Benzathine benzylpenicillin (Benzathini benzylpenicillinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antibiotics

Included in the formulation
  • Bicillin®-1
    powder w / m 
    SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products     Russia
  • Retarpen®
    powder w / m 
    Sandoz GmbH     Austria
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    J.01.C.E.08   Benzathine benzylpenicillin

    Pharmacodynamics:

    Benzathine benzylpenicillin is an antibiotic of a group of biosynthetic penicillins.

    The mechanism of antimicrobial action is based on the disruption of the synthesis of peptidoglycan - mucopeptide of the cell membrane, which leads to inhibition of the synthesis of the cell wall of the microorganism, suppression of growth and reproduction of bacteria.

    It is active against gram-positive bacteria, gram-negative cocci, Actinomyces spp., Spirochaetaceae.

    Inactive against strains Staphylococcus spp., producing penicillinase.

    May have a prolonged effect.

    Pharmacokinetics:

    When intramuscular injection is slowly absorbed from the injection site, providing a prolonged effect.

    Badly penetrates the BBB.

    Metabolism

    It is metabolized by hydrolysis to benzylpenicillin. Due to prolonged absorption, benzylpenicillin is detected in the urine within 12 weeks after the administration of a single dose.

    Indications:

    Infectious and inflammatory diseases,caused by benzylpenicillin-susceptible pathogens, including syphilis, yaws, acute tonsillitis, scarlet fever, erysipelas, wound infection; prevention of exacerbations of rheumatism, scarlet fever (after contact with patients), erysipelas; prevention of infectious complications after tonsillectomy or extraction of teeth.

    ICD-10

    I.A30-A49.A38   Scarlet fever

    I.A30-A49.A46   Erys

    I.A50-A64.A50   Congenital syphilis

    I.A50-A64.A51   Early syphilis

    I.A50-A64.A52   Late syphilis

    I.A65-A69.A66   Yaws

    I.A65-A69.A67   Pinta [karate]

    IX.I00-I02.I00   Rheumatic fever without mention of involvement of the heart

    IX.I00-I02.I01   Rheumatic fever with involvement of the heart

    X.J00-J06.J03   Acute tonsillitis

    XIX.T79.T79.3   Post-traumatic wound infection, not elsewhere classified

    XXI.Z20-Z29.Z29.2   Another type of preventive chemotherapy

    Contraindications:

    Increased sensitivity of the body to benzathine benzylpenicillin and other antibiotics of the penicillin series.

    Carefully:

    With caution apply in patients with impaired renal function, in case of predisposition to allergic reactions (especially with drug allergies), with increased sensitivity to cephalosporins (due to the possibility of developing cross-allergy).

    Pregnancy and lactation:

    Use in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

    Benzathine benzylpenicillin penetrates the placental barrier, excreted in breast milk.

    If it is necessary to use during the lactation period, the question of stopping breastfeeding should be solved.

    Dosing and Administration:

    Enter intramuscularly. For adults, the single dose varies from 300,000 units to 2.4 million units, for children, a single dose of 5000-10,000 units / kg. The frequency and duration of application depend on the etiology of the disease.

    Side effects:

    From the side of the hematopoiesis system: anemia, thrombocytopenia, leukopenia, blood clotting disorders.

    Allergic reactions: urticaria, skin rash, rash on the mucous membranes, fever, joint pain, eosinophilia, angioedema, erythema multiforme, exfoliative dermatitis, stomatitis, glossitis, in exceptional cases - anaphylactic and anaphylactoid reactions.

    Effects due to chemotherapeutic action: with prolonged treatment, the development of superinfection with resistant microorganisms and fungi is possible.


    Overdose:

    In case of an overdose, symptomatic treatment should be given.

    Interaction:

    In combination with antibiotics, acting bacteriostatically, there is a decrease in the bactericidal effect of benzathine benzylpenicillin.

    When combined with non-steroidal anti-inflammatory drugs (in particular, with indomethacin, phenylbutazone and salicylates), one should keep in mind the possibility of developing a competitive inhibition of excretion of drugs from the body.

    Combination with other antibiotics is possible only with the expected synergy of action.

    Special instructions:

    It is not recommended to use for the treatment of neurosyphilis (since the necessary concentration in the blood plasma is not achieved).

    Intravenous and endolumbral administration is not allowed.

    Instructions
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