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Бициллин-5

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Бициллин-5

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

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Overview of Бициллин-5

Quick Facts

Property Description
Active Ingredient Benzathine Benzylpenicillin & Benzylpenicillin Procaine
Form Powder for Suspension for Intramuscular Injection
Pharmacological Class Beta-Lactam Antibacterial, Combination of Natural Penicillins
General Purpose Provides long-acting systemic treatment against susceptible bacteria
Origin Derived (salts of natural Penicillin G)

What Type of Medicine is Бициллин-5?

Бициллин-5 is a prescription-only, long-acting Combination Antibiotic belonging to the pharmacological class of Beta-Lactam Antibacterials. It is specifically composed of two salts of the antibiotic Penicillin G (Benzylpenicillin) and is clinically utilized for its role in long-term prophylactic and systemic treatment strategies. The active compounds are ultimately derived from the structure of Natural Penicillins, which traces its origin to Penicillium molds, classifying it as a semi-synthetic compound engineered for systemic anti-bacterial action.

Composition and Depot Formulation of Бициллин-5

This medication is defined by its two key components: the very long-acting salt Benzathine Benzylpenicillin and the intermediate-acting salt Benzylpenicillin Procaine. The formulation is supplied as a sterile powder that is reconstituted to create an Intramuscular Suspension. The combination of these two low-solubility salts is the foundation of the drug's design, as it creates a "depot" at the injection site. These long-acting forms of penicillin are utilized in various global health protocols due to their pharmacological properties.

This depot mechanism ensures that the salts dissolve slowly, continuously releasing the active compound into the systemic circulation over many days. Furthermore, the inclusion of Procaine in one of the salts, which is a local anesthetic, serves the practical purpose of reducing the pain and discomfort associated with the necessary deep intramuscular injection.

General Therapeutic Purpose of the Long-Acting Penicillin

The primary therapeutic purpose of Бициллин-5 is to guarantee sustained therapeutic levels of the antibiotic in the bloodstream over an extended period. This design is beneficial in situations requiring consistent anti-bacterial coverage, such as the management of chronic infections caused by susceptible bacterial populations. The key functional advantage is the avoidance of frequent dosing, which maximizes adherence and provides continuous, reliable exposure to the anti-bacterial agent, leading to the resolution of the underlying infection.

Regulatory References

  1. World Health Organization confirms the essential nature of these long-acting forms of penicillin
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What side effects are possible with Бициллин-5?

Possible Side Effects and Safety Information

The safety profile of Бициллин-5 (Benzathine Benzylpenicillin / Penicillin G Procaine) is formally defined by regulatory authorities based on the nature and frequency of observed adverse reactions. The most critical safety constraint is that this product is strictly for deep intramuscular injection only; inadvertent intravenous administration is explicitly warned against due to the risk of severe neurovascular damage, cardiac arrest, and death.

Adverse Reaction Classifications

Side effects are classified by physiological system and frequency, as documented in official prescribing information.

Classification Aspect Example of Officially Documented Reactions
Common (e.g., >1/100 occurrences) Pain at the injection site, mild diarrhea, nausea.
Uncommon (e.g., >1/1,000 occurrences) Urticaria, vomiting, other non-severe allergic reactions.

Serious Adverse Reactions

The most significant safety concern is the risk of hypersensitivity reactions, which include immediate, life-threatening anaphylaxis and anaphylactic shock. Other serious, though rare, adverse reactions include Severe Cutaneous Adverse Reactions (SCARs) such as Stevens-Johnson syndrome (SJS) and Clostridioides difficile-associated diarrhea (CDAD), which may occur even long after treatment cessation.

Population and Context-Specific Safety

Neurotoxicity is a documented risk, which increases in patients with renal impairment. Furthermore, patients being treated for syphilis may experience a Jarisch-Herxheimer reaction, a transient systemic response that typically occurs within the first 12 hours of the initial dose.

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Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory documents specify that overdose of the active ingredients in Бициллин-5 may result in manifestations of neuromuscular hyperirritability. Documented signs include twitching, confusion, and gastrointestinal disturbances such as nausea, vomiting, and diarrhea. The most severe, life-threatening outcomes involve the Central Nervous System (CNS), potentially leading to convulsive seizures and coma.

Documented Overdose Profile

  • Physiological Systems Affected: Primarily the Central Nervous System (CNS) and Gastrointestinal (GI) systems.
  • Risk Factors: There is an increased risk of toxicity for patients with impaired renal function (kidney disease) due to reduced drug clearance and heightened potential for CNS effects.
  • Management Constraint: The official labeling confirms that no specific antidote is known for this overdose.

Emergency Response and Management

Regulatory guidance mandates seeking immediate medical attention for suspected severe overdose. Individuals must contact emergency services immediately if the affected person collapses, has a seizure, or has difficulty breathing.

Management is defined as symptomatic and supportive treatment, which includes measures for controlling convulsions and correcting fluid or electrolyte imbalances. For severe cases, hemodialysis is an officially described procedural option that may be considered to accelerate the removal of Benzylpenicillin from the circulation.

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Therapeutic Uses of Бициллин-5

Quick Facts: Uses and Domains

  • Treatment: Certain bacterial infections susceptible to penicillin G.
  • Prophylaxis: Prevention of recurrent rheumatic fever and related conditions.
  • Specific Conditions: Management of venereal diseases, including syphilis.

Бициллин-5 (Penicillin G Benzathine) is indicated as a therapeutic option for treating a number of established bacterial infections. Its primary use includes the management of infections caused by susceptible microorganisms, such as mild to moderate upper respiratory tract infections associated with streptococci.

This medication is also applied in the treatment of specific venereal infections, including primary, secondary, and latent syphilis, as well as yaws, bejel, and pinta. Treatment is intended to address the underlying bacterial cause of these conditions and may assist in clinical improvement.

Beyond treating active infections, this formulation is also employed as a prophylactic measure. It is generally recommended for the long-term secondary prevention of acute rheumatic fever and/or chorea. Furthermore, it is used for follow-up prophylactic therapy for rheumatic heart disease and acute glomerulonephritis.

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Eligibility and Restrictions for Use

Who can and cannot use Бициллин-5?

Eligibility for Бициллин-5 (Benzathine and Procaine Penicillin G) is strictly defined by regulatory documents, focusing primarily on hypersensitivity status, age, and organ function.


Contraindicated Populations

Category Non-Eligibility Status
Penicillin Hypersensitivity Absolute Contraindication for patients with a history of allergy to any penicillin antibiotic or Benzylpenicillin.
Procaine Allergy Absolute Contraindication due to hypersensitivity to the Procaine component of the formulation.

Age- and Condition-Based Restrictions

Population Group Regulatory Limitation
Renal Impairment Caution advised; use is restricted due to delayed clearance, risking drug accumulation.
Infants under 6 months Caution advised due to the higher risk of methemoglobinemia linked to the Procaine component.
Asthma/Severe Allergies Caution advised due to an increased risk of severe hypersensitivity reactions.
Pregnancy/Lactation Permitted when clearly indicated; caution during lactation due to drug excretion in breast milk.

Use is established in adults, adolescents, and older children for labeled indications. For older adults, use is established but caution is advised due to the increased likelihood of underlying organ impairment.

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What should I know about interactions with other medicines?

️ Interactions with other medicines and products — Official Regulatory Information

The interaction profile for Бициллин-5 (Penicillin G salts) is derived exclusively from documented information in governmental regulatory sources, classifying interactions based on their effect on drug disposition and activity.


Interaction Scope

Detail Content (Strictly Label-Based)
Medicinal product categories with documented interactions: Bacteriostatic Antibiotics; Drugs cleared by renal tubular secretion; Uricosuric Agents.
Specific interacting medicines (if explicitly listed): Probenecid, Methotrexate, Tetracycline.
Mechanistic basis of interactions (only if stated in label): Inhibition of renal tubular secretion; Interference with bactericidal action.
Timing-based interaction rules (if applicable): No mandatory timing separation rules are explicitly documented.
Population-specific interaction notes (if applicable): Combination with Probenecid is not recommended in the presence of known renal impairment.
Interaction-related restrictions: Avoid co-administration with bacteriostatic antibiotics. Do not combine with Methotrexate.

Interaction Classifications

Classification Detail Content (Strictly Label-Based)
Interaction severity classification: Contraindicated/Avoidance Advised (Tetracyclines, Methotrexate); Clinically Significant / Intentional Alteration (Probenecid).
Regulatory basis: U.S. FDA Prescribing Information, U.S. FDA DailyMed.

Resulting Interaction Structure

Official Interaction Statements:

  • Co-administration with Tetracyclines may interfere with the bactericidal action of penicillin.
  • Penicillins reduce the renal clearance of Methotrexate, which can lead to increased serum concentrations and subsequent toxicity.
  • Probenecid inhibits the renal tubular secretion of penicillin and is officially documented to elevate and prolong penicillin plasma levels, resulting in a mathbf2 -fold to mathbf4 -fold elevation of drug exposure.
  • The use of Probenecid in conjunction with penicillin is not recommended in known renal impairment.

Connection to the overall interaction profile: Regulatory documents define the interaction structure by identifying agents that alter drug exposure via competitive inhibition of renal tubular secretion (Probenecid and Methotrexate) and agents that cause pharmacodynamic antagonism (Tetracyclines). This profile explicitly documents interactions that require avoidance alongside one interaction that is leveraged intentionally to increase concentration.

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Mechanism of Action

Core Action: Irreversible Blockade of Cell Wall Construction

The primary mechanism of Бициллин-5 involves the active molecule, Benzylpenicillin, acting as an irreversible inhibitor of crucial bacterial enzymes known as Penicillin-Binding Proteins (PBPs). This molecular interaction permanently halts the final, cross-linking step of peptidoglycan synthesis, which is essential for building the rigid bacterial cell wall. This targeted failure in structural integrity leads directly to bacterial lysis (bursting) under its own osmotic pressure.


⏳ Sustained Release for Prolonged Mechanism Engagement

The combination of two salts of Benzylpenicillin is a delivery strategy designed to ensure the continuous engagement of the bactericidal mechanism. By forming a depot at the injection site, the active compound is released into the system slowly and consistently over a long duration. This sustained, high-level exposure maximizes the Time above Minimum Inhibitory Concentration (T > MIC), supporting a prolonged, continuous PBP inhibition in the systemic circulation. Additionally, the Procaine component provides a separate mechanism: the Procaine blockade of local sodium channels modulates nociceptive signaling at the injection site.


️ Mechanistic Limitations and Enzymatic Override

The efficacy of this cell wall inhibition mechanism is constrained by bacterial resistance factors. The most critical constraint occurs when bacteria produce the enzyme beta-Lactamase, which chemically destroys the beta-lactam ring, eliminating the drug's ability to inhibit the PBPs. The mechanism is also physiologically ineffective against pathogens that naturally lack the peptidoglycan target.

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Dosage and Administration Information

Administration and Precautions for Benzathine Benzylpenicillin (Bicillin-5)

Benzathine benzylpenicillin, which includes the formulation known as Bicillin-5, is a long-acting injectable antibiotic indicated for the treatment and prophylaxis of specific bacterial infections, such as streptococcal respiratory infections and syphilis. Its administration requires strict adherence to intramuscular (IM) injection technique.

Method of Administration

  • Route: Bicillin-5 is strictly for deep intramuscular (IM) injection only. DO NOT inject intravenously (IV), near an artery or nerve, or admix with other intravenous solutions. Inadvertent IV administration has been associated with severe reactions, including cardiorespiratory arrest and death.
  • Injection Site: The recommended site for injection in adults is the upper, outer quadrant of the buttock (dorsogluteal) or the ventrogluteal site. For infants and small children, the mid-lateral aspect of the thigh may be preferable. The injection site should be varied when repeated doses are given.
  • Technique: The suspension is viscous and should be administered slowly and steadily. Aspiration must be performed prior to injection to ensure the needle has not entered a blood vessel.

Key Patient Considerations

  • Allergies: Before administration, a careful inquiry must be made regarding any history of hypersensitivity reactions to penicillins, cephalosporins, or other allergens, as serious and potentially fatal anaphylactic reactions are possible. The drug is contraindicated in patients with a previous penicillin allergy.
  • Completion of Therapy: Even if symptoms improve early, the medication must be used exactly as directed by a healthcare provider to ensure complete eradication of the infection and to minimize the risk of developing drug-resistant bacteria.
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Recent Clinical Evidence

Research Evidence / Overview of Studies for Бициллин-5

The research base for the long-acting penicillin G component of Бициллин-5 primarily consists of clinical evaluations focusing on two major indications: studies examining patterns related to the frequency of recurrent rheumatic fever and treating syphilis. The evidence generally comes from a mix of Randomized Controlled Trials (RCTs), long-term observational studies, and comprehensive reviews of existing findings, all aimed at understanding clinical patterns and outcomes.


Evidence for Use in Secondary Prevention of Rheumatic Fever Recurrence

Research has extensively explored the use of long-acting penicillin in studies examining patterns related to the frequency of future episodes in individuals who have already experienced Acute Rheumatic Fever (ARF). Studies utilized systematic reviews and long-term prospective observational cohort studies to follow patient groups, often including children and adolescents, for extended periods. Studies report that measurements of RF recurrences observed in patient groups were low during the observation period. Pharmacokinetic studies described serum penicillin concentrations that were observed to be above established threshold levels for extended durations following injection. Overall, the available data for this indication is classified as supported by Moderate certainty evidence.


Evidence for Use in Syphilis Treatment

The clinical evidence for treating syphilis was evaluated in Randomized Controlled Trials (RCTs) and various clinical and serologic follow-up studies. Research examined treatment outcomes in cohorts of Adults with primary, secondary, and latent syphilis, including subgroups like Pregnant Women and individuals living with HIV. Trials for early syphilis reported serologic patterns that were measured during the study period. The evidence supporting the single-dose regimen for early stages is generally classified as High. Regimens for late-stage latent syphilis were often based on theoretical considerations or older clinical data.


Research Gaps and Uncertainties

Researchers note that evidence quality varies across studies, and findings were mixed for high-level outcomes such as effects on mortality. There is limited information for long-term outcomes related to the progression of established Rheumatic Heart Disease, meaning the research is ongoing in this area. Additionally, the evidence base for certain dosing regimens (e.g., multi-dose for latent syphilis) is described as largely theoretical or based on older studies, suggesting that the certainty remains low for these specific protocols. These research limitations highlight what is known—and what is still uncertain—about the long-acting penicillin formulation.

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Frequently Asked Questions (FAQ)

Common questions about Бициллин-5 (FAQ)

Q: How long does the effect of one injection of Бициллин-5 usually last?

A: This medication is formulated to achieve a long-lasting effect, designed to maintain continuous therapeutic levels in the bloodstream. Official information indicates that measurable concentrations of the active drug are typically sustained for up to 28 days (four weeks) following a single deep intramuscular injection.

Q: What kind of bacteria is Бициллин-5 effective against?

A: The active substance in this medicine, Penicillin G, is officially classified as a narrow-spectrum antibiotic. This means it is active against specific types of susceptible bacteria, primarily many Gram-positive bacteria, including most Streptococci. It is generally not effective against bacteria that have developed resistance by producing the beta-Lactamase enzyme.

Q: Can Бициллин-5 affect my kidney function over time?

A: The active ingredient is primarily cleared from the body by the kidneys. Official documents indicate that high serum concentrations, such as those that can occur in patients with pre-existing renal impairment (kidney issues), may increase the risk of neurological toxicity. Nephropathy (kidney damage) has been reported in rare cases as an adverse reaction.

Q: How quickly does the antibiotic start working in the body after the injection?

A: The formulation is specifically designed for a slow, sustained release from the injection site. Because of this 'depot' effect, the active drug gradually enters the bloodstream, and therapeutic levels are typically detectable within 1 to 2 days following the intramuscular injection.

Q: Can I drink alcohol while receiving treatment with Бициллин-5?

A: Official regulatory labels for this specific medication do not typically list a direct chemical interaction with alcohol. However, official health advisories often note that alcohol consumption can potentially exacerbate common side effects of antibiotics, such as nausea or dizziness, and may interfere with general recovery from illness.

Q: Are there any common foods that should be avoided with Бициллин-5?

A: According to official regulatory documents, there are no specific food restrictions or dietary guidelines that need to be followed to ensure the medicine's effectiveness or safety.

Q: Can I take pain relievers like ibuprofen while being treated with Бициллин-5?

A: The specific drug label information does not explicitly name Ibuprofen. However, some literature and regulatory guidance note that certain non-steroidal anti-inflammatory drugs (NSAIDs) may potentially alter how the penicillin component is cleared by the kidneys, which could affect the drug’s concentration in the blood.

Q: Does Бициллин-5 interact with blood thinners or anticoagulants?

A: Yes, official sources advise caution, as penicillins may increase the effect of oral anticoagulants (blood thinners). This potential effect could increase the risk of bleeding. Official guidance indicates that close monitoring of blood clotting tests may be necessary if these medications are used together.

Q: Does taking certain supplements or vitamins impact the effectiveness of Бициллин-5?

A: Official regulatory documents do not list any specific vitamin or herbal supplements that are known to chemically interfere with the drug’s effectiveness or its concentrations in the blood.

Q: What does 'benzathine benzylpenicillin' mean in simple terms?

A: This term refers to a salt form of the antibiotic Penicillin G (also called Benzylpenicillin). The 'Benzathine' component makes the salt nearly insoluble in water, allowing it to form a depot in the muscle. This mechanism is essential for providing the slow, long-lasting release of the active drug.

Q: Where can I find published studies about the long-term safety of Бициллин-5?

A: Information is summarized on government health sites like the NIH's MedlinePlus or other national clinical resources. Additionally, the FDA drug label often contains a Reference section listing the key clinical studies that support its approval and long-term use.

Q: How long does it take for the drug to clear out of the system?

A: Due to its design for slow release over a month, the drug and its active metabolites may remain detectable in the body for a considerable time. Elimination depends largely on kidney function; delayed clearance is a specific warning for patients with renal impairment.

Q: Are there different doses of Бициллин-5, or is it always the same?

A: Official regulatory guidelines indicate that the dosage of this medication is not always the same. Dosing can vary depending on the specific condition being treated (e.g., syphilis treatment versus rheumatic fever prevention) and the patient population (e.g., adults versus children).

Q: Does Бициллин-5 treatment require any special laboratory tests?

A: While no routine test is mandated for every patient, regulatory documents advise that certain monitoring should be performed for patients undergoing long-term therapy. This includes monitoring of renal (kidney) and hematopoietic (blood) function.

Q: Can a rash appear several days after the Бициллин-5 injection?

A: Yes, regulatory documents describe that certain delayed allergic reactions (such as urticaria or serum sickness-like reactions) can appear days after the injection. Serious skin reactions, including Severe Cutaneous Adverse Reactions (SCARs), have also been reported.

Q: Is a fever after the injection considered a normal side effect?

A: Fever is listed as a potential symptom of general hypersensitivity reactions (allergic reactions). It is also a characteristic symptom of the temporary Jarisch-Herxheimer reaction observed in some patients treated for syphilis.

Q: Does Бициллин-5 affect birth control pills?

A: Official regulatory labels do not list hormonal contraceptives as a specific contraindication or interaction. Some authorities suggest consulting a healthcare professional regarding hormonal contraceptive efficacy when using any antibiotic.

Q: Can taking Бициллин-5 make you feel unusually tired?

A: Fatigue and asthenia (abnormal physical weakness or lack of energy) are listed among the reported adverse reactions in official prescribing information. These symptoms are sometimes noted as part of generalized hypersensitivity reactions (allergic responses).

Q: What is the general success rate mentioned in research for its main uses?

A: Regulatory summaries cite studies showing a high evidence classification (e.g., High certainty) for specific uses like early syphilis treatment. For rheumatic fever prevention, research reports a low frequency of recurrence measurements when the medication is administered according to protocol.

Q: Can I drive immediately after receiving a Бициллин-5 shot?

A: Official documents state that the drug may cause adverse reactions that can affect alertness, such as dizziness, confusion, or somnolence (drowsiness). Patients who experience these effects are cautioned against driving or operating machinery.

Q: What if I experience dizziness after the injection?

A: Dizziness is documented in official safety information as a reported adverse reaction. It is also noted as a symptom of a transient central nervous system syndrome (Hoigne's syndrome) that may be reported after administration.

Q: What are the general guidelines for its use in patients with heart conditions?

A: While the medication is frequently used in the prevention of Rheumatic Heart Disease (a heart condition), official warnings note that acute myocardial ischemia (a type of heart event) has been reported as part of a severe allergic reaction. Patients with existing heart conditions may require careful monitoring.

Q: Is a small lump or hardness at the injection site common?

A: Yes, local reactions at the injection site are commonly reported adverse effects. Official adverse reaction lists explicitly include a lump, pain, inflammation, and induration (hardness) in the area where the medication was administered.

Q: Are there specific instructions for travel if I need a Бициллин-5 shot?

A: Official storage instructions mandate that the dry powder formulation must be protected from temperatures exceeding 25 C and from light. Regulatory authorities emphasize the need to maintain proper storage conditions for the product at all times, including during transport, to preserve its quality and effectiveness.

Q: Is the penicillin component considered a narrow or broad-spectrum antibiotic?

A: The active substance, Penicillin G (Benzylpenicillin), is officially classified in regulatory documents as a narrow-spectrum antibiotic. This classification means it is active against a limited, specific range of susceptible Gram-positive bacteria.

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How should Бициллин-5 be stored and disposed of?

Storage and Disposal of Бициллин-5 (Dry Powder)


Storage Conditions

Бициллин-5 (Benzathine Benzylpenicillin and Benzylpenicillin Procaine) as a dry powder must be stored in a dry place at a temperature not exceeding 25 C to maintain its labeled shelf life. It is mandatory to keep the product protected from light and stored in its original packaging.

Regulatory documents require the medicine to be stored out of the sight and reach of children.

Stability and Disposal

The prepared suspension for injection is not stable and must be used immediately after reconstitution; it is not subject to storage. For disposal, any unused or expired product must be discarded according to local and national regulations for pharmaceutical waste. Care must be taken to avoid environmental release.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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