Bicillin-3 powder for suspension for injection 600,000 IU in a bottle of 1 pc.

Pharmacodynamics

The drug has a bactericidal effect by inhibiting the synthesis of mucopeptides of the cell membrane of microorganisms. Bicillin-3 is active against gram-positive microorganisms (staphylococcus spp., except those producing penicillinase), streptococcus spp. (including streptococcus pneumoniae), corynebacterium diphtheriae, bacillus anthracis; gram-negative: neisseria gonorrhoeae, neisseria meningitidis, actinomyces israelii, as well as treponema spp., anaerobic spore-forming rods. Most gram-negative bacteria, mycobacteria, fungi, viruses, protozoa are resistant to the drug.

Pharmacokinetics

Bicillin-3 is a form of benzylpenicillin with prolonged action. When administered intramuscularly, a depot of the drug is formed in the muscle tissue. In the first hours after the injection, a high level of benzylpenicillin is created in the blood serum. Bicillin is well distributed in tissues and body fluids. High concentrations of the drug are achieved in the liver, kidneys, lungs, mucous membranes; it has the ability to penetrate fibrous tissues. Bicillin-3 is mainly excreted in the urine in a biologically active form (50-70%), in small quantities – with saliva, sweat, milk, bile.

Infections caused by microorganisms sensitive to the drug, in cases where long-term maintenance of a constant concentration of the drug in the blood is necessary:

• respiratory tract and ENT infections: streptococcal pharyngitis and tonsillitis;
• genitourinary system infections: syphilis;
• erysipelas;
• exacerbation of rheumatism.

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

Bicillin-3 is administered only in / m. Intravenous administration of the drug is prohibited!

The drug is administered at a dose of 600,000 IU once every 6 days. Usually the duration of treatment is 3-12 months, depending on the severity of the disease.

Rules for preparation and administration of the suspension. Prepare the suspension aseptically, immediately before use. Add 5-6 ml of 0.9% sodium chloride solution or sterile water for injection, or 0.25-0.5% novocaine solution to the vial, mix until a homogeneous suspension is formed and inject deeply i / m into the upper outer quadrant of the gluteal muscle (2 injections should be made into different buttocks).

Before injecting Bicillin-3 suspension, make sure that the needle has not entered a blood vessel. If blood appears, the needle must be removed and the injection performed in another place.

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

On the part of the immune system: hypersensitivity reactions, including skin rashes, itching, fever, chills, joint pain, edema, urticaria, erythema multiforme, exfoliative dermatitis, contact dermatitis; anaphylactic or anaphylactoid reactions, including bronchial asthma, 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, headache, tinnitus.

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

From the genitourinary system: interstitial nephritis.

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

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

Local reactions: reactions at the injection site, including pain.

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 syphilis of the cardiovascular system or conditions in which there is a serious risk of increased local damage, such as optic nerve atrophy.

Before starting treatment with Bicillin-3, the drug should be tested for tolerability and a local anesthetic tolerance test should be performed. It is necessary to find out whether there were any reactions to drugs of the group (β-lactams and/or novocaine) during their previous use. The drug should be prescribed with caution to patients prone to allergic reactions. If signs of allergic reactions appear, Bicillin-3 should be discontinued 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 require 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 has been reported to be 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 therapy.

The drug is not recommended for the treatment of patients with acute lymphocytic 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 i / m 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 prolonged 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.

Use during pregnancy and breastfeeding is contraindicated.

Children: The efficacy and safety of the drug in children have not been studied.

Ability to influence the reaction rate when driving vehicles or working with other mechanisms. It is recommended to refrain from activities that require quick reactions (driving vehicles, working with potentially dangerous mechanisms), taking into account possible adverse reactions from the nervous system (dizziness, headache, tinnitus).

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-3 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. Bicillin-3 suspension should not be mixed with other injection solutions.

It is not recommended to use Ringer’s solution or other sodium solutions containing glucose as a solvent.

The drug is incompatible with metal ions and sympathomimetic amines.

Possible toxic effects on the CNS, namely: 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.