    Hypersensitivity to aztreonamu or Larginine, lactation, children's age (up to 9 months).

    Carefully:Chronic renal failure (CRF) (creatinine clearance of 10-30 ml / min).
    Pregnancy and lactation:In pregnant women, Azrereal® is used only on strict indications or in life-threatening conditions, with the belief that the potential benefit from using for the mother exceeds the possible harm to the fetus. If necessary, use nursing women breast feeding is stopped.
    Dosing and Administration:

    Azrethaball® injected intravenously (struyno, drip) and intramuscularly.

    The IV route is recommended in patients who require single doses of more than 1 g, septicemia, with peritonitis or other severe systemic or life-threatening infections.

    Adults and children over 12 years of age for the treatment of urinary tract infections Azrerebol® is prescribed in a dose of 0.5-1.0 g IV or IM every 8-12 hours. For the treatment of moderate infections of other localizations, a dose of 1 g or 2 g every 8 or 12 hours is administered. In cases of severe or life-threatening infections and infections caused by R. aeruginosa, a single dose is increased to 2.0 g and administered iv at intervals of 6 or 8 hours.

    The maximum daily dose of the drug should not exceed 8 g. The duration of antibiotic therapy is determined individually, based on the severity of the infection and the selected pathogens. The course of treatment depends on the severity of the infection; The drug should be continued for at least 48 hours after the disappearance of the clinical symptoms of the infection.

    In renal failure, dose adjustment is required when creatinine clearance is less than or equal to 30 ml / min / 1.73 m2.

    Treatment begins with a loading (first) dose, which depends on the location and severity of the infection (see Table 1).

    Table 1.

    Creatinine clearance, ml / min / 1.73 m2

    >30

    10-30

    <10

    Hemodialysis

    Dose correction is not required

    The loading dose is 1-2 g, then 1/2 of

    loading dose every 6, 8 or 12 hours

    The loading dose is 0.5.1 g or 2 g, then 1/4 of

    loading dose every 6.8 or 12 hours

    The loading dose is 0.5.1 grams 2 g, then 1/4 of the loading dose every 6, 8 or 12 hours *

    * - with severe infection - additionally 1/8 of the loading dose after each hemodialysis session.

    The usual dosages of Azreaabol® children from 9 months. under 12 years old are 30 mg / kg every 8 hours IV. For the treatment of severe and life-threatening infections, 30 mg / kg is administered every 6 to 8 hours IV. The maximum dose of Azreaabol® is 120 mg / kg / day.

    Rules for the preparation of solutions for intravenous and / or intramuscular injection

    Intramuscular injection

    For the / m introduction sterile Azreteabol® powder is dissolved in sterile water for injection or in a 0.9% solution of sodium chloride. The following minimum amounts of solvent is added directly to the vial of dry antibiotic powder: into a vial containing 0.5 g of Azreaabol® 1.5 ml into a vial containing 1.0 g of Azreaabol® 3.0 ml. Enter deeply intramuscularly into areas of the body with a pronounced muscular layer (upper-outer quadrant of the buttock or lateral surface of the thigh).It is recommended that an aspiration test be carried out to avoid undesirable introduction of the solution into the blood vessel.

    Intravenous administration

    For in / in the jet Azrerebol® is dissolved in sterile water for injection. The following minimum amounts of the solvent are added directly to the vial of dry antibiotic powder: into a vial containing 0.5 g Azreaabol® 6 ml per vial containing 1.0 g Azrethabol® 10 ml. Enter iv slowly, for 3-5 min; it is possible to administer through a special node or port for injection of a system for intravenous infusions if the patient receives parenterally compatible fluids with Azrethabol.

    For in / in the drip Azrerebol ® is dissolved in two stages:

    1. sterile water for injection is used for initial dissolution, 3 ml of solvent per gram of Azrethabol®;

    2. the resulting solution is transferred to a vial containing 50-100 ml of a compatible infusion medium. Enter through the system for IV infusions for at least 30 minutes. Azreaabol® solutions are compatible with 0.9% sodium chloride solution (recommended), 5% dextrose solution (recommended), 10% dextrose solution; aqueous solution,containing 0.45% sodium chloride 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; solutions of Normozol, Normozol-R, Normozol-M with 5% glucose; 5% and 10% solutions of mannitol; 10% solution of invert sugar; solution of Ionosol with 5% glucose; solutions Isolit E and Izolit M with 5% glucose.

    Side effects:

    Allergic reactions: bronchospasm, angioedema, anaphylactic shock .

    On the part of the organs of hematopoiesis: leukopenia, neutropenia, granulocytopenia, thrombocytopenia, anemia, eosinophilia, leukocytosis, thrombocytosis.

    From the digestive system: spastic abdominal pain, nausea, very rarely jaundice, stomatitis, glossitis, taste disorders, bad breath, diarrhea caused by FROM. difficile, including pseudomembranous colitis or bleeding from the digestive tract.

    From the skin: urticaria, petechiae, itchy skin, toxic epidermal necrosis, erythema multiforme, exfoliative dermatitis, profuse sweating.

    From the nervous system: paresthesia, convulsions, insomnia, headache, dizziness.

    From the sense organs: noise in ears, diplopia, perversion of taste, numbness of tongue, sneeze, nasal congestion.

    From the respiratory system: shortness of breath, pain in the chest, wheezing.

    From the cardiovascular system: decrease in blood pressure, passing changes on the ECG (ventricular bigeminy, ventricular extrasystole), "tides".

    From the side of skeletal musculature: muscle pain.

    Changes in laboratory indicators: rarely - increase activity "hepatic" transaminase, alkaline phosphatase, hyperbilirubinemia, false positive Coombs test, increased serum creatinine, increased prothrombin time and partial thromboplastin time.

    Local Reactions: phlebitis, soreness along the vein, unpleasant sensations in the place of the / m introduction.

    Other: candidal vaginitis, increased body temperature, tenderness of mammary glands, weakness, malaise.

    Overdose:

    There is no information about an overdose of aztreonam.

    If necessary, the concentrations of aztreonama in the serum can be reduced by hemo- and peritoneal dialysis.
    Interaction:

    With the simultaneous administration of Azreaabol® with antisignagic penicillins, ampicillin, cephalosporins (except cefoxytin), aminoglycosides and fluoroquinolones are observed synergistic effect on some enterobacteria and R. aeruginosa.

    In solution, it is pharmaceutically incompatible with nafcillin, cefradine and metronidazole. At simultaneous application not should be mixed in one syringe or one infusion medium; with the / m introduction to enter into different parts of the body; with intravenous administration Enter separately, observing a certain sequence with as long a time interval between injections (infusions), or use separate intravenous catheters.
    Special instructions:

    Although aztreonam practically does not render selective pressure on the anaerobic microflora of the intestine, if diarrhea occurs during treatment with Azreaabol®, be wary of possible development pseudomembranous colitis. If a diagnosis of antibiotic-associated diarrhea or pseudomembranous colitis is established, immediately discontinue Azreaabol® and appoint appropriate treatment.

    As with other antibiotics, the use of Azreaabol® can lead to colonization insensitive microflora and the development of superinfection.

    Effect on the ability to drive transp. cf. and fur:

    Studies on the effect of aztreonam on the performance of potentially hazardous activities requiring special attention and rapidity of reactions have not been conducted. Considering the possible development of dizziness and lowering of arterial pressure, when using aztreonama, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Powder for the preparation of solution for intravenous and intramuscular injection in vials of 0.5 g and 1.0 g.

    Packaging:

    0.5 g or 1.0 g of active substance are placed in glass vials with a capacity of 10 ml. For each bottle (bottle), glue a label or self-adhesive label, a radio emission sensor RFID - Radiometry or without sensor.

    The solvent - "Water for injection" in glass ampoules of 5 ml.

    1. 1 bottle with the drug and instructions for use are placed in a pack of cardboard.

    2. 1 vial with the preparation and 1 ampoule with solvent are packed in a contour mesh box made of polyvinyl chloride film and aluminum lacquered foil without foil. One outline package and instructions for use are put in a pack of cardboard.

    3. 5 bottles of the drug are packed in contour mesh packaging from polyvinyl chloride film and foil of aluminum lacquered or without foil. One outline package and instructions for use are put in a pack of cardboard.

    4. 5 bottles with the preparation complete with 5 ampoules of the solvent are packed in contoured cell packs made of polyvinylchloride film and foil of aluminum lacquered or without foil. One outline package with the preparation, one outline package with a solvent and instruction for use is put in a pack of cardboard.

    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000123/09
    Date of registration:14.01.2009 / 17.09.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.06.2017
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