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- Chloramphenicol Succinate
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Chloramphenicol succinate | CAS No: 3544-94-3 | GMP-certified suppliers
A medication that treats serious bacterial infections resistant to alternative therapies, requiring careful monitoring due to its narrow therapeutic index and safety considerations.
Therapeutic categories
Primary indications
- Chloramphenicol succinate is indicated to treat serious and susceptible bacterial infections where less dangerous drugs are ineffective or contraindicated
Product Snapshot
- Chloramphenicol succinate is available as injectable formulations including lyophilized powder and powder for solution
- It is primarily used for the treatment of serious bacterial infections resistant to other therapies
- The product is approved in key regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, chloramphenicol succinate itself exhibits limited antibacterial activity. It undergoes in vivo hydrolysis to release the active moiety chloramphenicol. Chloramphenicol exerts its antibacterial effect by binding specifically to the 23S rRNA region of the 50S bacterial ribosomal subunit, notably at residues A2451 and A2452. This binding inhibits peptidyl transferase activity, thereby preventing peptide bond formation and halting protein synthesis. As a result, bacterial translation is impaired, leading to bacteriostatic effects. The structural similarity of chloramphenicol to uridine-5’-phosphate underlies its ribosomal interaction.
Key ADME parameters include moderate duration of action and metabolism predominantly through hydrolysis of the succinate ester. The therapeutic index is narrow, calling for careful dosing and monitoring. Chloramphenicol and its prodrug form are substrates of P-glycoprotein transporters, which may influence distribution and excretion.
A critical safety consideration is the risk of serious and potentially fatal blood dyscrasias, including aplastic anemia and other bone marrow toxicities. The frequency and severity of these adverse effects have led to a decline in widespread use. Clinical dosing requires vigilant patient monitoring with education on potential hematologic toxicity.
Chloramphenicol succinate belongs chemically to the class of nitrobenzenes and benzene derivatives, with additional classification as narrow therapeutic index drugs. Historically approved since 1959, its utility remains confined to specific, carefully selected cases.
When sourcing chloramphenicol succinate API, strict adherence to pharmacopeial quality standards and regulatory compliance is essential due to its toxicity profile. Reliable suppliers should provide comprehensive certificates of analysis, batch-to-batch consistency data, and evidence of manufacturing according to current Good Manufacturing Practices (cGMP). Special attention should be given to impurity profiling and stability to ensure safe and effective API for pharmaceutical formulation.
Identification & chemistry
| Generic name | Chloramphenicol succinate |
|---|---|
| Molecule type | Small molecule |
| CAS | 3544-94-3 |
| UNII | ZCX619U9A1 |
| DrugBank ID | DB07565 |
Pharmacology
| Summary | Chloramphenicol succinate is a prodrug that is hydrolyzed to chloramphenicol, which inhibits bacterial protein synthesis by binding to the 23S rRNA of the 50S ribosomal subunit. This binding prevents translation, exerting a bacteriostatic effect against susceptible bacteria. It is used to treat serious bacterial infections when alternative therapies are ineffective or contraindicated. |
|---|---|
| Mechanism of action | Chloramphenicol succinate is hydrolyzed into the active chloramphenicol. Chloramphenicol resembles uridine-5'-phosphate. It binds to the residues A2451 and A2452 in the 23S rRNA of the 50S ribosomal subunit of _E. coli_, which prevents translation. |
| Pharmacodynamics | Chloramphenicol succinate is a prodrug of chloramphenicol, which binds to bacterial ribosomes and prevents translation. It has a narrow therapeutic index and a moderate duration of action. Patients should be counselled regarding the risk of serious fatal blood dyscrasias. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dr hemagglutinin structural subunit | Escherichia coli | inhibitor |
ADME / PK
| Absorption | Chloramphenicol succinate has a high degree of interpatient variability, with a T<sub>max</sub> of 18 minutes to 3 hours. A 1g oral chloramphenicol succinate dose every 6-8 hours reaches a mean C<sub>max</sub> of 11.2µg/mL with a T<sub>max</sub> of 1 hour. |
|---|---|
| Half-life | The half life of chloramphenicol succinate in patients with normal renal and hepatic function is 0.6-2.7h. |
| Protein binding | Chloramphenicol succinate is 57-92% protein bound in plasma. |
| Metabolism | Chloramphenicol succinate is hydrolyzed to chloramphenicol. The propane-diol moiety of chloramphenicol can be metabolised through a number of pathways including glucuronidation, sulfate conjugation, phosphorylation, acetylation, and oxidation. The dichloroacetate moiety can be metabolised through hydrolysis of the amide group and dechlorination. The nitro functional group can also be metabolised to an aryl amine and aryl amide metabolite. |
| Route of elimination | 6-80% of chloramphenicol succinate is eliminated unchanged in the urine, though this is highly variable between patients. On average, 30% of chloramphenicol succinate is eliminated unchanged in the urine and 10% is eliminated as the active chloramphenicol in the urine. |
| Volume of distribution | Chloramphenicol succinate has a volume of distribution of 0.2-3.1L/kg. |
| Clearance | Chloramphenicol succinate's total clearance is 530-540mL/min in patients with normal renal and hepatic function, and 354mL/min in patients with renal or hepatic dysfunction. Chloramphenicol succinate's renal clearance is 222-260mL/min in patients with normal renal and hepatic function, and 66mL/min in patients with renal or hepatic dysfunction. |
Formulation & handling
- Chloramphenicol succinate is formulated primarily for intravenous administration, typically as a lyophilized powder for solution.
- As a small molecule with moderate water solubility, reconstitution and solution stability must be carefully controlled prior to injection.
- The nitrobenzene moiety indicates potential chemical sensitivity; handling should minimize exposure to light and extreme pH conditions to preserve stability.
Regulatory status
| Lifecycle | The API's patents have expired in both the US and Canada, allowing for generic manufacturing and entry. Consequently, the product is in a mature market phase with established availability across these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Chloramphenicol succinate is marketed primarily in the US and Canada with multiple branded products indicating the presence of several originator companies. The availability of established brand names suggests a competitive landscape with a global footprint focused on North America. Given its status and market presence, patent expiry likely permits generic competition, indicating existing or potential generic suppliers in the supply chain. |
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Safety
| Toxicity | Patients experiencing an overdose may present with shock, cyanosis, and coma. Treat patients with symptomatic and supportive measures which may include administration of fluids, exchange transfusions, and administration of dopamine. |
|---|
- Chloramphenicol succinate may cause severe systemic toxicity in overdose, including shock, cyanosis, and coma
- Handle with precautions to prevent accidental exposure
- Use appropriate personal protective equipment
Chloramphenicol Succinate 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.
