Instructions Bicillin-5 powder for preparation of suspension for injection 1500000 units vial
Composition
active ingredient:
1 bottle contains: Bicillin-5, powder 1,500,000 IU (mixture of sterile benzathine benzylpenicillin (bicillin-1) – 1,200,000 IU, sterile benzylpenicillin novocaine salt – 300,000 IU).
Dosage form
Powder for suspension for injection.
Main physicochemical properties: white or white powder with a slightly yellowish tint.
Pharmacotherapeutic group
Antibacterial drugs for systemic use. Combinations of penicillins sensitive to the action of b-lactamases. ATX code J01C E30.
Pharmacological properties
Pharmacodynamics
The drug exhibits bactericidal action by inhibiting the synthesis of mucopeptides of the cell membrane of microorganisms. Active against gram-positive microorganisms: Staphylococcus spp. (except those that produce penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative: Neisseria gonorrhoae, Neisseria meningitidis, Actinomyces israelii, as well as Treponema spp., spore-forming anaerobic. Most gram-negative bacteria, mycobacteria, fungi, viruses, protozoa are resistant to the drug.
Pharmacokinetics
The drug exhibits 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 is excreted with sputum, sweat, saliva, tear fluid, and penetrates into breast milk.
Indication
Treatment of 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.
The use of Bicillin®-5 is particularly indicated for year-round prevention of rheumatism relapses in adults and children.
Contraindication
Hypersensitivity to β-lactam antibiotics (penicillins, cephalosporins, carbapenems), novocaine; Bronchial asthma, urticaria, hay fever and severe allergic reactions.
Interaction with other medicinal products and other types of interactions
When used simultaneously with bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides), synergism of action is noted; with bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamide, tetracyclines) - antagonism.
Bicillin®-5 reduces the effectiveness of oral contraceptives and ethinylestradiol (risk of breakthrough bleeding). It is not recommended to combine with nonsteroidal anti-inflammatory drugs. 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, 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 excretion from the body when benzylpenicillin is used simultaneously with anti-inflammatory and antipyretic agents (indomethacin, phenylbutazone, salicylates in high doses). Aspirin, probenecid, thiazide diuretics, furosemide, ethacrynic acid increase the half-life of benzylpenicillin, increasing its concentration in the blood plasma, as a result of which the risk of its toxic effect increases by affecting the tubular secretion of the kidneys. Allopurinol increases the risk of allergic reactions (skin rash).
Avoid simultaneous use with chloramphenicol, erythromycin, tetracycline, sulfonamides.
When used simultaneously with methotrexate, the excretion of the latter decreases 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 Bacillus subtilis.
Application features
It is necessary to find out whether there were any reactions to drugs of the group (β-lactam and/or novocaine) 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 adverse reactions, only intramuscular administration of the drug should be used.
In patients with known hypersensitivity to cephalosporins, the possibility of cross-allergy should be considered.
Treatment of symptoms of an anaphylactic reaction may require immediate administration of adrenaline, steroids (intravenously), 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 incidence was noted in patients treated for 10 days or more. Monitoring of white blood cells is recommended for prolonged periods of high-dose treatment.
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 patients with diabetes mellitus may have reduced absorption of the active substance from the intramuscular depot.
In severe renal dysfunction, large doses of penicillin can cause cerebral disorders, seizures, 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 (in most cases caused by Clostridium difficile), it is recommended to stop using the drug and take appropriate measures. The use of agents 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 in the stage manifested by damage to the cardiovascular system, blood vessels and meninges, the Jarisch-Herxheimer reaction can be avoided by using prednisolone 50 mg per 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 decompose with the formation of decomposition products and metabolites.
Skin contact with penicillins should be avoided as sensitization may occur.
Ability to influence reaction speed when driving vehicles or other mechanisms
There are currently no reports, but the possibility of adverse reactions from the central nervous and cardiovascular systems should be borne in mind.
Use during pregnancy or breastfeeding
There are no data on the use of the drug Bicillin®-5.
Method of administration and doses
Before administration, it is necessary to collect a patient's history of drug and local anesthetic tolerance!
Bicillin®-5 should be administered only intramuscularly! Intravenous administration of the drug is prohibited!
Children aged 3 to 8 years should be given Bicillin®-5 in a single dose of 600,000 IU once every 3 weeks.
Children over 8 years old – at a dose of 1,200,000 IU once every 4 weeks.
Adults should be administered a single dose of 1,500,000 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 ranges from 3 to 12 months.
Rules for preparation and administration of the suspension. Prepare the Bicillin®-5 suspension aseptically, immediately before use. Inject 9 ml of sterile water for injection or 0.9% sodium chloride solution or 0.25-0.5% novocaine solution into the vial with the drug under pressure. Mix the contents of the vial until a homogeneous suspension is formed. Inject the suspension deeply intramuscularly into the upper outer quadrant of the gluteal muscle (make 2 injections into different buttocks).
Before injecting Bicillin®-5 suspension, make sure that the needle has not entered a blood vessel. If blood appears, the needle must be removed and the injection carried out in another place.
Children
The drug should be prescribed to children over 3 years of age. When administering Bicillin®-5 to children, the preparation of a Bicillin®-5 suspension using novocaine solution is contraindicated.
Overdose
It manifests itself as a toxic effect on the central nervous system: reflex excitation, headache, nausea, vomiting, convulsions, myalgia, arthralgia, 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.
Adverse reactions
On the part of the immune system: skin rash, itching, edema, exfoliative dermatitis, erythema multiforme exudative, fever, arthralgia, urticaria, 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, tinnitus, headache.
On the part of the digestive 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 caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms) may occur. In patients undergoing treatment for syphilis, a Jarisch-Herxheimer reaction secondary to bacteriolysis may also occur, which is characterized by the following symptoms: fever, chills, myalgia, headache, exacerbation of skin symptoms, tachycardia, vasodilation with changes in blood pressure.
The reaction can be dangerous in cardiovascular syphilis or conditions in which there is a serious risk of increased local damage, such as optic nerve atrophy.
Expiration date
4 years.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C.
Packaging
1,500,000 IU per bottle.
Vacation category
According to the recipe.
Producer
PJSC "Kyivmedpreparat", Ukraine.
Location of the manufacturer and its business address
Ukraine, 01032, Kyiv, Saksaganskoho St., 139.
