Active substanceAmpicillin + SulbactamAmpicillin + Sulbactam
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    ALVILS, LTD.     Russia
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:

    Per 1 bottle:

    Active substances:

    Ampicillin sodium 1063 mg in terms of ampicillin 1000 mg; sulbactam sodium 547 mg in terms of sulbactam 500 mg.

    Description:White or white with a yellowish tinge powder, hygroscopic.
    Pharmacotherapeutic group:Antibiotic - penicillin semisynthetic + beta-lactamase inhibitor
    ATX: & nbsp

    J.01.C.R.   Combinations of penicillins (including those with beta-lactamase inhibitors)

    Pharmacodynamics:

    Ampicillin + sulbactam is a combined preparation that has a bactericidal effect against ampicillin-sensitive microorganisms, including strains producing beta-lactamases.

    Ampicillin is a semi-synthetic penicillin with a wide spectrum of activity, inhibits the synthesis of cell wall proteins of pathogenic microorganisms. Sulbactam is an irreversible beta-lactamase inhibitor; expands the spectrum of ampicillin activity against resistant strains, the resistance of which develops under the exposure to beta-lactamases; does not change the activity of ampicillin against sensitive strains; by binding to certain penicillin-binding bacteria proteins, exhibits synergism with simultaneous use with beta-lactam antibiotics. Stable in aqueous solution, has an independent antibacterial activity against the family Neisseriaceae and Acinetobacter spp. and is resistant to the action of most plasmid beta-lactamases.

    Ampicillin + sulbactam is active against the following microorganisms (including strains producing beta-lactamases):

    Aerobic Gram-positive bacteria: Staphylococcus aureus (producing and non-producing beta-lactamase strains), Staphylococcus epidermidis (producing and non-producing beta-lactamase strains), Staphylococcus saprophyticus (producing and non-producing beta-lactamase strains), Streptococcus pyogenes, Streptococcus pneumoniae (including strains resistant to penicillin), Streptococcus spp. groups viridans, Enterococcus faecalis, Listeria monocytogenes.

    Aerobic Gram-negative bacteria: Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella spp., Neisseria gonorrhoeae (producing and non-producing beta-lactamase strains), Moraxella catarrhalis (producing and non-producing beta-lactamase strains), Morganella morganii, Haemophilus influenzae (including strains resistant to ampicillin), Providencia rettgeri, Providencia stuartii.

    Anaerobic microorganisms: Bacteroides spp., including Bacteroides fragilis, Clostridium spp. (Besides Clostridium difficile), Peptococcus spp., Peptostreptococcus spp.

    Resistant: methicillin-resistant Staphylococcus spp., Citrobacter spp., most strains Enterobacter spp., Pseudomonas aeruginosa, Mycobacterium spp., Clostridium difficile, Chlamydia pneumoniae, Mycoplasma pneumoniae.

    Pharmacokinetics:

    Maximum serum concentrations (Cmah) ampicillin and sulbactam after intravenous (iv) administration 1.5 g and 3 g of the drug are 40-71 μg / ml and 109-150 μg / ml for ampicillin; 21-40 μg / ml and 48-88 μg / ml for the sulbactam, respectively. After intramuscular (intramuscular) injection, 1.5 g of ampicillin + sulbactam CmThe amplitude of ampicillin varies from 8 μg / ml to 37 μg / ml, Cmsulbactam - from 6 μg / ml to 24 μg / ml. The degree of binding to plasma proteins is 28% for ampicillin and 38% for sulbactam.

    Both sulbactam and ampicillin well distributed in a variety of tissues and fluids.Therapeutic concentrations after IM and IV administration are created in peritoneal and pleural fluids, interstitial fluid, intestinal wall, pelvic organs, skin and subcutaneous tissue. Poor penetrate the blood-brain barrier, with inflammation of the meninges, permeability to the cerebrospinal fluid increases. The half-life period (T1 / 2) of ampicillin and sulbactam averages about 1 hour. Both components of the drug are excreted mainly by the kidneys in unchanged form. From 75% to 85% of the administered dose of ampicillin and sulbactam are excreted by the kidneys within the first 8 hours. In patients with varying degrees of renal dysfunction, the T1 / 2 component of the drug is increased, which requires dose adjustment and administration of the drug.

    Indications:

    Infectious-inflammatory diseases caused by susceptible to ampicillin + sulbactam strains of microorganisms:

    -infections of ENT organs (including sinusitis, otitis media, tonsillitis);

    -infection of respiratory organs (acute and exacerbation of chronic bronchitis, pneumonia, lung abscess, pleural empyema);

    -infective endocarditis, bacterial meningitis, sepsis;

    - uncomplicated and complicated infections of the abdominal organs (cholecystitis, cholangitis, peritonitis, abscess of the abdominal cavity);

    -infection of the urinary tract (acute and exacerbation of chronic pyelonephritis, pyelitis);

    Infectious-inflammatory diseases of the pelvic organs (salpingitis, salpingoophoritis, tubo-ovarian abscess, endometritis, pelvioperitonitis);

    -gonococcal infection;

    -infection of the skin and soft tissues (erysipelas, abscess, phlegmon, wound and postoperative infection);

    -infection of bones and joints.

    Prevention of postoperative complications in operations on the abdominal and pelvic organs.

    Contraindications:

    Hypersensitivity to any of the components of the drug and other beta-lactam antibiotics; infectious mononucleosis (including when there is a measles-like rash), lymphocytic leukemia.

    Safety of ampicillin + sulbactam in patients with terminal stage of chronic renal failure (creatinine clearance less than 5 ml / min) not installed.

    When using procaine, lidocaine as a solvent - increased sensitivity to local anesthetics of the amide type, severe shock, blockade of intracardiac conduction, severe heart failure.

    Carefully:

    Bronchial asthma, pollinosis and other allergic diseases, liver failure, chronic diseases of the gastrointestinal tract in history, previously suffered colitis associated with the use of antibacterial drugs, impaired renal function, and advanced age.

    Pregnancy and lactation:

    Use during pregnancy is only possible if the intended benefit to the mother exceeds the potential risk to the fetus. Ampicillin and sulbactam penetrate into breast milk in low concentrations. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

    Dosing and Administration:

    Intravenous (jet and drip), intramuscularly. The mode of administration depends on the severity of the infection and the chosen dose. The following are the total doses of ampicillin and sulbactam (in a 2: 1 ratio).

    In adults and children over 12 years old and weighing more than 40 kg, for the treatment of infections of moderate severity, injected / m or IV 1.5 g every 6 hours. In severe infections - 3 g every 6 hours. The maximum daily dose of sulbactam should not exceed 4 g, which corresponds to a daily dose of 12 g.

    Treatment should be continued for at least another 2-3 days after the disappearance of the clinical symptoms of the disease. The duration of treatment is 5-14 days, however, in more severe cases it can be increased or supplemented ampicillin.

    With uncomplicated gonorrhea - 1.5 g once.

    For the prevention of postoperative infection - 1.5-3 g during anesthesia, then within 24 hours after the operation in the same dose every 6-8 hours.

    In children older than 1 month and up to 12 years of age (or body weight less than 40 kg), the drug is administered at a dose of 150 mg / kg per day, which is divided into 3-4 injections. In severe infection, the dose can be increased to 300 mg / kg / day. The duration of the course of therapy should not exceed 14 days.

    In preterm infants and children of the first week of life, the daily dose of the drug is 75 mg / kg, which is divided into two injections.

    In children from 7 days to 28 days, the drug is prescribed at a dose of 150 mg / kg per day, divided into 3 intravenous infusions.

    In patients with impaired renal function, correction of the dosing regimen is performed depending on the values ​​of creatinine clearance (CK).

    Creatinine clearance, ml / min

    T1 / 2, h

    Recommended mode of administration

    30

    1

    1.5-3 g every 6-8 hours

    15-29

    5

    1.5-3 g every 12 hours

    5-14

    9

    1.5-3 g every 24 hours

    In children with kidney failure (CC less than 30 ml / min), the drug is administered in usual single doses (50-75 mg / kg), increasing the intervals between administrations, as indicated in adults.

    Preparation of solutions:

    To prepare the solution for the / m introduction, sterile water for injection, 0.5% solution of procaine, 0.5% lidocaine solution is used as the solvent. 4 ml of the solvent are added to the vial containing 1.5 g of the preparation.

    To prepare a solution for IV infusion into the bottle containing 1.5 g of the drug, add 12 ml of water for injection, 0.9% solution of sodium chloride. Enter slowly for 3-5 minutes.

    To prepare a solution for intravenous drip 1.5-3 g of the drug is dissolved in 12 ml of water for injection, then the resulting solution is added to 150-200 ml of a 0.9% solution of sodium chloride or 5% solution of dextrose and injected at a rate of 60-80 drops in minute.

    Side effects:

    Allergic reactions: urticaria, skin hyperemia, skin itch, Quincke's edema, rhinitis, conjunctivitis, fever, arthralgia, anaphylactic shock, Stevens-Johnson syndrome, multiform exudative erythema, toxic epidermal necrolysis.

    From the digestive system: nausea, vomiting, decreased appetite, diarrhea, flatulence, glossitis, pseudomembranous colitis, increased activity hepatic transaminase.

    On the part of the organs of hematopoiesis: hemolytic anemia, reduction of hemoglobin, thrombocytopenia, eosinophilia, leukopenia, neutropenia, lymphopenia, lymphocytosis, thrombocytosis, monocytosis, false-positive Coombs test.

    From the central nervous system: drowsiness, headache.

    Laboratory indicators: azotemia, increased urea concentration in blood plasma, hypercreatininaemia, a decrease in serum protein, leukocyturia, cylindruria.

    Local reactions: with the / m introduction - soreness at the injection site, with / in the introduction - phlebitis, thrombophlebitis.

    Other: malaise, chest pain, sore throat, dysuria, swelling, bleeding, with long-term treatment - candidamycosis, development of superinfection.

    Overdose:

    Symptoms: neurological disorders up to seizures (especially in patients with impaired renal function), nausea, vomiting, diarrhea, disturbance of water-electrolyte balance (as a consequence of vomiting and diarrhea).

    Treatment: symptomatic therapy; in severe cases - hemodialysis.

    Interaction:

    When used simultaneously with indirect anticoagulants ampicillin + sulbactam potentiates their action; reduces the effectiveness of oral contraceptives, drugs, in the process of metabolism which forms para-aminobenzoic acid and ethinyl estradiol (risk of bleeding "breakthrough").

    With simultaneous use with aminoglycosides, there is a pronounced synergism of bactericidal action against gram-positive and gram-negative bacteria.

    Pharmaceutically incompatible with blood products or protein hydrolysates, aminoglycosides. When using the drug with aminoglycosides simultaneously, do not mix drugs in one syringe or one infusion system; with the / m introduction to enter into different parts of the body; when IV introduction, enter separately, observing a certain sequence with as long as possible a time interval between introductions, or use separate intravenous catheters.

    Probenecid, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs reduce tubular secretion of ampicillin and sulbactam and increase their half-life. Diuretics reduce the clearance of penicillins.

    Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic.

    Simultaneous use of ampicillin and allopurinol increases the risk of skin rash.

    Special instructions:

    With prolonged use of the drug, periodic monitoring of the kidneys, liver and general blood analysis is necessary.

    Before the start of therapy, a thorough anamnesis should be made about the previous allergic reactions to beta-lactam antibiotics. When developing an allergic reaction, the drug should be immediately discontinued.

    When using the drug, both in the background of taking and 2-3 weeks after the cessation of treatment, it is possible to develop diarrhea caused by Clostridium difficile (pseudomembranous colitis). In mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole. Do not use drugs that inhibit the intestinal motility.

    With the use of ampicillin + sulbactam (as well as other antibiotics), it is possible to develop superinfection, which requires the withdrawal of the drug and the appointment of appropriate treatment.

    It is possible to detect a false positive sample of Coombs, a false positive test for glucose in the urine (using the method of Benedict or Felling).

    In the treatment of patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

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

    Data on the adverse effect of the drug at recommended doses on the ability to drive a vehicle or work with mechanisms are not present.

    However, given the likelihood of side effects from the central nervous system, caution should be exercised when practicing potentially dangerous Activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:

    Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg + 500 mg.

    Packaging:

    By 1500 mg (1000 mg + 500 mg) in terms of the amount of active substances in colorless transparent glass bottles, closed with rubber stoppers,Crimped aluminum caps with protective plastic covers for the first opening. For each the bottle is labeled or labeled quick-fixing paint.

    On 1 bottle together with the instruction on application place in a pack a cardboard.

    For hospitals:

    10 bottles per pallet. For 1 or 5 pallets, together with the instructions for use, put in a cardboard box.
    Storage conditions:

    Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002539
    Date of registration:21.07.2014
    Expiration Date:21.07.2019
    The owner of the registration certificate:ALVILS, LTD. ALVILS, LTD. Russia
    Manufacturer: & nbsp
    Information update date: & nbsp22.08.2017
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