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Procaine benzylpenicillin | CAS No: 54-35-3 | GMP-certified suppliers
A medication that provides prolonged antibacterial treatment for serious infections including syphilis, anthrax, pneumonia, and diphtheria with sustained systemic exposure.
Therapeutic categories
Primary indications
- For the treatment of a number of bacterial infections such as syphilis, anthrax, mouth infections, pneumonia and diphtheria
Product Snapshot
- Procaine benzylpenicillin is available as an intramuscular injection in suspension and powder forms for solution
- It is primarily indicated for the treatment of bacterial infections including syphilis, anthrax, mouth infections, pneumonia, and diphtheria
- This API is approved for human and veterinary use in the US and Canadian markets
Clinical Overview
Clinically, procaine benzylpenicillin is indicated for the treatment of various bacterial infections including syphilis, anthrax, respiratory tract infections such as pneumonia, diphtheria, and oropharyngeal infections. Its antibacterial activity is directed against penicillin-susceptible microorganisms, serving as a first-line agent in many clinical scenarios. The drug is also widely employed in veterinary medicine.
Pharmacodynamically, the active component benzylpenicillin acts as a bactericidal agent by inhibiting bacterial cell wall synthesis. Specifically, it interferes with the biosynthesis of peptidoglycan—a critical structural polymer in the bacterial cell wall—leading to osmotic instability and bacterial cell lysis. Mechanistically, once absorbed, procaine benzylpenicillin hydrolyzes to penicillin G, which binds penicillin-binding proteins (PBPs). This binding inhibits transpeptidase enzymes responsible for crosslinking peptide chains in peptidoglycan, ultimately triggering activation of autolytic enzymes and bacterial death.
Regarding absorption, distribution, metabolism, and excretion (ADME), the slow release from the injection site correlates with sustained plasma levels of penicillin G. The drug is primarily eliminated renally. Safety considerations include hypersensitivity reactions typical of beta-lactam antibiotics, as well as local injection site reactions mitigated by the presence of procaine as a local anesthetic.
Procaine benzylpenicillin belongs to the beta-lactam class of antibiotics, specifically beta-lactamase sensitive penicillins. Its procurement for pharmaceutical use requires attention to strict compliance with quality standards governing purity, potency, and batch consistency. Due to its veterinary and human medical applications, sourcing should ensure adherence to regulatory guidelines and verification of supply chain integrity to avoid contamination or degradation.
Identification & chemistry
| Generic name | Procaine benzylpenicillin |
|---|---|
| Molecule type | Small molecule |
| CAS | 54-35-3 |
| UNII | 1LW5K9CIR1 |
| DrugBank ID | DB09320 |
Pharmacology
| Summary | Procaine benzylpenicillin is a beta-lactam antibiotic that exerts bactericidal activity by inhibiting the synthesis of bacterial cell wall peptidoglycan. It binds to penicillin-binding proteins, disrupting transpeptidation and activating autolytic enzymes, leading to bacterial cell lysis. It is primarily used against penicillin-susceptible bacteria in various infections. |
|---|---|
| Mechanism of action | Procaine benzylpenicillin is hydrolyzed into penicillin G once it is released from the injection site. Penicillin G attaches to the penicillin-binding proteins on bacterial cell wall and inhibit the transpeptidation enzyme that crosslinks the peptide chains attached to the backbone of the peptidoglycan. The final bactericidal event involves the inactivation of an inhibitor of autolytic enzymes in the cell wall, leading to lysis of the bacterium . |
| Pharmacodynamics | It is an antibiotic against penicillin-susceptible microorganisms with bactericidal effect. Like all penicillins, procaine benzylpenicillin interferes with the synthesis of the bacterial cell wall peptidoglycan. It acts through the inhibition of biosynthesis of cell-wall peptidoglycan, rendering the cell wall osmotically unstable. It is part of the penicillin and beta lactam family of antibacterial drugs. |
ADME / PK
| Absorption | After intramuscular injection, it dissolves slowly at the site of injection, giving a plateau type of blood level at about 4 hours which falls slowly over a period of the next 15 to 20 hours. |
|---|---|
| Half-life | Intramuscular injection of benzylpenicillin has a plasma half-life of 30 minutes . |
| Protein binding | Approximately 60% of penicillin G is bound to serum protein. |
| Metabolism | Procaine is rapidly hydrolyzed by plasma esterases to nontoxic metabolites. |
| Route of elimination | The drug is rapidly and predominantly cleared via renal elimination, with 90% being through tubular secretion. Approximately 60 -90 % of a dose of parenteral penicillin G is excreted in the urine within 24 to 36 hours. |
| Volume of distribution | The drug is distributed throughout the body tissues in widely varying amounts and spinal fluid to a lesser degree. Highest levels are found in the kidneys with lesser amounts in the liver, skin, and intestines. It displays low solubility thus results in blood serum levels much lower but more prolonged than other parenteral penicillins. |
Formulation & handling
- Procaine benzylpenicillin is administered exclusively via intramuscular injection, available as suspensions and powders for solution.
- The compound is a small molecule dipeptide with moderate water solubility and a low logP, indicating balanced hydrophilicity for injectable formulations.
- Due to its peptide-like structure, stability considerations include protection from hydrolysis and maintenance of sterility during handling and formulation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has patent protection expiring in the US and Canada within the next 12 months, entering the late lifecycle phase with increasing generic competition across these markets. Product availability is established in both regions, reflecting a mature commercial presence. |
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| Markets | Canada, US |
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Supply Chain
| Supply chain summary | The manufacturing landscape for procaine benzylpenicillin involves several originator companies supplying branded products across the US and Canadian markets. Multiple branded formulations, including suspensions and injections, are available primarily in these regions. Patent expirations indicate the presence of existing generic competition within these markets. |
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Safety
| Toxicity | Procaine benzylpenicillin is associated with the pain at the injection site, blood clotting problems, and seizures. Treatment targeted against syphilis is often associated with Jarisch-Herxheimer reaction. The main unwanted effects are hypersensitivity reactions caused by the degradation products of penicillin, which combine with host protein and become antigenic. Other common adverse effects include skin rashes, fever and delayed serum sickness. Rare but fatal anaphylactic shock may occur. Oral LD50 values in mouse and rat are > 2000 mg/kg. Overdosage can cause convulsions, paralysis and even death. Emesis and gastric lavage may be of value if begun within a few hours of injection. Excessive blood concentrations can be lowered by haemodialysis . |
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- Procaine benzylpenicillin may induce hypersensitivity reactions, including rare but potentially fatal anaphylactic shock
- Appropriate precautions should be in place during handling
- Exposure is associated with injection site pain, coagulation disturbances, and neurological effects such as seizures at high doses
Procaine benzylpenicillin is a type of 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.
Procaine benzylpenicillin API manufacturers & distributors
Compare qualified Procaine benzylpenicillin API suppliers worldwide. We currently have 2 companies offering Procaine benzylpenicillin API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Arshine Pharmaceutical Co... | Distributor | China | China | BSE/TSE, CoA, GMP, MSDS, USDMF | 176 products |
| Sandoz | Producer | Austria | Unknown | CoA, USDMF | 58 products |
When sending a request, specify which Procaine 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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