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Colistimethate | CAS No: 12705-41-8 | GMP-certified suppliers
A medication that treats acute or chronic infections caused by sensitive gram-negative bacilli, especially Pseudomonas aeruginosa, including multidrug-resistant strains.
Therapeutic categories
Primary indications
- For the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli, particularly _Pseudomonas aeruginosa_
Product Snapshot
- Colistimethate is available in multiple formulation types including injectable powders (lyophilized and for solution), ophthalmic solutions, ointments, and inhalation solutions
- It is primarily indicated for the treatment of acute or chronic infections caused by gram-negative bacilli such as Pseudomonas aeruginosa
- The product is approved for human use in key regulatory markets including the US, Canada, and the EU, with additional veterinary approvals
Clinical Overview
Pharmacologically, colistimethate is a polymyxin antibiotic with bactericidal activity achieved by disrupting the bacterial cell membrane. This effect results from the compound’s cationic nature and amphipathic structure, which allows it to interact with the lipid components of the bacterial cytoplasmic membrane, altering permeability and causing cell death. Additionally, evidence suggests polymyxins penetrate the cell interior and precipitate cytoplasmic constituents, notably ribosomes, further contributing to their antibacterial effect.
Clinically, polymyxins including colistimethate have historically been reserved for multidrug-resistant infections due to concerns about toxicity. While colistimethate sodium was initially considered less toxic than polymyxin B, comparative doses demonstrate similar risks. Nephrotoxicity is a significant safety consideration, along with potential neuromuscular blockade, necessitating careful dose management and monitoring during therapy.
Absorption of colistimethate when administered parenterally involves conversion to the active colistin form. The drug exhibits complex pharmacokinetics with renal clearance as a major elimination pathway. Its usage has resurged due to the increasing prevalence of multidrug-resistant gram-negative pathogens and the paucity of alternative therapies.
Colistimethate is approved for use in human medicine and veterinary applications. Its role remains critical in managing resistant infections, especially pulmonary infections in cystic fibrosis patients.
For API procurement, the polypeptide structure and complex synthesis demand stringent quality controls to ensure batch consistency, purity, and absence of endotoxin contamination. Suppliers should provide full compliance documentation, including verification of identity, potency, and microbiological standards consistent with international pharmacopeial guidelines.
Identification & chemistry
| Generic name | Colistimethate |
|---|---|
| Molecule type | Small molecule |
| CAS | 12705-41-8 |
| UNII | DL2R53P963 |
| DrugBank ID | DB01111 |
Pharmacology
| Summary | Colistimethate is a polymyxin antibiotic that targets the outer membrane of gram-negative bacteria, disrupting membrane integrity through a detergent-like, surface-active mechanism. Its polycationic structure allows it to increase bacterial membrane permeability, resulting in bactericidal activity. The agent is primarily employed against multidrug-resistant gram-negative pathogens, including Pseudomonas aeruginosa. |
|---|---|
| Mechanism of action | Colistimethate is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistimethate is polycationic and has both hydrophobic and lipophilic moieties. It interacts with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. There is also evidence that polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes. |
| Pharmacodynamics | Colistimethate is a polymyxin antibiotic agent. Originally, colistimethate sodium was thought to be less toxic than polymyxin B; however, if the drugs are administered at comparable doses, their toxicities may be similar. Polymyxins are cationic polypeptides that disrupt the bacterial cell membrane through a detergentlike mechanism. With the development of less toxic agents, such as extended-spectrum penicillins and cephalosporins, parenteral polymyxin use was largely abandoned, except for the treatment of multidrug-resistant pulmonary infections in patients with cystic fibrosis. More recently, however, the emergence of multidrug-resistant gram-negative bacteria, such as _Pseudomonas aeruginosa_ and _Acinetobacter baumannii_, and the lack of new antimicrobial agents have led to the revived use of the polymyxins. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Bacterial outer membrane | Bacteria | incorporation into and destabilization |
ADME / PK
| Absorption | Very poor absorption from gastrointestinal tract. |
|---|---|
| Half-life | 2-3 hours following either intravenous or intramuscular administration in adults and in the pediatric population, including premature infants. |
| Metabolism | As 80% of the dose can be recovered unchanged in the urine, and there is no biliary excretion, it can be assumed that the remaining drug is inactivated in the tissues, however the mechanism is unknown. |
Formulation & handling
- Colistimethate is primarily formulated for parenteral and respiratory administration, including intravenous, intramuscular, inhalation, and ophthalmic routes, with no oral dosage forms.
- The API is a high-molecular-weight polypeptide with low lipophilicity and moderate water solubility, requiring careful handling to maintain stability in aqueous solutions and lyophilized forms.
- Due to its peptide nature, colistimethate may require protection from enzymatic degradation and should be stored and prepared under controlled conditions to preserve potency.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient’s patent protection has expired in the US, Canada, and the EU, allowing for generic competition and indicating a mature market presence in these regions. Product availability reflects established regulatory approvals across these markets. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Colistimethate involves multiple packagers serving primarily the US, Canadian, and EU markets. Branded products are present across these regions, indicating established global distribution. Given the availability of numerous packagers and absence of specific patent information, generic competition is likely existing or imminent. |
|---|
Safety
| Toxicity | Oral LD<sub>50</sub> in rats is 5450 mg/kg. Overdosage with colistimethate can cause neuromuscular blockade characterized by paresthesia, lethargy, confusion, dizziness, ataxia, nystagmus, disorders of speech and apnea. Respiratory muscle paralysis may lead to apnea, respiratory arrest and death. |
|---|
- Oral LD50 in rats is 5450 mg/kg, indicating moderate acute toxicity
- Overexposure may induce neuromuscular blockade symptoms such as paresthesia, ataxia, and respiratory muscle paralysis
- Proper handling and exposure controls are recommended to minimize risk of respiratory arrest associated with inhalation or systemic absorption
Colistimethate 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.
Colistimethate API manufacturers & distributors
Compare qualified Colistimethate API suppliers worldwide. We currently have 5 companies offering Colistimethate 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 |
|---|---|---|---|---|---|
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Lianyungang Runzhong | Producer | China | China | CEP, CoA, FDA | 6 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 762 products |
When sending a request, specify which Colistimethate 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.).
Use the list above to find high-quality Colistimethate API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
