glibenclamide

Actions and Spectrum: 

Actions: 

• Increases insulin secretion: glibenclamide binds to the sulfonylurea receptor on the beta cells of the pancreas, leading to the opening of ATP-sensitive potassium channels and subsequent cell membrane depolarization. It stimulates the release of insulin from the beta cells, which helps to lower blood glucose levels. 
• Increases insulin sensitivity: glibenclamide can also increase the sensitivity of peripheral tissues to insulin, which can further help to lower blood glucose levels. 

Spectrum:

glibenclamide has a broad spectrum of activity and is effective in managing blood glucose levels in individuals with type 2 diabetes mellitus. It is typically used with other medications, such as metformin, which has a different mechanism of action, to achieve better blood sugar control. 

DRUG INTERACTION

Contraindicated  

Serious Use Alternative  

Monitor Closely  

Minor  

Frequency not defined 

Angioedema 

Rash 

Urticaria 

Pruritis 

Heartburn 

Photosensitivity 

Vasculitis 

Nocturia 

Hyponatremia 

Hemolytic anemia 

Agranulocytosis 

Thrombocytopenia 

Pancytopenia 

Paresthesia 

Blurred vision 

Myalgia 

Hypoglycemia 

Minor diuretic effect 

Erythema 

Dermatitis 

Weight gain 

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity to glibenclamide or any other sulfonylurea medications 
• Type 1 diabetes mellitus 
• Diabetic ketoacidosis 
• Severe liver or kidney disease 
• Pregnancy and breastfeeding 

Precautions: 

• Hypoglycemia: glibenclamide can cause low blood sugar levels (hypoglycemia), which is potentially dangerous, especially in older adults or individuals with impaired liver or kidney function. Dosage adjustments may be necessary to avoid hypoglycemia. 
• Cardiovascular disease: There have been reports of an increased risk of cardiovascular events in individuals taking glibenclamide. The medication should be used cautiously in individuals with a history of cardiovascular disease. 
• Adrenal or pituitary insufficiency: glibenclamide can interfere with glucagon release from the pancreas, which can be problematic in individuals with adrenal or pituitary insufficiency. Close monitoring of blood sugar levels may be necessary for these individuals. 
• Alcohol consumption: Alcohol consumption can increase the risk of hypoglycemia in individuals taking glibenclamide. 

Pregnancy consideration:  

Category C 

Breastfeeding warnings:  

No data is available about the excretion of glibenclamide in breast milk. Avoid using in lactating women. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology: 

glibenclamide, also known as glyburide, is a sulfonylurea medication used to treat type 2 diabetes mellitus. It works by stimulating the release of insulin from the beta cells in the pancreas, thereby helping to lower blood glucose levels. 

The mechanism of action of glibenclamide involves binding to specific receptors on the beta cells known as sulfonylurea receptors (SURs). This binding leads to the closure of ATP-sensitive potassium (KATP) channels, which depolarizes the cell membrane and triggers the opening of voltage-dependent calcium (Ca2+) channels. This influx of calcium triggers the release of insulin from the beta cells. 

glibenclamide has a rapid onset of action, with peak effects occurring within 2-4 hours of administration. The medication is metabolized in the liver and excreted in the urine. 

In addition to its effects on insulin release, glibenclamide may also have other effects on glucose metabolism, including increasing insulin sensitivity in peripheral tissues and decreasing hepatic glucose production. 

glibenclamide is typically used in combination with lifestyle modifications such as diet and exercise to help manage type 2 diabetes. It is available in immediate-release tablets and should be taken with food to help prevent gastrointestinal side effects such as nausea and upset stomach. 

Pharmacodynamics: 

glibenclamide, also known as glyburide, is a sulfonylurea medication used to treat type 2 diabetes mellitus. It works by stimulating the release of insulin from the beta cells in the pancreas, thereby helping to lower blood glucose levels. 

The mechanism of action of glibenclamide involves binding to specific receptors on the beta cells known as sulfonylurea receptors (SURs). This binding leads to the closure of ATP-sensitive potassium (KATP) channels, which depolarizes the cell membrane and triggers the opening of voltage-dependent calcium (Ca2+) channels. This influx of calcium triggers the release of insulin from the beta cells. 

glibenclamide has a rapid onset of action, with peak effects occurring within 2-4 hours of administration. The medication has a short duration of action, and its effects typically last for 12-24 hours, depending on the dosage. 

Pharmacokinetics: 

Absorption 

The bioavailability is variable, depending on the oral dosage form 

Onset of action takes place 15-60 min after a single dose  

Duration of action is less than 24 hours 

The volume of distribution is 9-10 L 

Peak serum concentration is achieved in 2-4 hours (adults) 

Distribution 

The protein bound is 99% 

Metabolism 

The drug is metabolized extensively in the liver to less-active metabolites 

The metabolites formed are 4-trans-hydroxyglyburide and 3-cis-hydroxyglyburide (active) 

Elimination and Excretion 

The half-life is 10 hours (for DiaBeta) and 4 hours (for Glynase, PresTab) 

The drug is excreted 50% in the Urine and 50% in the feces

Administration:  

glibenclamide, also known as glyburide, is an oral medication used to treat type 2 diabetes mellitus. The medication is usually taken once or twice daily, with the dosage and timing determined by the healthcare provider based on the individual’s blood glucose levels and response to treatment. 

glibenclamide is available in immediate-release tablets and should be taken with food to help prevent gastrointestinal side effects such as nausea and upset stomach. The immediate-release tablets are typically taken 30 minutes before a meal. 

The dosage of glibenclamide will depend on several factors, including the individual’s blood glucose levels, kidney function, and response to the medication. It’s important to take glibenclamide as directed by your healthcare provider to ensure that you get the maximum benefit from the medication. 

Missing a dose of glibenclamide can lead to high blood glucose levels, and taking too much glibenclamide can cause low blood glucose levels, also known as hypoglycemia. If you miss a dose, take it as soon as you remember, unless it’s almost time for your next dose. In that case, skip the missed dose and continue with your regular dosing schedule. Don’t take a double dose to make up for a missed dose. 

Patient information leaflet 

Generic Name: glibenclamide 

Pronounced: gli-ben-clay-mide 

Why do we use glibenclamide? 

glibenclamide, or glyburide in the United States, is an oral medication for treating type 2 diabetes mellitus. It belongs to the class of medications known as sulfonylureas, which stimulate insulin release from the beta cells in the pancreas. 

glibenclamide is used to help lower blood glucose levels in people with type 2 diabetes who cannot control their blood sugar levels with diet and exercise alone. It is typically prescribed along with lifestyle modifications such as diet and exercise, and it may also be used in combination with other medications for diabetes management. 

Like other sulfonylureas, glibenclamide binds to specific receptors on the beta cells in the pancreas known as sulfonylurea receptors (SURs). This binding leads to the closure of ATP-sensitive potassium (KATP) channels, which depolarizes the cell membrane and triggers the opening of voltage-dependent calcium (Ca2+) channels. This influx of calcium triggers the release of insulin from the beta cells. 

By increasing insulin release, glibenclamide helps to lower blood glucose levels in people with type 2 diabetes. It is generally considered effective and safe when used appropriately and as directed by a healthcare provider.