Bicillin-3® [Benzatin benzylpenicillin, benzylpenicillin]

Pharmacological properties

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 gonorrhoеae, 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 action of the drug.

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

Indications

Infections caused by microorganisms sensitive to the drug, in cases when it is necessary to maintain a constant concentration of the drug in the blood for a long time:

• infections of the respiratory tract and ENT organs: streptococcal pharyngitis and tonsillitis;
• urinary tract infections: syphilis;
• erysipelas;
• exacerbation of rheumatism.

Application

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

Bicillin-3 is administered only in oil. In / in the introduction of the drug is prohibited!

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

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

Before administering a suspension of Bicillin-3, you must make sure that the needle does not enter the blood vessel. If blood appears, the needle must be removed and the injection carried out in another place.

Contraindications

Hypersensitivity to β-lactam antibiotics (penicillins, cephalosporins, carbapenems) and Novocaine; hives; ba; allergic reactions, hay fever.

Side effects

On the part of the immune system: hypersensitivity reactions, including skin rashes, itching, fever, chills, arthralgia, swelling, urticaria, erythema multiforme, exfoliative dermatitis, contact dermatitis, anaphylactic or anaphylactoid reactions, including bronchial asthma, thrombocytopenia angioedema of angioedema, anaphylactic shock, which can be fatal in case of untimely and poor-quality medical care; serum sickness, possible reactions at the injection site.

On the part of the respiratory system: bronchospasm, laryngospasm.

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

From the digestive tract: nausea, vomiting, stomatitis, glossitis, staining of the tongue black, diarrhea, pseudomembranous colitis, hepatitis, stagnation of bile.

From the genitourinary system: interstitial nephritis.

From the cardiovascular system: fluctuations in blood pressure, impaired pump function of the myocardium, tachycardia.

On the part of the blood and lymphatic system: eosinophilia, positive Coombs test results, hemolytic anemia, leukopenia, neutropenia, thrombocytopenia, agranulocytosis.

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

Others: in debilitated patients, newborns, elderly people with prolonged treatment, superinfection may occur due to drug-resistant microflora (yeast-like fungi, gram-negative microorganisms). Patients undergoing treatment for syphilis may also experience a Yarish-Herksheimer reaction secondary to bacteriolysis, which is characterized by the following symptoms: fever, chills, myalgia, headache, exacerbation of skin symptoms, tachycardia, vasodilation with a change in blood pressure.

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

special instructions

Before starting treatment with bicillin-3, you should check the tolerance of the drug and make a test for tolerance of local anesthetics. it is necessary to find out whether reactions to group drugs (β-lactam and / or Novocaine) were noted with their preliminary use. in patients prone to allergic reactions, prescribe the drug with caution. when signs of allergic reactions appear, bicilin-3 should be discontinued and appropriate therapy prescribed.

In order to prevent the occurrence of adverse reactions should be carried out only in / in the introduction of the drug.

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

Severe and sometimes fatal cases of hypersensitivity (anaphylactic reactions) were observed in patients undergoing penicillin therapy. Such reactions occur more often in patients with a history of severe allergic reactions.

For the treatment of symptoms of an anaphylactic reaction, it may be necessary: ​​immediate administration of epinephrine, steroids (iv) and emergency treatment of respiratory failure.

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

Neutropenia was widespread in patients receiving high doses of β-lactams and in patients receiving treatment for 10 days or more. White blood cell monitoring is recommended for a long time during treatment with high doses.

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, the absorption of the active substance with a / m depot can be reduced.

In severe renal impairment, high doses of penicillin due to a neurotoxic effect can cause cerebral disorders, convulsions, coma.

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 high-dose therapy.

Long-term use of the drug can lead to the development of colonization of resistant microorganisms or yeast. Superinfection may occur, which requires careful monitoring of such patients.

In case of severe diarrhea characteristic of pseudomembranous colitis (in most cases caused by Clostridium difficile), it is recommended to stop the use of the drug and take appropriate measures. The use of drugs that inhibit peristalsis is contraindicated.In the treatment of sexually transmitted diseases with suspected syphilis before the start of therapy and within 4 months after its completion, a serological study is necessary.

To suppress or alleviate the Yarish-Herxheimer reaction, it is recommended that 50 mg of prednisolone or its equivalent be introduced at the first use of the drug.

In patients with syphilis with damage to the cardiovascular system, blood vessels and meninges, the Jarisch-Herxheimer reaction can be avoided by using prednisolone at 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 to form decomposition products and metabolites.

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

Use during pregnancy and lactation is contraindicated.

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

The ability to influence the reaction rate when driving vehicles and working with other mechanisms. It is recommended to refrain from activities that require the speed of psychomotor reactions (driving, working with potentially dangerous mechanisms), including possible adverse reactions from the nervous system (dizziness, headache, tinnitus).

Interactions

With simultaneous use with bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides), a synergistic effect is observed; with bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - 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 clearance and increases the toxicity of methotrexate.

With simultaneous use with allopurinol, the risk of developing allergic reactions increases.

Pharmacokinetic interaction. With the simultaneous use of diuretics, allopurinol, phenylbutazone, NSAIDs reduce tubular secretion and increase the concentration of penicillin.

It should be borne in mind the possibility of competitive inhibition of the process of elimination from the body with the simultaneous use of benzylpenicillin with anti-inflammatory and antipyretic drugs (indomethacin, phenylbutazone, salicylates in high doses). Acetylsalicylic acid, probenecid, thiazide diuretics, furosemide, ethacrylic acid increase T_½ benzylpenicillin, increasing its concentration in blood plasma, resulting in an increased risk of developing its toxic effect by affecting the tubular secretion of the kidneys. Allopurinol increases the risk of allergic reactions (skin rash).

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

With simultaneous use with methotrexate, the excretion of the latter decreases and the risk of its toxicity increases.

Penicillins can distort diagnostic tests, for example, determination of glucose in the urine using copper sulfate, direct antiglobulin test (Coombs test), some tests to determine serum proteins or protein in the urine. Penicillins can also distort the results of tests that use bacteria, such as the Guthrie phenylketonuria test, which uses Bacillus subtilis microorganisms.

Incompatibility. Do not mix Bicillin-3 suspension with other injection solutions.

It is not recommended to use Ringers solution or other sodium-containing solutions containing glucose as a solvent.

The drug is incompatible with metal ions and sympathomimetic amines.

Overdose

Possible toxic effects on the central nervous system, namely: reflex agitation, headache, nausea, vomiting, convulsions, myalgia, arthralgia, symptoms of meningism, coma. in such cases, the drug should be discontinued.

The treatment is symptomatic, including hemodialysis, peritoneal dialysis, special attention should be paid to restoring the water-electrolyte balance.

Storage conditions

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