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Glipizide | CAS No: 29094-61-9 | GMP-certified suppliers
A medication that improves glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet and exercise by enhancing endogenous insulin secretion.
Therapeutic categories
Primary indications
- Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Product Snapshot
- Glipizide is an oral small molecule formulation available primarily as immediate and extended-release tablets with various coating types
- It is indicated for adjunctive use in glycemic control for adults with type 2 diabetes mellitus
- The product holds approval status in the US market and is subject to ongoing investigational evaluations
Clinical Overview
Pharmacologically, glipizide acts primarily on pancreatic beta cells by binding to sulfonylurea receptors associated with ATP-sensitive potassium channels. This binding causes channel closure, leading to cell membrane depolarization and subsequent opening of voltage-gated calcium channels. The resulting calcium influx triggers exocytosis of insulin-containing granules, increasing plasma insulin concentrations. This insulinotropic effect enhances glucose uptake by peripheral tissues and suppresses hepatic gluconeogenesis. Additionally, glipizide exerts extrapancreatic effects such as promoting insulin signaling in muscle, adipose, and liver cells, inhibiting lipolysis, and modulating hormone secretion from pancreatic alpha and delta cells, including decreased glucagon and increased somatostatin secretion.
Pharmacokinetically, glipizide demonstrates rapid absorption with onset of action approximately 30 minutes after oral administration. It has the shortest half-life and duration of action among sulfonylureas, typically lasting 12 to 24 hours, which reduces prolonged hypoglycemia risk. Metabolism primarily occurs hepatically via cytochrome P450 enzymes, notably CYP2C9, with renal excretion of metabolites. The drug does not cause sustained elevations in fasting insulin but maintains enhanced postprandial insulin response upon chronic dosing.
Safety considerations include potential hypoglycemia and weight gain, common to sulfonylureas due to increased insulin levels. Chronic use may lead to down-regulation of beta-cell sulfonylurea receptors, potentially diminishing long-term efficacy. Careful patient selection and dose titration are essential to minimize adverse effects.
Glipizide is approved for clinical use in multiple countries, including the United States and Canada, available as immediate and extended-release oral formulations under brand names such as Glucotrol® and in combination with metformin as Metaglip®.
For API procurement, it is critical to ensure compliance with regulatory standards, including purity, batch consistency, and stability parameters. The active pharmaceutical ingredient should meet pharmacopeial requirements and be sourced from manufacturers with validated synthetic routes that minimize impurities and ensure reproducible quality suitable for pharmaceutical formulation development.
Identification & chemistry
| Generic name | Glipizide |
|---|---|
| Molecule type | Small molecule |
| CAS | 29094-61-9 |
| UNII | X7WDT95N5C |
| DrugBank ID | DB01067 |
Pharmacology
| Summary | Glipizide is an oral antidiabetic agent indicated for type 2 diabetes mellitus that primarily stimulates insulin secretion from pancreatic beta cells by binding to sulfonylurea receptors, leading to ATP-sensitive potassium channel closure and calcium-mediated insulin exocytosis. Additionally, it enhances peripheral glucose uptake and insulin receptor sensitivity in muscle and liver tissues. Secondary effects include modulation of glucagon and somatostatin secretion, inhibition of hepatic glucose output, and increased insulin receptor expression on various cell types. |
|---|---|
| Mechanism of action | Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder with increasing prevalence worldwide. Characterized by higher-than-normal levels of blood glucose, T2DM is a complex disorder that arises from the interaction between genetic, environmental and behavioral risk factors. Insulin is a peptide hormone that plays a critical role in regulating blood glucose levels. In response to high blood glucose levels, insulin promotes the uptake of glucose into the liver, muscle cells, and fat cells for storage. Although there are multiple events occurring that lead to the pathophysiology of T2DM, the disorder mainly involves insulin insensitivity as a result of insulin resistance, declining insulin production, and eventual failure of beta cells of pancreatic islets that normally produce insulin. Early management with lifestyle intervention, such as controlled diet and exercise, is critical in reducing the risk of long-term secondary complications, such as cardiovascular mortality. Glipizide, like other sulfonylurea drugs, is an insulin secretagogue, which works by stimulating the insulin release from the pancreatic beta cells thereby increasing the plasma concentrations of insulin. Thus, the main therapeutic action of the drug depends on the functional beta cells in the pancreatic islets. Sulfonylureas bind to the sulfonylurea receptor expressed on the pancreatic beta-cell plasma membrane, leading to the closure of the ATP-sensitive potassium channel and reduced potassium conductance. This results in depolarization of the pancreatic beta cell and opening of the voltage-sensitive calcium channels, promoting calcium ion influx. Increased intracellular concentrations of calcium ions in beta cells stimulates the secretion, or exocytosis, of insulin granules from the cells.[label,T28] Apart from this main mechanism of action, the blood-glucose-lowering effect of glipizide involves increased peripheral glucose utilization via stimulating hepatic gluconeogenesis and by increasing the number and sensitivity of insulin receptors. |
| Pharmacodynamics | Glipizide is a blood glucose-lowering agent. The initial onset of blood glucose-lowering effect occurs around 30 minutes post-administration with the duration of action lasting for about 12 to 24 hours. While the chronic use of glipizide does not result in elevations in the fasting insulin levels over time, the postprandial insulin response, or insulin response to a meal, is observed to be enhanced, even after 6 months of treatment. The main therapeutic actions of glipizide primarily occur at the pancreas where the insulin release is stimulated, but glipizide also mediates some extrapancreatic effects, such as the promotion of insulin signaling effects on the muscles, fat, or liver cells. Due to its action on the endogenous cells, sulfonylureas including glipizide is associated with a risk for developing hypoglycemia and weight gain in patients receiving the drug. Chronic administration of glipizide may result in down-regulation of the sulfonylurea receptors on pancreatic beta cells, which are molecular targets of the drug, leading to a reduced effect on insulin secretion. Like other sulfonylureas, glipizide may work on pancreatic delta (δ) cells and alpha (α) cells to stimulate the secretion of somatostatin and suppress the secretion of glucagon, which are peptide hormones that regulate neuroendocrine and metabolic pathways. Other than its primary action on the pancreas, glipizide also exerts other biological actions outside of the pancreas, or "extrapancreatic effects", which is similar to other members of the sulfonylurea drug class. Glipizide may enhance the glucose uptake into the skeletal muscles and potentiate the action of insulin in the liver. Other effects include inhibited lipolysis in the liver and adipose tissue, inhibited hepatic glucose output, and increased uptake and oxidation of glucose. It has also been demonstrated by several studies that the chronic therapeutic use of sulfonylureas may result in an increase in insulin receptors expressed on monocytes, adipocytes, and erythrocytes. |
Targets
| Target | Organism | Actions |
|---|---|---|
| ATP-binding cassette sub-family C member 8 | Humans | inhibitor |
| Peroxisome proliferator-activated receptor gamma | Humans | agonist |
ADME / PK
| Absorption | Gastrointestinal absorption of glipizide is uniform, rapid, and essentially complete. The absolute bioavailability of glipizide in patients with type 2 diabetes receiving a single oral dose was 100%. The maximum plasma concentrations are expected to be reached within 6 to 12 hours following initial dosing. The steady-state plasma concentrations of glipizide from extended-release oral formulations are maintained over the 24-hour dosing interval. In healthy volunteers, the absorption of glipizide was delayed by the presence of food but the total absorption was unaffected. |
|---|---|
| Half-life | The mean terminal elimination half-life of glipizide ranged from 2 to 5 hours after single or multiple doses in patients with type 2 diabetes mellitus. |
| Protein binding | Glipizide is about 98-99% bound to serum proteins, with albumin being the main plasma protein. |
| Metabolism | Glipizide is subject to hepatic metabolism, in which its major metabolites are formed from aromatic hydroxylation. These major metabolites are glipizide are reported to be pharmacologically inactive. In contrast, an acetylaminoethyl benzine derivative is formed as a minor metabolite which accounts for less than 2% of the initial dose and is reported to have one-tenth to one-third as much hypoglycemic activity as the parent compound. |
| Route of elimination | Glipizide is mainly eliminated by hepatic biotransformation, where less than 10% of the initial dose of the drug can be detected in the urine and feces as unchanged glipizide. About 80% of the metabolites of glipizide is excreted in the urine while 10% is excreted in the feces. |
| Volume of distribution | The mean volume of distribution was approximately 10 L following administration of single intravenous doses in patients with type 2 diabetes mellitus. In mice and rat studies, the presence of the drug and its metabolites was none to minimal in the fetus of pregnant female animals. Other sulfonylurea drugs were shown to cross the placenta and enter breast milk thus the potential risk of glipizide in fetus or infants cannot be excluded. |
| Clearance | The mean total body clearance of glipizide was approximately 3 L/hr following administration of single intravenous doses in patients with type 2 diabetes mellitus. |
Formulation & handling
- Glipizide is formulated exclusively for oral administration, primarily as immediate and extended-release tablets.
- It is a small molecule benzenesulfonamide with low water solubility, requiring consideration for formulation bioavailability.
- Alcohol consumption should be avoided due to increased hypoglycemia risk; dosing is recommended before meals for optimal efficacy.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is marketed primarily in the United States, where key patents expired between 2009 and 2019, indicating a mature market with potential generic competition. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Glipizide involves multiple originator and generic pharmaceutical companies, with significant participation from both branded and generic packagers primarily serving the US market. The presence of several patents, with the latest expiry dates ranging around 2014 to 2019, indicates that patent protection has generally lapsed, allowing for established generic competition. Branded formulations remain available in the US, but the extensive network of generic manufacturers supports broad sourcing options within this region. |
|---|
Safety
| Toxicity | In rats, the oral LD<sub>50</sub> is reported to be greater than 4000 mg/kg and the intraperitoneal LD<sub>50</sub> is 1200 mg/kg. The lowest published toxic dose (TDLo) via oral route in child was 379 μg/kg.[MSDS] Symptoms of overdose in sulfonylureas, including glipizide, may be related to severe hypoglycemia and may include coma, seizure, or other neurological impairment. These are symptoms of severe hypoglycemia and require immediate treatment with glucagon or intravenous glucose and close monitoring for a minimum of 24 to 48 hours since hypoglycemia may recur after apparent clinical recovery. Mild hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated with oral glucose. |
|---|
- Handle with care to avoid exposure, as sulfonylureas like glipizide have a low toxic dose in humans, with reported oral TDLo at 379 μg/kg
- In case of significant exposure, risk of severe hypoglycemia necessitates readiness for immediate intervention and extended monitoring
- Use appropriate PPE to minimize risk of accidental ingestion or dermal absorption, considering reported intraperitoneal LD50 of 1200 mg/kg in animal studies
Glipizide 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.
Glipizide (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.
Glipizide API manufacturers & distributors
Compare qualified Glipizide API suppliers worldwide. We currently have 18 companies offering Glipizide API, with manufacturing taking place in 8 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 |
|---|---|---|---|---|---|
| Amsa S.P.A. | Producer | Italy | Italy | CoA, GMP, USDMF | 10 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Auro Laboratories | Producer | India | India | CoA, USDMF | 6 products |
| Cambrex | Producer | Italy | Unknown | CoA, GMP, USDMF | 104 products |
| Fermion | Producer | Finland | Finland | CoA, USDMF | 29 products |
| Janssen Pharma | Producer | Belgium | Netherlands | CoA, GMP | 63 products |
| Kreative Organics | Producer | India | India | CoA, GMP, USDMF, WC | 9 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Pharmacia & Upjohn | Producer | United States | United States | CoA, USDMF | 30 products |
| Rini Life Science Pvt | Producer | India | India | CoA | 2 products |
| Sai-Tech Pharmaceuticals ... | Producer | India | India | CoA | 8 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA | 757 products |
| Taizhou Highsun | Producer | China | China | CEP, CoA, USDMF | 2 products |
| Unichem Labs. | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF, WC | 62 products |
| USV | Producer | India | India | CoA, FDA, GMP, USDMF, WC | 35 products |
| Weihai Disu Pharma | Producer | China | China | CEP, CoA, FDA | 2 products |
| Yangtze River Pharmaceuti... | Producer | China | China | CoA, GMP, ISO14001 | 34 products |
When sending a request, specify which Glipizide 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 Glipizide 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.
