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Glyburide | CAS No: 10238-21-8 | GMP-certified suppliers
A medication that improves glycemic control as an adjunct to diet and exercise in adults with type 2 diabetes mellitus, used alone or combined with metformin.
Therapeutic categories
Primary indications
- Glyburide is indicated alone or as part of combination product with metformin, as an adjunct to diet and exercise, to improve glycemic control in adults with type 2 diabetes mellitus
Product Snapshot
- Glyburide is an oral small molecule available in multiple tablet and suspension formulations
- It is primarily used to improve glycemic control in adults with type 2 diabetes mellitus
- Glyburide is approved for use in major regulatory markets including the US, EU, and Canada
Clinical Overview
Pharmacologically, glyburide acts by stimulating insulin secretion from pancreatic beta cells. Its mechanism involves binding to the sulfonylurea receptor 1 (SUR1), a regulatory subunit of ATP-sensitive potassium channels on these cells. By inhibiting potassium efflux, glyburide induces cell membrane depolarization, which opens voltage-gated calcium channels. The resultant calcium influx raises intracellular calcium concentrations, promoting exocytosis of insulin-containing granules. This mode of action facilitates increased insulin release independently of ambient glucose fluctuations, differentiating it from physiological regulation.
Glyburide exhibits a long duration of action, enabling once-daily dosing. Therapeutic dosing typically begins at approximately 0.75 mg, with titration up to 10 mg or more as clinically indicated. The drug is metabolized primarily via the cytochrome P450 system, including isoforms CYP2C9, CYP2C19, and CYP3A4, and exhibits interactions with various transporters such as BCRP/ABCG2 and P-glycoprotein. These factors contribute to its pharmacokinetic profile and potential drug-drug interactions.
Safety considerations include the risk of hypoglycemia, inherent to sulfonylurea use, and a reported association with increased cardiovascular mortality observed in related compounds. Monitoring for adverse effects and dose adjustment is warranted in susceptible populations.
From a chemical classification perspective, glyburide is a benzenesulfonamide compound comprising a sulfonamide group linked to a benzene ring. In API procurement, attention should be given to the compound’s purity, polymorphic form, and compliance with pharmacopeial standards to ensure consistent bioavailability and therapeutic efficacy. Suppliers must also provide comprehensive documentation on stability and impurity profiles due to the compound’s regulatory and safety considerations.
Identification & chemistry
| Generic name | Glyburide |
|---|---|
| Molecule type | Small molecule |
| CAS | 10238-21-8 |
| UNII | SX6K58TVWC |
| DrugBank ID | DB01016 |
Pharmacology
| Summary | Glyburide is a second-generation sulfonylurea that enhances insulin secretion by binding to the sulfonylurea receptor 1 (SUR1) component of ATP-sensitive potassium channels on pancreatic beta cells. This binding induces channel closure, leading to cell depolarization, increased intracellular calcium, and subsequent insulin release. The primary pharmacodynamic effect is improved glycemic control through stimulation of endogenous insulin in type 2 diabetes mellitus. |
|---|---|
| Mechanism of action | Glyburide belongs to a class of drugs known as sulfonylureas. These drugs act by closing ATP-sensitive potassium channels on pancreatic beta cells. The ATP-sensitive potassium channels on beta cells are known as sulfonylurea receptor 1 (SUR1). Under low glucose concentrations, SUR1 remains open, allowing for potassium ion efflux to create a -70mV membrane potential. Normally SUR1 closes in response to high glucose concentrations, the membrane potential of the cells becomes less negative, the cell depolarizes, voltage gated calcium channels open, calcium ions enter the cell, and the increased intracellular calcium concentration stimulates the release of insulin containing granules. Glyburide bypasses this process by forcing SUR1 closed and stimulating increased insulin secretion. |
| Pharmacodynamics | Glyburide is a second generation sulfonylurea that stimulates insulin secretion through the closure of ATP-sensitive potassium channels on beta cells, raising intracellular potassium and calcium ion concentrations. Glibenclamide has a long duration of action as it is given once daily, and a wide therapeutic index as patients are started at doses as low as 0.75mg but that can increase as high as 10mg or more. Patients taking glyburide should be cautioned regarding an increased risk of cardiovascular mortality as seen with tolbutamide, another sulfonylurea. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 | Humans | blocker |
| ATP-binding cassette sub-family C member 9 | Humans | modulator |
| Bile salt export pump | Humans | inhibitor |
ADME / PK
| Absorption | Elderly patients taking glyburide reached a C<sub>max</sub> of 211-315ng/mL with a T<sub>max</sub> of 0.9-1.0h, while younger patients reached a C<sub>max</sub> of 144-302ng/mL with a T<sub>max</sub> of 1.3-3.0h. Patients taking glyburide have and AUC of 348ng*h/mL. |
|---|---|
| Half-life | Elderly patients have a terminal elimination half life of 4.0-13.4h, while younger patients have a terminal elimination half life of 4.0-13.9h. |
| Protein binding | Glyburide is 99.9% bound to protein in plasma with >98% accounted for by binding to serum albumin. |
| Metabolism | Glyburide is metabolized mainly by CYP3A4, followed by CYP2C9, CYP2C19, CYP3A7, and CYP3A5. These enzymes metabolize glyburide to 4-trans-hydroxycyclohexyl glyburide (M1), 4-cis-hydroxycyclohexyl glyburide (M2a), 3-cis-hydroxycyclohexyl glyburide (M2b), 3-trans-hydroxycyclohexyl glyburide (M3), 2-trans-hydroxycyclohexyl glyburide (M4), and ethylhydroxycyclohexyl glyburide (M5). The M1 and M2b metabolites are considered active, along with the parent molecule. |
| Route of elimination | Unlike other sulfonylureas, glyburide is 50% excreted in the urine and 50% in the feces. Glyburide is mainly excreted as the metabolite 4-trans-hydroxyglyburide. |
| Volume of distribution | Elderly patients have a volume of distribution of 19.3-52.6L, while younger patients have a volume of distribution of 21.5-49.3L. |
| Clearance | Elderly patients have a clearance of 2.70-3.55L/h, while younger patients have a clearance of 2.47-4.11L/h. |
Formulation & handling
- Glyburide is a small molecule oral antidiabetic agent formulated primarily as tablets and suspensions.
- It exhibits low water solubility and moderate lipophilicity (LogP 3.79), which may impact formulation strategies to enhance bioavailability.
- Administration timing relative to meals is essential due to its impact on pharmacodynamics; avoid concomitant alcohol use to reduce hypoglycemia risk.
Regulatory status
| Lifecycle | The API's patent expired in the United States on January 14, 2020, allowing for generic entry in this market. It is currently marketed in the EU, Canada, and the US, reflecting a mature product lifecycle in these regions. |
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| Markets | EU, Canada, US |
|---|
Supply Chain
| Supply chain summary | Glyburide is produced by multiple manufacturers including both originator and generic pharmaceutical companies, reflecting a competitive supply landscape. The branded products have a global presence across the US, EU, and Canadian markets. Patent expiration in the US as of January 2020 indicates established generic competition in these regions. |
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Safety
| Toxicity | The oral LD<sub>50</sub> in rats is >3200mg/kg, in mice is >1500mg/kg, in rabbits is >10,000mg/kg, and in guinea pigs is >1500mg/kg. Patients experiencing an overdose may present with hypoglycemia. Mild hypoglycemia should be treated with oral glucose and adjustments to drug doses or meal schedules. Severe hypoglycemia may present with coma, seizure, and neurological impairment. This should be treated immediately in hospital with intravenous glucose and monitoring for 24-48 hours. |
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- Handle with appropriate personal protective equipment to avoid accidental ingestion or exposure
- Store in a secure, labeled container to prevent unauthorized access
- In case of accidental exposure, monitor for symptoms related to hypoglycemia and seek immediate medical attention if severe neurological signs occur
Glyburide 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.
Glyburide (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.
Glyburide API manufacturers & distributors
Compare qualified Glyburide API suppliers worldwide. We currently have 3 companies offering Glyburide 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 |
|---|---|---|---|---|---|
| Cambrex | Producer | Italy | Unknown | CoA, USDMF | 104 products |
| Lusochimica | Producer | Italy | Italy | CoA, USDMF | 23 products |
| USV | Producer | India | India | CoA, USDMF | 35 products |
When sending a request, specify which Glyburide 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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