Active substanceAmpicillinAmpicillin
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:

    Per one vial: 0.5 g 1.0 g 2.0 g

    Ampicillin sodium

    (in terms of ampicillin) 0.5 g 1.0 g 2.0 g

    Description:Powder white or white with a yellowish tint of color
    Pharmacotherapeutic group:Antibiotic, penicillin semisynthetic
    ATX: & nbsp

    J.01.C.A   Penicillins of a wide spectrum of action

    J.01.C.A.01   Ampicillin

    Pharmacodynamics:

    Ampicillin is a broad-spectrum bactericidal antibiotic. The bactericidal effect of ampicillin is due to irreversible binding to bacterial transpeptidases involved in the biosynthesis of peptidoglycans, the main component of the bacterial cell wall.

    Active against Gram-positive aerobic bacteria / Staphylococcus spp. (except strains that produce penicillinase). Enterococcus spp., at t.ch. Enterococcus faecalis, Streptococcus pneumoniae (except strains that produce penicillinase), Streptococcus pyogenes, Streptococcus spp. groups viridans, Listeria monocytogenes, Bacillus anthracis, Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae; Gram-negative aerobic bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Bordetella p ertussis, some strains Hemophilus influenzae, Escherichia coli, Shigella spp., Salmonella spp., Helicobacter pylori; some anaerobes: Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Prevotella melaninogenica.

    Ampicillin is destroyed by penicillinases, produced by microorganisms.

    Inactive against penicillinase-producing strains Staphylococcus spp. and Streptococcus pneumoniae, all strains Pseudomonas aeruginosa, Clostridium difficile, most strains Klebsiella spp. and Enterobacter spp., most strains Bacteroides spp., in t.ch. Bacteroides fragilis.

    Pharmacokinetics:

    Maximum concentrations (FROMmOh) To ampicillin after / in 1.0 g and 2.0 g of drug ranged from 40 ug / mL to 71 micrograms / ml and from 109 pg / ml to 150 ug / ml, respectively. After intramuscular injection, 1.0 g of ampicillin CmOh are varied from 8 μg / ml to 37 μg / ml. Communication with plasma proteins is 28%.

    Ampicillin penetrates well and evenly distributed in organs n tissues of the body, found at therapeutic concentrations in the pleural, peritoneal, amniotic and synovial fluids, cerebrospinal fluid, skin and subcutaneous tissue, urine (high concentration), intestinal mucosa, bones, gall bladder, lung, female genital tissues, bile, in the bronchial secretions, paranasal sinuses, middle ear fluid (if inflammation), saliva. Practically it does not penetrate the intact blood-brain barrier permeability which increases in inflammation of the meninges.

    The half-life of ampicillin is about 1 hour.

    Ampicillin is excreted mainly by the kidneys in an unchanged form, in part - through the intestine. From 75% to 85% of the administered dose of ampicillin is excreted by the kidneys during the first 8 hours, while in the urine very high concentrations of unchanged antibiotic are created. With repeated administration does not cumulate. Removed during hemodialysis.

    Indications:

    Infections caused by ampicillin-sensitive microorganisms:

    - bacterial meningitis;

    - infective endocarditis (prevention and treatment);

    - infections of the ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media); -infection of the respiratory tract (including acute and exacerbation of chronic bronchitis, pneumonia, lung abscess);

    - intra-abdominal infections (including peritonitis);

    - bile duct infection (including cholecystitis, cholangitis);

    - infections of the gastrointestinal tract (including typhoid and paratyphoid, shigellosis, salmonellosis);

    -infection of the kidneys and urinary tract (pyelonephritis, pyelitis, cystitis, urethritis);

    - infectious and inflammatory diseases of the pelvic organs in women (cervicitis, salpingitis, endometritis, pelvioperitonitis, tubo-ovarian abscess);

    - infections of the skin and soft tissues (including erysipelas, infected dermatoses, impetigo);

    - infections of bones and joints;

    - sepsis;

    - rheumatism;

    - pasteurellosis;

    - listeriosis;

    - Gonorrhea.

    Contraindications:

    Hypersensitivity (including other antibiotics from the penicillin group); infectious mononucleosis, lymphocytic leukemia.

    Carefully:

    Bronchial asthma, pollinosis and other allergic diseases, increased sensitivity to antibiotics of cephalosporin series and carbapenems; severe renal dysfunction, hepatic impairment; Colon disease in history (especially colitis associated with the use of antibiotics).

    Pregnancy and lactation:

    During pregnancy, appoint in cases where the intended benefit to the mother exceeds the possible risk to the fetus.

    Ampicillin penetrates into breast milk in low concentrations. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

    Dosing and Administration:

    Intramuscularly, intravenously.

    Doses and dosing regimen are chosen individually depending on the severity of the course, the localization of the infection and the sensitivity of the pathogen. The average therapeutic dose for adults and children with a body weight of more than 40 kg - 250-500 mg, which is injected in / m or IV (jet, drip) every 6 hours. In case of severe infection, the daily dose can be increased to 10 g. For the treatment of gonorrhea, 2 doses of 500 mg with an interval of 8 or 12 hours. For the treatment of bacterial meningitis and sepsis, the daily dose of the drug is 150,200 mg / kg, divided by 6-8 IV infusions with an interval of 3-4 hours. The maximum daily dose is 8-14 g.

    For the prevention of bacterial endocarditis in patients from the high-risk group who undergo dental, endoscopic interventions, "small" surgeries on ENT organs, as well as operations on the organs of the gastrointestinal tract or bile ducts - 2 g IV or IM 30 minutes before the procedure or operation; if necessary, after 6 hours, re-injected at a dose of 1 g.

    In children weighing less than 40 kg for the treatment of infections of the respiratory tract, skin and soft tissues, the daily dose of ampicillin is 25-50 mg / kg; To treat infections of the abdominal cavity or urinary tract, 50-100 mg / kg per day is administered. The daily dose is divided into 4 injections at an interval of 6 hours. For the treatment of septicemia or infections of the central nervous system (bacterial meningitis), the daily dose of 100-200 mg / kg is divided into 6-8 intravenously injected with an interval between administrations of 3-4 h.

    For the prevention of bacterial endocarditis - 50 mg / kg IV or IM for 30 minutes before the procedure or operation; if necessary, after 6 hours, re-injected at a dose of 25 mg / kg.

    Newborns under the age of 7 days with a body weight of less than 2 kg administered intravenously or intravenously at 25-50 mg / kg every 12 hours, with a body weight of more than 2 kg - 25-50 mg / kg every 8 hours.

    Newborns aged 7 up to 28 days with a body weight of 1.2-2 kg administered at 25-50 mg / kg every 8 hours, with a body weight of more than 2 kg - 25-50 mg / kg every 6 hours.

    For the treatment of bacterial meningitis: in newborns under 7 days of daily dose of ampicillin - 200-300 mg / kg, which is divided into 3 in / in the introduction at an interval of 8 hours; in newborns aged 7 to 28 days the daily dose is 300 mg / kg, which is divided into 4-6 intravenous injections with an interval of 4-6 hours.

    The duration of the / m introduction is 7-14 days. The duration of IV application is 5-7 days, with the subsequent transition (if necessary) to the / m introduction. It is recommended to continue the introduction of ampicillin for another 48-72 hours after the disappearance of clinical signs of the disease.

    Rules for solution preparation and introduction

    For Preparing the solution for the / m administration as a solvent, sterile water for injection is used. In a vial containing 500 mg - 1.8 ml, 1 g - 3.5 ml and 2 g - 6.8 ml of solvent.

    For intravenous string introduction: 5 ml of water for injections are added to a vial containing 500 mg of ampicillin; injected iv slowly for 3-5 min; 7.4 ml are added to bottles containing 1 g of the preparation, and 2 grams to 14.8 ml of water for injection; injected iv slowly for 10-15 min.

    With a single dose exceeding 2 g, the drug is administered intravenously drip. To do this, the drug (2-4 g) is dissolved in 7.5-15 ml of water for injection, then the resulting solution is added to 125-250 ml of a 0.9% solution of sodium chloride or 5% solution of dextrose and injected at a rate of 60-80 drops per minute .

    Side effects:

    Allergic reactions: itching and flaky skin, hives, rhinitis, conjunctivitis, angioedema, fever, arthralgia, eosinophilia, erythematous and maculopapular rash, exfoliative dermatitis, multiform exudative erythema (including Stevens-Johnson syndrome), reactions similar to whey anaphylactic shock.

    From the digestive system: dysbacteriosis, stomatitis, gastritis, dry mouth, taste change, abdominal pain, vomiting, nausea, diarrhea, stomatitis, glossitis, moderate increase in hepatic transaminase activity, pseudomembranous colitis.

    From the central nervous system: headache, tremor, convulsions (with high-dose therapy).

    On the part of the blood system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, anemia.

    Local reactions: pain and infiltrates in places with / m introduction, phlebitis with IV injection in large doses.

    Other: interstitial nephritis, nephropathy, superinfection, vaginal candidiasis; non-allergic "ampicillin" rash, can disappear without discontinuing the drug.

    Overdose:

    Symptoms: manifestations of toxic effects on the central nervous system (especially in patients with renal insufficiency); nausea, vomiting, violation of water-electrolyte balance (as a consequence of vomiting and diarrhea).

    Treatment: medicines to maintain the water-electrolyte balance, symptomatic therapy. In severe cases: hemodialysis.

    Interaction:

    In solution, it is pharmaceutically incompatible with aminoglycosides. If used simultaneously, do not mix them in a single 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 as possible a time interval between injections (infusions), or use separate intravenous catheters.

    When combined with a friend "bactericidal antibiotics (including aminoglycosides, vancomycin, rifampicin) acts synergistically.

    Drugs that block tubular secretion (probenecid), diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs increase the concentration of ampicillin in the plasma by reducing its tubular secretion.

    Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index).

    Reduces the effectiveness of estrogen-containing oral contraceptives, so additional methods of contraception are recommended during ampicillin therapy.

    Reduces clearance and increases the toxicity of methotrexate.

    Allopurinol increases the risk of developing an "ampicillin" skin rash.

    Special instructions:

    At course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys. When using the drug in high doses in patients with renal insufficiency, a toxic effect on the central nervous system is possible.Perhaps the development of superinfection due to the growth of microflora insensitive to ampicillin, which requires a corresponding change in antibacterial therapy. With the appointment of patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible. In patients who have increased sensitivity to penicillins, there may be cross-allergic reactions with other beta-lactam antibiotics. If diarrhea occurs during treatment with ampicillin should be cautious because of the possible development of pseudomembranous colitis. If a diagnosis of antibiotic-associated diarrhea or pseudomembranous colitis is established, ampicillin should be discontinued immediately and appropriate treatment should be prescribed. Treatment should necessarily continue for another 48-72 hours after the disappearance of clinical signs of the disease.

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

    There is no evidence pointing to the negative effects of sodium ampicillin in the ability to drive vehicles and other classes of potentially hazardous activities that require high concentration and psychomotor speed reactions.

    Form release / dosage:

    Powder for solution for intravenous and intramuscular injection 0.5 g, 1.0 g, 2.0 g.

    Packaging:

    0.5 g and 1.0 g of active substance into glass bottles with a capacity of 10 ml or 2.0 g of active substance into 20 ml glass vials, hermetically sealed with rubber stoppers, crimped with aluminum caps or crimped with aluminum caps and closed with a protective plastic lid.

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

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

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

    Five vials of the drug are packed in contour mesh packages made of polyvinyl chloride film and aluminum foil foil or without foil. One outline package and instructions for use are put in a pack of cardboard.

    5 vials with the preparation complete with 5 ampoules of the solvent are packed in contoured cell packs made of polyvinyl chloride 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 dry protected from light, 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:LP-000089
    Date of registration:15.12.2010
    Expiration Date:15.12.2015
    The owner of the registration certificate:ABOLMED, LLC ABOLMED, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp21.08.2017
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