Glibenclamide

Glibenclamide (also known as glyburide) is an oral hypoglycemic drug of the sulfonylurea class, which is widely used to treat type 2 diabetes. This medication helps control blood sugar levels by stimulating the pancreas to secrete more insulin. Insulin is a hormone that is needed to allow cells to take up glucose from the blood and use it as energy.

Glibenclamide works by binding to certain receptors on beta cells in the pancreas, which stimulates the release of insulin. This results in lower blood glucose levels.

Indications Glibenclamide

Type 2 diabetes: Glibenclamide is used to lower blood glucose levels in patients with type 2 diabetes 2, when diet and exercise do not achieve the desired glucose control.

Release form

1. Tablets: Usually taken orally, i.e. Through the mouth. Glibenclamide tablets usually come in a variety of strengths and may contain additional ingredients to provide structure and stability.
2. Powder for solution: Glibenclamide may sometimes be supplied as a powder for solution. This solution can be given for injection or for oral administration after dilution in liquid.
3. Other Forms: In addition to tablets and powder, glibenclamide may be available in other forms, including capsules or injectable solutions, depending on regional standards and manufacturers.

Pharmacodynamics

1. Increasing insulin release: Glibenclamide binds to specific receptors on the beta cells of the pancreas, which stimulates the release of insulin. This mechanism helps lower blood sugar levels after meals.
2. Decreased glucagon secretion: Glibenclamide may also reduce the secretion of glucagon, a hormone that increases blood glucose levels. This helps reduce glucose production in the liver and lower blood sugar levels.
3. Improving peripheral insulin sensitivity: Some studies suggest that glibenclamide may also increase the sensitivity of peripheral tissues to insulin, which helps the body use glucose more efficiently.

Pharmacokinetics

Glibenclamide, like other sulfonylureas, is usually absorbed from the gastrointestinal tract and is rapidly metabolized in the liver. Its maximum concentration in the blood is usually achieved within 1-3 hours after administration. Glibenclamide binds to blood plasma proteins, mainly albumin.

The bioavailability of glibenclamide is approximately 80-100%. After metabolism in the liver, it is excreted mainly through the kidneys as metabolites and partly with bile. The half-life of glibenclamide from the blood is usually about 2-5 hours. Its duration of action may vary depending on the form of the drug and the individual characteristics of the patient.

Dosing and administration

1. Dosage: Usually, the initial dose of glibenclamide for adults is 2.5-5 mg once or twice a day. Further dose adjustments can be made in accordance with the effectiveness and individual tolerability of the drug.
2. Method of administration: Glibenclamide is usually taken orally, i.e. Through the mouth. It is taken immediately before meals to reduce the risk of hypoglycemia. The tablets are usually swallowed whole with water.
3. Frequency of administration: The drug is usually taken once or twice a day, depending on the doctor's prescription. Regularity and adherence to the schedule are very important to achieve the desired effect.
4. Following the doctor's instructions: It is important to follow your doctor's instructions regarding dosage and route of administration, and not to change the dosage without his or her consent.
5. Blood glucose monitoring: It is important to regularly monitor blood glucose levels while taking glibenclamide to prevent possible complications such as hypoglycemia or hyperglycemia.

Use Glibenclamide during pregnancy

Risks of using glibenclamide during pregnancy:

1. Hypoglycemia: Glibenclamide can cause hypoglycemia (low blood sugar), which is especially dangerous for both the pregnant woman and the fetus. Hypoglycemia in the mother can lead to loss of consciousness and other serious health problems.
2. Placental Transmission: Glibenclamide can cross the placenta, potentially leading to fetal hypoglycemia. This can negatively affect the development of the fetus and even lead to severe complications during childbirth.
3. Effects on fetal growth: Some studies have shown that use of glibenclamide during pregnancy may be associated with an increased risk of macrosomia (excessive fetal growth), which may complicate labor.

Recommendations:

• Alternative Treatments: In many cases, doctors recommend using insulin to control blood glucose levels during pregnancy because insulin does not cross the placenta and pose no risk to the fetus. Insulin is considered a safer and preferred option for managing diabetes during pregnancy.
• Consultation with your doctor: If you are using glibenclamide and are planning to become pregnant or are already pregnant, it is important to discuss this with your doctor. Your doctor will help you tailor your treatment plan to minimize risks for you and your unborn baby.
• Careful monitoring: If glibenclamide is used, strict medical monitoring of blood sugar levels is necessary to avoid hypoglycemia and other possible complications.

Contraindications

1. Type 1 diabetes: Glibenclamide is not effective for treating type 1 diabetes because in this type of diabetes the pancreas does not produce enough insulin. Its use may be contraindicated in such patients.
2. Hypoglycemia: Patients with an increased risk of hypoglycemia (low blood sugar) should use glibenclamide with caution. This may include older patients, those with poor diets, or those taking other medications that lower blood sugar.
3. Renal Impairment: Glibenclamide is excreted through the kidneys and its use may be contraindicated in patients with severe renal impairment.
4. Liver failure: The liver plays an important role in the metabolism of glibenclamide. Therefore, in patients with severe hepatic impairment, its use may be contraindicated or require dosage adjustment.
5. Pregnancy and breastfeeding: The use of glibenclamide during pregnancy may be contraindicated or require special caution and medical supervision. Its use should also be avoided during breastfeeding as there is insufficient data on its safety for the baby.
6. Allergic reaction: People with a known allergy to glibenclamide or other sulfonylureas should avoid its use.
7. Stable control of diabetes: Glibenclamide should be used with caution in patients with long-term control of diabetes to avoid the risk of hypoglycemia or other complications.

Side effects Glibenclamide

1. Hypoglycemia: The most serious side effect of glibenclamide is a decrease in blood sugar (hypoglycemia). This can manifest itself in the form of dizziness, fasting, weakness, irritability, sweating, tachycardia and even loss of consciousness. Patients taking glibenclamide should have their blood glucose monitored continuously.
2. Gastrointestinal reactions: Digestive disorders such as nausea, vomiting, diarrhea, constipation and abdominal pain may occur.
3. Skin reactions: Allergic reactions such as itching, skin rash, hives may occur.
4. Systemic reactions: Possible headaches, fatigue, depression, insomnia, and rarely - agranulocytosis, hemolytic anemia and dyshidrotic erythema.
5. Effects on the liver: Some patients may experience changes in liver function, including increased liver enzymes.
6. Effects on blood: Thrombocytopenia and leukopenia may rarely occur.
7. Allergy reactions: Rare allergic reactions, such as angioedema and anaphylactic reactions, may occur.

Overdose

1. Hypoglycemia: This is the main and most serious effect of glibenclamide overdose. Symptoms of hypoglycemia may include headache, hunger, weakness, sweating, tremors, tachycardia, changes in vision, drowsiness, unconsciousness, and even seizures.
2. Coma: In cases of severe hypoglycemia, if timely assistance is not provided, hypoglycemic coma may develop, which is a dangerous condition requiring medical intervention.
3. Arterial hypoglycemia: Since glibenclamide can also lower arterial blood glucose levels, arterial hypoglycemia may develop, which can threaten the blood supply to organs and tissues.
4. Other symptoms: Overdose may also cause adverse effects associated with the action of glibenclamide on other organs and systems, such as gastrointestinal disorders, dizziness, drowsiness, and etc.

Interactions with other drugs

1. Hypoglycemic drugs: The use of glibenclamide with other hypoglycemic drugs, such as insulin or other sulfonylureas, can lead to an increase in the hypoglycemic effect. This may require adjustment of the dose of glibenclamide.
2. Antibiotics: Some antibiotics, such as sulfonamides and tetracyclines, may enhance the hypoglycemic effect of glibenclamide.
3. Cardiovascular drugs: Some drugs, such as beta-blockers and angiotensin-converting enzyme inhibitors (ACE inhibitors), may reduce the hypoglycemic effect of glibenclamide.
4. NSAIDs: Using NSAIDs (non-steroidal anti-inflammatory drugs) with glibenclamide may lead to an increase in blood sugar levels due to a decrease in its excretion by the kidneys.
5. Alcohol: Drinking alcohol while taking glibenclamide may enhance the hypoglycemic effect effect.

Storage conditions

Glibenclamide is usually stored at room temperature (15°C to 30°C), in a dry place, protected from light and moisture. Proper storage conditions can help maintain the stability of the product and extend its shelf life.