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Benzylpenicillin | CAS No: 61-33-6 | GMP-certified suppliers
A medication that treats severe bacterial infections like septicemia, meningitis, endocarditis, and pneumonia caused by penicillin-susceptible microorganisms requiring rapid, high antibiotic levels.
Therapeutic categories
Primary indications
- For use in the treatment of severe infections caused by penicillin G-susceptible microorganisms when rapid and high penicillin levels are required such as in the treatment of septicemia, meningitis, pericarditis, endocarditis and severe pneumonia
Product Snapshot
- Benzylpenicillin is available primarily as an injectable powder for solution or suspension, intended for parenteral administration via intravenous, intramuscular, intrathecal, and intrapleural routes
- It is indicated for the treatment of severe infections caused by penicillin G-susceptible microorganisms, including septicemia, meningitis, pericarditis, endocarditis, and severe pneumonia
- Benzylpenicillin is approved for use in the United States and Canada with both human and veterinary approvals noted
Clinical Overview
Pharmacodynamically, Benzylpenicillin exhibits bactericidal activity against a range of primarily gram-positive aerobic bacteria, including Streptococcus pneumoniae, groups A, B, C, and G streptococci, nonenterococcal group D streptococci, viridans group streptococci, and non-penicillinase producing staphylococci. It also displays activity against some gram-positive aerobic bacilli like Bacillus anthracis, Corynebacterium diphtheriae, and Erysipelothrix rhusiopathiae. Its efficacy against certain gram-negative organisms such as Neisseria meningitidis and Pasteurella species is limited but clinically relevant in specific contexts. Natural penicillins generally do not cover anaerobic infections. Resistance patterns vary regionally and should be considered when selecting therapy.
The mechanism of action involves targeting penicillin-binding proteins (PBPs) within the bacterial cell wall. By inhibiting the final stage of peptidoglycan synthesis, Benzylpenicillin compromises cell wall integrity, leading to bacterial cell lysis mediated by autolytic enzymes. This beta-lactam antibiotic is sensitive to hydrolysis by beta-lactamases but retains stability against several enzyme variants.
Key ADME characteristics include its poor oral absorption, necessitating parenteral administration to achieve therapeutic concentrations. It is subject to renal elimination and interacts with organic anion transporters such as OAT1 and OAT3, which influence its renal clearance.
Safety considerations require monitoring for hypersensitivity reactions typical of beta-lactams, including anaphylaxis and delayed-type hypersensitivity. Use in patients with known penicillin allergy is contraindicated. Dosage adjustment may be necessary in renal impairment.
Benzylpenicillin is available under various brand names worldwide and remains a critical agent in both human and veterinary medicine. For API sourcing, ensuring compliance with pharmacopoeial standards for assay, purity, and microbial limits is essential. The natural origin and chemical stability of Benzylpenicillin require controlled manufacturing conditions to prevent degradation and contamination.
Identification & chemistry
| Generic name | Benzylpenicillin |
|---|---|
| Molecule type | Small molecule |
| CAS | 61-33-6 |
| UNII | Q42T66VG0C |
| DrugBank ID | DB01053 |
Pharmacology
| Summary | Penicillin G is a beta-lactam antibiotic that targets penicillin-binding proteins (PBPs) to inhibit the final stage of bacterial cell wall synthesis, leading to cell lysis. It exhibits bactericidal activity primarily against susceptible gram-positive and some gram-negative bacteria. Its mechanism involves interference with bacterial cell wall autolytic enzymes, contributing to its antimicrobial effects. |
|---|---|
| Mechanism of action | By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, penicillin G inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that penicillin G interferes with an autolysin inhibitor. |
| Pharmacodynamics | Penicillin G is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Penicillin G has <i>in vitro</i> activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of penicillin G results from the inhibition of cell wall synthesis and is mediated through penicillin G binding to penicillin binding proteins (PBPs). Penicillin G is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Penicillin-binding protein 3 | Staphylococcus aureus (strain USA300) | inhibitor |
| Solute carrier family 22 member 8 | Humans | substrate, inhibitor |
| Solute carrier family 15 member 1 | Humans | substrate, inhibitor |
ADME / PK
| Absorption | Rapidly absorbed following both intramuscular and subcutaneous injection. Initial blood levels following parenteral administration are high but transient. Oral absorption in fasting, healthy humans is only about 15-30% as it is very susceptible to acid-catalyzed hydrolysis. |
|---|---|
| Half-life | In adults with normal renal function is reportedly 0.4–0.9 hours |
| Protein binding | Bind to serum proteins (45-68%), mainly albumin. |
| Metabolism | About 16-30% of an intramuscular dose is metabolized to penicilloic acid, an inactive metabolite. Small amounts of 6-aminopenicillanic acid have been recovered in the urine of patients on penicillin G. A small percentage of the drug appears to be hydroxylated into one or more active metabolites, which are also excreted via urine. |
| Route of elimination | Penicillin G is eliminated by the kidneys. Nonrenal clearance includes hepatic metabolism and, to a lesser extent, biliary excretion. |
| Volume of distribution | 0.53–0.67 L/kg in adults with normal renal function |
| Clearance | 560ml/min in healthy humans |
Formulation & handling
- Benzylpenicillin is primarily formulated for parenteral administration, including intramuscular and intravenous injections, with limited oral formulations due to low water solubility.
- As a small molecule dipeptide antibiotic, it requires reconstitution from powders for solution or suspension prior to injection to maintain stability and efficacy.
- Handling considerations include protection from moisture and exposure to heat to preserve stability, especially in its powder forms used for injectable preparations.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has patent protection expiring in the United States and Canada, with generic competition expected to increase following expiry. Current market presence reflects established use in these regions, transitioning towards greater availability of generic formulations. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Benzylpenicillin is supplied by multiple packagers servicing primarily the US and Canadian markets, with branded products such as Bicillin formulations present in these regions. The presence of several known pharmaceutical companies indicates a competitive originator landscape. Patent expirations have enabled or will enable generic competition, reflected by multiple generics available alongside branded options. |
|---|
Safety
| Toxicity | Oral LD<sub>50</sub> in rat is 8900 mg/kg [MSDS]. Neurological adverse reactions, including convulsions, may occur with the attainment of high CSF levels of beta-lactams. Neutropenia can occur if high doses are administered consistently for over 2 weeks. |
|---|
- Oral LD50 in rat is 8900 mg/kg, indicating low acute toxicity at typical exposure levels
- High cerebrospinal fluid (CSF) concentrations may induce neurological effects, including convulsions
- Prolonged high-dose administration (›2 weeks) can lead to neutropenia
Benzylpenicillin is a type of Penicillins
Penicillins belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) and play a crucial role in the treatment of various bacterial infections. They are a class of antibiotics derived from the fungus Penicillium, and are widely used in the pharmaceutical industry.
Penicillins exert their antibacterial effect by inhibiting the formation of bacterial cell walls. They target a specific enzyme, called transpeptidase, which is responsible for cross-linking the peptidoglycan chains in the bacterial cell wall. By blocking this process, penicillins weaken the cell wall, leading to its rupture and subsequent bacterial death.
These APIs are classified into several subclasses, such as penicillin G, penicillin V, and extended-spectrum penicillins. Each subclass has unique characteristics and mechanisms of action. Penicillin G, for example, is effective against a broad range of Gram-positive bacteria, while penicillin V is primarily used for oral administration.
The pharmaceutical industry produces penicillins through a fermentation process using Penicillium strains. The obtained penicillin products are then isolated, purified, and formulated into different dosage forms, including tablets, capsules, and injectables.
Penicillins have been instrumental in the treatment of various infections, including respiratory, skin, urinary tract, and sexually transmitted infections. However, it's essential to note that some bacteria have developed resistance to penicillins through different mechanisms, such as the production of beta-lactamases. As a result, pharmaceutical companies have developed combination therapies and modified penicillins to combat antibiotic resistance effectively.
In summary, penicillins are a vital subcategory of pharmaceutical APIs that provide effective treatment options for bacterial infections. Their diverse subclasses, mechanisms of action, and formulations contribute to their widespread use in the medical field.
Benzylpenicillin (Penicillins), classified under Antibacterials
Antibacterials, a category of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in combating bacterial infections. These APIs are chemical compounds that target and inhibit the growth or kill bacteria, helping to eliminate harmful bacterial pathogens from the body.
Antibacterials are essential for the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and more. They are commonly prescribed by healthcare professionals to combat both mild and severe bacterial infections.
Within the category of antibacterials, there are different classes and subclasses of APIs, each with distinct mechanisms of action and target bacteria. Some commonly used antibacterials include penicillins, cephalosporins, tetracyclines, macrolides, and fluoroquinolones. These APIs work by interfering with various aspects of bacterial cellular processes, such as cell wall synthesis, protein synthesis, DNA replication, or enzyme activity.
The development and production of antibacterial APIs require stringent quality control measures to ensure their safety, efficacy, and purity. Pharmaceutical manufacturers must adhere to Good Manufacturing Practices (GMP) and follow rigorous testing protocols to guarantee the quality and consistency of these APIs.
As bacterial resistance to antibiotics continues to be a significant concern, ongoing research and development efforts aim to discover and develop new antibacterial APIs. The evolution of antibacterials plays a crucial role in combating emerging bacterial strains and ensuring effective treatment options for infectious diseases.
In summary, antibacterials are a vital category of pharmaceutical APIs used to treat bacterial infections. They are designed to inhibit or kill bacteria, and their development requires strict adherence to quality control standards. By continually advancing research in this field, scientists and pharmaceutical companies can contribute to the ongoing battle against bacterial infections.
Benzylpenicillin API manufacturers & distributors
Compare qualified Benzylpenicillin API suppliers worldwide. We currently have 3 companies offering Benzylpenicillin API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| ACS Dobfar | Producer | Italy | Italy | CoA, USDMF | 36 products |
| CSPC Zhongnuo | Producer | China | China | CoA, USDMF | 6 products |
| Sandoz | Producer | Austria | Germany | CEP, CoA, FDA, GMP, USDMF | 58 products |
When sending a request, specify which Benzylpenicillin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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