Glibenclamide

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

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

Release form

1. Tablets: Usually taken orally, i.e. by mouth. Glibenclamide tablets are usually available in different dosages and may contain additional ingredients that ensure their structure and stability.
2. Powder for solution: Sometimes glibenclamide may be supplied as a powder for solution. This solution may be intended for injection or for oral administration after dilution with liquid.
3. Other forms: In addition to tablets and powder, glibenclamide may be available in other forms, including capsules or injection solutions, depending on regional standards and manufacturers.

Pharmacodynamics

1. Increased insulin release: Glibenclamide binds to specific receptors on the beta cells of the pancreas, which stimulates the release of insulin. This mechanism helps to lower blood sugar levels after meals.
2. Decreased secretion of glucagon: Glibenclamide can also decrease the secretion of glucagon, a hormone that increases blood glucose levels. This helps reduce the production of glucose 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 reached within 1-3 hours after administration. Glibenclamide binds to plasma proteins, primarily 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 in 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: The usual starting dose of glibenclamide for adults is 2.5-5 mg once or twice daily. Further dose adjustments can be made based on the efficacy and individual tolerability of the drug.
2. Directions for use: Glibenclamide is usually taken orally, i.e. by mouth. It is taken immediately before meals to reduce the risk of hypoglycemia. The tablets are usually swallowed whole with water.
3. Regularity of administration: The drug is usually taken once or twice a day, depending on the doctor's prescription. Regularity and adherence to the schedule of administration are very important to achieve the desired effect.
4. Following your doctor's instructions: It is important to follow your doctor's instructions regarding dosage and administration, and not to change the dosage without your doctor's approval.
5. Blood glucose monitoring: It is important to monitor your blood glucose regularly 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 transfer: Glibenclamide can cross the placenta, potentially causing hypoglycemia in the fetus. This may adversely affect fetal development and even lead to severe complications during delivery.
3. Effects on fetal growth: Some studies have suggested that the use of glibenclamide during pregnancy may be associated with an increased risk of macrosomia (excessive growth of the fetus), which may complicate the birth process.

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 poses no risk to the fetus. Insulin is considered a safer and preferred option for managing diabetes during pregnancy.
• Talk to your doctor: If you are using glibenclamide and are planning to become pregnant or are already pregnant, it is important to talk to your doctor. Your doctor will help tailor your treatment plan to minimize the risks to 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 in treating type 1 diabetes because in this type of diabetes the pancreas does not produce enough insulin. Its use may be contraindicated in these patients.
2. Hypoglycemia: Patients at increased risk of hypoglycemia (low blood sugar) should use glibenclamide with caution. This may include elderly patients, those with poor nutrition, or those taking other medications that can lower blood sugar.
3. Renal impairment: Glibenclamide is excreted via the kidneys, so 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 liver failure, its use may be contraindicated or require dosage adjustment.
5. Pregnancy and breastfeeding: 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 sulfonylurea drugs should avoid its use.
7. Stable compensated diabetes: Glibenclamide should be used with caution in patients with long-term compensated diabetes to avoid the risk of hypoglycemia or other complications.

Side effects Glibenclamide

1. Hypoglycemia: The most serious side effect of glibenclamide is low blood sugar (hypoglycemia). This may include dizziness, hunger, weakness, irritability, sweating, tachycardia, and even loss of consciousness. Patients taking glibenclamide should have their blood glucose monitored regularly.
2. Gastrointestinal reactions: Gastrointestinal disturbances 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: Headaches, fatigue, depression, insomnia, and rarely agranulocytosis, hemolytic anemia and dyshidrotic erythema are possible.
5. Effects on the liver: Some patients may experience changes in liver function, including increased liver enzymes.
6. Effect on blood: Thrombocytopenia and leukopenia may rarely occur.
7. Allergic reactions: Rare allergic reactions such as angioedema and anaphylactic reactions may occur.

Overdose

1. Hypoglycemia: This is the primary 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 that requires medical intervention.
3. Arterial hypoglycemia: Since glibenclamide can also lower arterial blood glucose levels, arterial hypoglycemia may develop, which may threaten the blood supply to organs and tissues.
4. Other symptoms: Overdose can also cause adverse effects associated with the action of glibenclamide on other organs and systems, such as gastrointestinal disorders, dizziness, drowsiness, etc.

Interactions with other drugs

1. Hypoglycemic agents: The use of glibenclamide with other hypoglycemic agents, such as insulin or other sulfonylureas, may lead to an increased hypoglycemic effect. This may require a dose adjustment 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) together with glibenclamide may result in increased blood sugar levels due to decreased excretion of sugar by the kidneys.
5. Alcohol: Drinking alcohol while taking glibenclamide may enhance the hypoglycemic effect.

Storage conditions

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