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

    Active substance: Ampicillin sodium in terms of ampicillin 500 mg.

    Description:Powder white or almost white; hygroscopic.
    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 producing penicillinases), Enterococcus spp., in t.ch. Enterococcus faecalis, Streptococcus pneumoniae (except strains producing penicillinases), Streptococcus pyogenes, Streptococcus spp. groups viridans, Listeria monocytogenes, Bacillus anthracis, Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae; Gram-negative aerobic bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Bordetella pertussis, some strains Haemophilus 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 for penicillinase-producing strains: Staphylococcus spp., Streptococcus pneumoniae, all strains Pseudomonas aeruginosa, Clostridium difficile, most strains Klebsiella spp. and Enterobacter spp., most strains Bacteroides spp., at t.h. Bacteroides fragilis.

    Pharmacokinetics:

    The maximum concentrations (Cmah) ampicillin after intravenous (iv) administration of 1 g and 2 g of the drug are from 40 μg / ml to 71 μg / ml and from 109 μg / ml to 150 μg / ml, respectively. After intramuscular (IM) injection of 1 g of ampicillin Cmah varies from 8 μg / ml to 37 μg / ml. The connection with plasma proteins is 28%.

    Ampicillin penetrates well and is evenly distributed in the organs and tissues of the body, is found in therapeutic concentrations in pleural, peritoneal, amniotic and synovial fluids, cerebrospinal fluid, skin and subcutaneous tissue, urine (high concentrations), intestinal mucosa, bones, gallbladder, lungs, tissues of female genital organs, bile, in bronchial secretions, paranasal sinuses, middle ear fluid (with its inflammation), saliva. Virtually does not penetrate through the intact blood-brain barrier, the permeability through which increases with inflammation of the meninges.

    The half-life (T1 / 2) is about 1 hour. Ampicillin excreted mainly by the kidneys in an unchanged form, partially through the intestine. From 75% to 85% 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:

    Infectious-inflammatory diseases caused by micro-organisms sensitive to ampicillin:

    - ENT organs: sinusitis, tonsillitis, pharyngitis, otitis media;

    - respiratory tract: acute and exacerbation of chronic bronchitis, pneumonia, lung abscess;

    - bile ducts: cholangitis, cholecystitis;

    - kidney and urinary tract: pyelonephritis, pyelitis, cystitis, urethritis;

    - pelvic organs in women: cervicitis, salpingitis, endometritis, pelvioperitonitis, tubo-ovarian abscess;

    - skin and soft tissues: rye, impetigo, infected dermatoses;

    - bones and joints: rheumatism;

    - gastrointestinal tract: typhoid fever and paratyphoid, shigellosis, salmonellosis;

    - intra-abdominal infections: peritonitis;

    - infectious endocarditis (prevention and treatment);

    - bacterial meningitis;

    - sepsis;

    - pasteurellosis;

    - listeriosis;

    - gonorrhea.

    Contraindications:Hypersensitivity to ampicillin, (including other penicillins, cephalosporins, carbapenems), infectious mononucleosis, lymphocytic leukemia, hepatic insufficiency, colon disease in the anamnesis (especially colitis associated with the use of antibiotics).
    Carefully:Bronchial asthma, pollinosis and other allergic diseases, severe renal dysfunction, children under 1 month of age, history of bleeding.
    Pregnancy and lactation:Use during pregnancy is possible if the expected benefit of treatment for the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation at the time of treatment should stop breastfeeding.
    Dosing and Administration:

    Intravenously (intravenously) (jet, drip), intramuscularly (in / m). 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. In cases of moderate infections, adults intramuscularly - 250-500 mg every 6-8 hours. In case of severe infection, 1-2 g 3-4 times a day or intravenously at 500 mg every 6 hours.

    Listeriosis - 50 mg / kg every 6 hours intramuscularly or intravenously.

    With meningitis - 14 g / day; the frequency of administration is 6-8 times.

    Adults with gonococcal urethritis - intramuscularly 0.5 g 2 times for one day; with gonorrheal uncomplicated urethritis - once 0.5 g.

    For the prevention of bacterial endocarditis in high-risk patients undergoing 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 for 30 min before the procedure or operation; if necessary, after 6 hours, re-injected at a dose of 1 g.

    Children with severe and medium-heavy infections - intramuscularly 25-50 mg / kg 4 times a day; when meningitis daily dose is 100-200 mg / kg for 6-8 injections.

    Children over 4 years of age are prescribed 1-2 g / day; up to 1 year - at the rate of 100 mg / kg; 1-4 years - 100-150 mg / kg. The daily dose is divided into 4-6 receptions.

    Newborns weighing up to 2 kg - 25-50 mg / kg every 12 hours in the first week of life, then 50 mg / kg every 8 hours; newborns with a body weight of 2 kg and above - 50 mg / kg every 8 hours in the first week of life, then 50 mg / kg every 6 hours.

    Children for the prevention of bacterial endocarditis - 50 mg / kg for 30 minutes before the procedure; if necessary,after 6 hours, re-injected at a dose of 25 mg / kg. The duration of treatment depends on the severity of the disease (7-14 days or more).

    Preparation of solutions and administration. Solutions are prepared ex tempore.

    For the / m introduction, 2 ml of water for injections is added to the contents of the vial (500 mg). For IV injection - to the contents of the bottle (500 mg), add 5 ml of water for injection, injected iv slowly for 3-5 minutes.

    With a single dose exceeding 2 g, the drug is administered intravenously drip. To do this, 5 ml of water for injection are added to the contents of the vial (500 mg), the resulting solution is added to 125-250 ml of a 0.9% solution of sodium chloride or 5% solution of dextrose, injected at a rate of 60-80 drops per minute.

    Solutions used immediately after preparation, it is unacceptable to add other medicines to them.

    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 serum sickness , anaphylactic shock.

    From the digestive system: dysbacteriosis, gastritis, dry mouth, taste change, abdominal pain, vomiting, nausea, diarrhea, stomatitis, glossitis, increased activity of "liver" transaminases, pseudomembranous colitis.

    From the central nervous system (CNS): headache, tremor, convulsions (with high-dose therapy), agitation, aggressiveness, anxiety, confusion, behavior change, depression.

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

    Local reactions: pain and infiltrates at the sites of the / 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.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

    Overdose:

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

    Treatment: maintenance of 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; when injected iv introduce separately, observing a certain sequence, with as long a time interval between injections (infusions), or use separate intravenous catheters.

    Other bactericidal antibiotics (including aminoglycosides, vancomycin, rifampicin) with a joint application have a synergistic effect.

    Bacteriostatic medicinal products (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - have an antagonistic effect.

    Reduces the effectiveness of drugs, in the process of metabolism of which forms para-aminobenzoic acid, ethinyl estradiol (in the latter case, the risk of bleeding "breakthrough" increases, therefore it is recommended to use additional methods of contraception during ampicillin therapy).

    Drugs that block tubular secretion, 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).

    Allopurinol increases the risk of developing an "ampicillin" skin rash. Reduces clearance and increases the toxicity of methotrexate.

    If you are taking other drugs, consult a doctor.

    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, caution should be exercised in view of the possible development of pseudomembranous colitis caused by clostridium difficile. If the diagnosis of antibiotic-associated diarrhea or pseudomembranous colitis caused by clostridium difficile, it is established, immediately stop the introduction of ampicillin and prescribe the appropriate treatment.

    After the expiry date of the drug, unused vials should be carefully opened, the contents dissolved in a large amount of water and drained into the drain.

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

    Care should be taken when driving a car and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:Powder for solution for intravenous and intramuscular injection 0.25 g, 0.5 g.
    Packaging:

    0.25 g, 0.5 g of active substance in 10 ml vials.

    1 bottle with instructions for use in a pack of cardboard.

    10 bottles with instructions for use in a cardboard box.

    For hospital:

    - 50 bottles and 1 -5 instructions for use in a cardboard box;

    - 1 bottle with instructions for use (from 1 to 50 bottles with an equal number of instructions for use) in a cardboard box.

    Storage conditions:

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

    Keep out of the reach of children.

    After the expiry date of the drug, unused vials should be carefully opened, the contents dissolved in a large amount of water and drained into the drain.

    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-000658
    Date of registration:01.06.2010 / 11.09.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp21.08.2017
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