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Chlorpropamide | CAS No: 94-20-2 | GMP-certified suppliers
A medication that lowers blood glucose by stimulating insulin secretion, used alongside diet and exercise for managing non-insulin-dependent diabetes mellitus (type 2 diabetes).
Therapeutic categories
Primary indications
- For treatment of NIDDM in conjunction with diet and exercise
Product Snapshot
- Chlorpropamide is an oral small molecule available in multiple tablet formulations
- It is primarily used for the management of non-insulin-dependent diabetes mellitus (NIDDM) alongside diet and exercise
- The compound is approved for use in the US and Canada, with both approved and investigational status
Clinical Overview
Pharmacodynamically, chlorpropamide is a second-generation sulfonylurea and exhibits approximately twice the potency of glipizide, another agent within this class. Its mechanism of action involves binding to ATP-sensitive potassium channels on pancreatic β cells, reducing potassium conductance and causing membrane depolarization. This depolarization opens voltage-sensitive calcium channels, leading to increased intracellular calcium concentrations that trigger insulin exocytosis.
In addition to stimulating insulin release, sulfonylureas including chlorpropamide may enhance peripheral glucose utilization, suppress hepatic gluconeogenesis, and potentially increase the number and sensitivity of insulin receptors. Pharmacokinetic data indicate that up to 80% of a single oral dose of chlorpropamide undergoes hepatic metabolism, and 80 to 90% is excreted in the urine as unchanged drug or metabolites. Renal and hepatic impairment can contribute to elevated drug levels and an increased risk of hypoglycemia.
Safety considerations include the potential for hypoglycemia, which is a common risk with sulfonylureas due to increased insulin levels. This risk is heightened in elderly, debilitated, and malnourished patients. Chlorpropamide use has been associated with increased blood pressure and a higher risk of retinopathy, and as such, it is generally not recommended as a first-line treatment in NIDDM. Weight gain is a noted adverse effect, though typically less pronounced than with exogenous insulin.
Chlorpropamide is classified chemically as a benzenesulfonamide and acts as a substrate of cytochrome P450 enzymes CYP2C9 and CYP2C19, which may have implications for drug interactions. The drug is primarily eliminated renally, necessitating careful consideration in patients with renal insufficiency.
From a sourcing perspective, chlorpropamide APIs should meet stringent quality standards including purity, consistent potency, and controlled residual solvents. Suppliers must ensure compliance with relevant pharmacopeial monographs and Good Manufacturing Practice (GMP) to safeguard product quality and batch-to-batch consistency. Due to its metabolism by CYP enzymes, API suppliers should provide comprehensive impurity profiles to support regulatory submissions and risk assessments.
Identification & chemistry
| Generic name | Chlorpropamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 94-20-2 |
| UNII | WTM2C3IL2X |
| DrugBank ID | DB00672 |
Pharmacology
| Summary | Chlorpropamide is a second-generation sulfonylurea that lowers blood glucose levels by binding to ATP-sensitive potassium channels (ABCC8) on pancreatic beta cells, leading to membrane depolarization and increased intracellular calcium. This calcium influx triggers insulin secretion, enhancing glycemic control in type 2 diabetes mellitus. Its mechanism centers on modulating ion channel activity to promote endogenous insulin release. |
|---|---|
| Mechanism of action | Sulfonylureas such as chlorpropamide bind to ATP-sensitive potassium channels on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin. |
| Pharmacodynamics | Chlorpropamide, a second-generation sulfonylurea antidiabetic agent, is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Chlorpropamide is twice as potent as the related second-generation agent glipizide. |
Targets
| Target | Organism | Actions |
|---|---|---|
| ATP-binding cassette sub-family C member 8 | Humans | inhibitor |
ADME / PK
| Absorption | Readily absorbed from the GI tract. Peak plasma concentrations occur within 2-4 hours and the onset of action occurs within one hour. The maximal effect of chlorpropamide is seen 3-6 hours following oral administration. |
|---|---|
| Half-life | Approximately 36 hours with interindividual variation ranging from 25-60 hours. Duration of effect persists for at least 24 hours. |
| Protein binding | Highly bound to plasma proteins. |
| Metabolism | Up to 80% of dose is metabolized likely through the liver to to 2-hydroxylchlorpropamide (2-OH CPA), p-chlorobenzenesulfonylurea (CBSU), 3-hydroxylchlorpropamide (3-OH CPA), and p-chlorobenzenesulfonamide (CBSA); CBSA may be produced by decomposition in urine. It is unknown whether chlorpropamide metabolites exert hypoglycemic effects. |
| Route of elimination | 80-90% of a single oral dose is excreted in the urine as unchaged drug and metabolites within 96 hours. |
Formulation & handling
- Chlorpropamide is a small molecule oral antidiabetic agent available primarily in tablet form.
- The compound has low water solubility and moderate lipophilicity (LogP 1.94), which may influence formulation strategies.
- Food intake decreases the rate of absorption, so dosing is recommended before or on an empty stomach for consistent bioavailability.
Regulatory status
| Lifecycle | The API's primary patents have expired in both the US and Canada, leading to the availability of multiple generic formulations and a mature market environment in these regions. Ongoing regulatory exclusivities may still apply but generally do not limit generic competition. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Chlorpropamide is manufactured by numerous companies, including both originators and generic producers, indicating a diversified supply base. The product is primarily available in the US and Canadian markets, with branded and generic formulations present. Patent expirations have allowed for widespread generic competition in these regions. |
|---|
Safety
| Toxicity | IPN-RAT LD<sub>50</sub> 580 mg/kg |
|---|
- Oral LD50 in rats: 580 mg/kg, indicating moderate acute toxicity
- Handle with appropriate personal protective equipment to avoid inhalation and skin contact
- Avoid environmental release due to potential toxicity
Chlorpropamide is a type of Sulfonylureas
Sulfonylureas belong to a subcategory of pharmaceutical active ingredients known as antidiabetic agents. These compounds play a crucial role in managing type 2 diabetes, a metabolic disorder characterized by high blood sugar levels. Sulfonylureas work by stimulating the pancreas to produce more insulin, a hormone responsible for regulating blood glucose levels.
As pharmaceutical API, sulfonylureas are highly effective in lowering blood sugar levels by promoting insulin secretion and increasing the sensitivity of cells to insulin. This mechanism of action makes them valuable in the treatment of type 2 diabetes, especially when other measures such as diet and exercise have proven inadequate.
Sulfonylureas are widely prescribed due to their proven efficacy, oral administration convenience, and cost-effectiveness. They are available in various formulations, including tablets and extended-release formulations, allowing flexibility in dosing regimens. Additionally, their long-established presence in the market has resulted in a comprehensive understanding of their safety profile and potential side effects.
Some common sulfonylurea drugs include glipizide, glimepiride, and gliclazide. These compounds are often prescribed as part of a comprehensive treatment plan for type 2 diabetes, along with lifestyle modifications and other antidiabetic medications.
It is important to note that the use of sulfonylureas should be carefully monitored by healthcare professionals to ensure optimal blood sugar control and to minimize the risk of hypoglycemia, a potential side effect. Patients taking sulfonylureas should also be educated about the importance of regular blood glucose monitoring and adhering to prescribed dosages.
In conclusion, sulfonylureas represent an essential subcategory of pharmaceutical APIs used in the treatment of type 2 diabetes. Their mechanism of action, proven efficacy, and cost-effectiveness make them a valuable tool in managing this chronic metabolic condition. Healthcare professionals play a vital role in guiding the appropriate use of sulfonylureas to optimize patient outcomes and ensure safety.
Chlorpropamide (Sulfonylureas), classified under Anti-diabetics
Anti-diabetics, belonging to the pharmaceutical API (Active Pharmaceutical Ingredient) category, are a group of compounds designed to manage and treat diabetes mellitus, a chronic metabolic disorder characterized by high blood sugar levels. These medications play a vital role in controlling diabetes and preventing complications associated with the disease.
Anti-diabetics encompass a wide range of drug classes, including biguanides, sulfonylureas, thiazolidinediones, dipeptidyl peptidase-4 (DPP-4) inhibitors, sodium-glucose cotransporter-2 (SGLT2) inhibitors, and glucagon-like peptide-1 (GLP-1) receptor agonists. Each class works through different mechanisms to regulate blood sugar levels and improve insulin sensitivity.
Biguanides, such as metformin, reduce glucose production by the liver and enhance insulin sensitivity in peripheral tissues. Sulfonylureas, like glipizide, stimulate insulin secretion from pancreatic beta cells. Thiazolidinediones, including pioglitazone, improve insulin sensitivity in muscle and adipose tissues. DPP-4 inhibitors, such as sitagliptin, increase insulin release and inhibit glucagon secretion. SGLT2 inhibitors, like dapagliflozin, decrease renal glucose reabsorption, leading to increased urinary glucose excretion. GLP-1 receptor agonists, such as exenatide, enhance insulin secretion, suppress glucagon release, slow gastric emptying, and promote satiety.
These anti-diabetic APIs serve as the foundational ingredients for the formulation of various oral tablets, capsules, and injectable medications used in the treatment of diabetes. By targeting different aspects of glucose regulation, they help patients achieve and maintain optimal blood sugar levels, thus reducing the risk of diabetic complications, such as cardiovascular disease, neuropathy, and nephropathy.
It is crucial for healthcare professionals to prescribe and administer these anti-diabetic medications appropriately, considering factors like the patient's medical history, co-existing conditions, and potential drug interactions. Regular monitoring of blood glucose levels and close medical supervision are necessary to ensure effective diabetes management.
In conclusion, anti-diabetics form a critical category of pharmaceutical APIs used for the treatment of diabetes. These compounds, encompassing various drug classes, work through distinct mechanisms to regulate blood sugar levels and improve insulin sensitivity. By facilitating glucose control, anti-diabetic APIs help mitigate the risk of complications associated with diabetes mellitus, ultimately promoting better health outcomes for patients.
Chlorpropamide API manufacturers & distributors
Compare qualified Chlorpropamide API suppliers worldwide. We currently have 3 companies offering Chlorpropamide 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 |
|---|---|---|---|---|---|
| Kothari Phyto | Producer | India | India | CoA, JDMF, WC | 3 products |
| Lusochimica | Producer | Italy | Italy | CoA, GMP, JDMF | 23 products |
| Quantum Drugs & Chemicals | Producer | India | India | CoA, WC | 2 products |
When sending a request, specify which Chlorpropamide 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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