Bicillin-5 powder for suspension for injection 1.5 million units in a bottle 1 pc.

Pharmacodynamics. The drug has a bactericidal effect by inhibiting the synthesis of mucopeptides of the cell membrane of microorganisms. Active against gram-positive microorganisms: staphylococcus spp. (In addition to producing penicillinase), streptococcus spp. (including streptococcus pneumoniae), corynebacterium diphtheriae, bacillus anthracis; gram-negative: neisseria gonorrhoae, neisseria meningitidis, actinomyces israelii, as well as treponema spp., anaerobic spore-forming.

Most gram-negative bacteria, mycobacteria, fungi, viruses, and protozoa are resistant to the drug.

Pharmacokinetics. The drug has a prolonged effect. When administered intramuscularly, a depot of the drug is formed in the muscle tissue. A high level of drug concentration is formed in the first hours after injection, the therapeutic concentration of benzylpenicillin is maintained in the blood for 28 days or more in the vast majority of patients (children and adults). It is excreted from the body mainly by the kidneys, a small amount of the drug – with sputum, then, saliva, tear fluid, penetrates into breast milk.

Treatment of infections caused by microorganisms sensitive to benzylpenicillin, if long-term maintenance of a constant concentration of the drug in the blood is necessary.

The use of Bicillin-5 is particularly indicated for year-round prevention of rheumatism relapses in adults and children.

Before administration, it is necessary to collect a patient’s history of drug and local anesthetic tolerance and conduct a preliminary intradermal drug and local anesthetic tolerance test!

Bicillin-5 is administered only intramuscularly! Intravenous administration is prohibited!

Children aged 3-8 years are given Bicillin-5 at a dose of 600 thousand units once every 3 weeks.

Children over 8 years old – at a dose of 1.2 million IU once every 4 weeks.

Adults are administered at a dose of 1.5 million IU once every 4 weeks.

More frequent injections of Bicillin-5 are contraindicated. Usually the duration of treatment depends on the severity of the disease and is 3-12 months.

Rules for preparation and administration of the suspension. The Bicillin-5 suspension is prepared aseptically, immediately before use: 9 ml of sterile water for injection or 0.9% sodium chloride solution or 0.25-0.5% novocaine solution is injected into the bottle with the drug under pressure. The contents of the bottle are mixed until a homogeneous suspension is formed. The suspension is injected deep into the upper outer quadrant of the buttock (2 injections are made into different buttocks).

Before injecting the suspension of Bicillin-5, it is necessary to make sure that the needle has not entered a blood vessel. If blood appears, the needle must be pulled out and the injection must be performed in another place.

Hypersensitivity to β-lactam antibiotics (penicillins, cephalosporins, carbapenems), procaine; urticaria, hay fever and severe allergic reactions.

On the part of the immune system: skin rashes, itching, edema, exfoliative dermatitis, erythema multiforme, fever, joint pain, urticaria, contact dermatitis, anaphylactic or anaphylactoid reactions, including urticaria; thrombocytopenic purpura, gastrointestinal symptoms, angioedema, anaphylactic shock, which can be fatal in case of untimely and poor-quality medical care; serum sickness, possible reactions at the injection site.

Respiratory system: bronchospasm, laryngospasm.

From the side of the central and peripheral nervous system: dizziness, tinnitus, headache.

Gastrointestinal tract: nausea, vomiting, stomatitis, glossitis, black tongue, diarrhea, pseudomembranous colitis, hepatitis, bile stasis.

From the genitourinary system: interstitial nephritis.

From the cardiovascular system: impaired myocardial pumping function, blood pressure fluctuations, tachycardia.

Blood and lymphatic system disorders: positive Coombs test, hemolytic anemia, leukopenia, neutropenia, thrombocytopenia, agranulocytosis, eosinophilia.

Local reactions: possible soreness at the injection site.

Others: in debilitated patients, newborns, and the elderly, with prolonged treatment, superinfection may occur caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms). In patients undergoing treatment for syphilis, a Jarisch-Herxheimer reaction may also occur a second time to bacteriolysis, which is characterized by the following symptoms: fever, chills, muscle pain, headache, exacerbation of skin symptoms, tachycardia, vasodilation with changes in blood pressure.

The reaction can be dangerous in syphilitic lesions of the cardiovascular system or conditions in which there is a serious risk of increased local damage, for example, optic nerve atrophy.

It is necessary to find out whether there were any reactions to drugs of the group (β-lactams and/or procaine) during their previous use. Patients prone to allergic reactions should be prescribed the drug with caution. If signs of allergic reactions appear, Bicillin-5 should be canceled and appropriate therapy should be prescribed.

In order to prevent the occurrence of adverse reactions, only intravenous administration of the drug should be carried out.

In patients with hypersensitivity to cephalosporins, the possibility of cross-allergy should be considered.

Severe and sometimes fatal cases of hypersensitivity (anaphylactic reactions) have been observed in patients receiving penicillin therapy. Such reactions occur more frequently in patients with a known history of severe allergic reactions.

Treatment of symptoms of an anaphylactic reaction may include immediate administration of adrenaline, steroids (intravenous), and emergency treatment for respiratory failure.

The drug should be used with extreme caution in patients with hay fever, urticaria, and other allergic diseases.

Neutropenia was widespread in patients receiving high doses of β-lactams and in patients treated for 10 days or more. Monitoring of leukocytes is recommended for prolonged periods of high-dose treatment.

The drug is not recommended for the treatment of patients with acute lymphoblastic leukemia or infectious mononucleosis due to the increased risk of erythematous skin rashes. It should be borne in mind that in patients with diabetes mellitus, absorption of the active substance from the intramuscular depot may be reduced.

In severe renal dysfunction, high doses of penicillin can cause cerebral disorders, convulsions, and coma due to neurotoxic effects.

Caution should be exercised when using the drug in patients with severe cardiopathy, hypovolemia, epilepsy, impaired renal or hepatic function. Hepatic, renal and hematological status should be monitored during long-term therapy with high doses.

Prolonged use of the drug may lead to the development of colonization with resistant microorganisms or yeasts. Superinfection is possible, which requires careful monitoring of such patients.

In the event of severe diarrhea typical of pseudomembranous colitis (most often caused by Clostridium difficile), it is recommended to stop using the drug and take appropriate measures. The use of drugs that inhibit peristalsis is contraindicated. In the treatment of venereal diseases with suspected syphilis, a serological test should be performed before starting therapy and within 4 months after its completion.

To suppress or alleviate the Jarisch-Herxheimer reaction, it is recommended to administer 50 mg of prednisolone or its equivalent when the drug is first used.

In patients with syphilis with damage to the cardiovascular system, blood vessels and meninges, the Jarisch-Herxheimer reaction can be avoided by using prednisolone 50 mg/day or an equivalent steroid for 1-2 weeks. Freshly prepared solutions for injection or infusion should be used immediately. Even when stored in a refrigerator, aqueous solutions of benzylpenicillin sodium salt decompose with the formation of decomposition products and metabolites.

Skin contact with penicillins should be avoided as sensitization may occur.

Pregnancy and breastfeeding. There are no data on the use of the drug Bicillin-5.

Children. The drug is prescribed to children over 3 years of age. When administering Bicillin-5 to children under 18 years of age, the preparation of a Bicillin-5 suspension using novocaine solution is contraindicated.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. There are currently no reports, but the possibility of adverse reactions from the central nervous and cardiovascular systems should be taken into account.

When used simultaneously with bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides), synergism of action is noted; with bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracycline) – antagonism.

Bicillin-5 reduces the effectiveness of oral contraceptives and ethinyl estradiol (risk of bleeding). It is not recommended to combine with NSAIDs. Benzylpenicillin reduces the clearance and increases the toxicity of methotrexate.

When used simultaneously with allopurinol, the risk of allergic reactions increases.

Pharmacokinetic interaction. With simultaneous use of diuretics, allopurinol, phenylbutazone, nonsteroidal anti-inflammatory drugs reduce tubular secretion and increase the concentration of penicillin.

It should be borne in mind the possibility of competitive inhibition of the process of excretion from the body when penicillin is used simultaneously with anti-inflammatory and antipyretic drugs (indomethacin, phenylbutazone, salicylates in high doses). Acetylsalicylic acid, probenecid, thiazide diuretics, furosemide, ethacrynic acid increase T _½ of benzylpenicillin, increasing its concentration in the blood plasma, as a result of which the risk of developing its toxic effect by affecting the tubular secretion of the kidneys increases. Allopurinol increases the risk of developing allergic reactions (skin rash).

Avoid simultaneous use with chloramphenicol, erythromycin, tetracycline, sulfonamides.

When used simultaneously with methotrexate, the excretion of the latter is reduced and the risk of its toxicity increases.

Penicillins may interfere with diagnostic tests, such as the copper sulfate urine glucose test, the direct antiglobulin test (Coombs’ test), and some tests for serum protein or protein in urine. Penicillins may also interfere with tests that use bacteria, such as the Guthrie test for phenylketonuria, which uses the organism Bacillus subtilis.

Incompatibility. Do not mix Bicillin-5 solution with other injection solutions.

It manifests itself as a toxic effect on the CNS: reflex excitation, headache, nausea, vomiting, convulsions, muscle pain, joint pain, symptoms of meningism, coma. In such cases, the administration of the drug should be discontinued.

Treatment is symptomatic, includes hemodialysis, peritoneal dialysis, and special attention should be paid to restoring water and electrolyte balance.

In the original packaging at a temperature not exceeding 25°C.