Glucovance

Glucovance is a combination oral hypoglycemic drug used to treat type 2 diabetes. This medication contains two active ingredients: glibenclamide and metformin.

1. Glibenclamide:

   • Glibenclamide belongs to a class of drugs called sulfonylurea. It works by stimulating the beta cells of the pancreas to produce more insulin. Insulin helps lower blood glucose levels by facilitating its transfer from the bloodstream to the body's cells.

2. Metformin:

   • Metformin belongs to the bolanglidase class of drugs. It works by reducing glucose production in the liver and increasing tissue sensitivity to insulin, which promotes better absorption.

Glucovance is intended to improve blood glucose control in adult patients with type 2 diabetes mellitus who are not responding well to metformin or glibenclamide monotherapy, as well as in those already taking both drugs alone.

Indications Glucovance

Glucovance is used in the treatment of type 2 diabetes mellitus in adult patients. It is prescribed when diet therapy and exercise are not sufficiently effective to ensure normal blood glucose levels, and when monotherapy with metformin or glibenclamide is also insufficient.

Release form

Glucovance is available as an oral tablet containing a combination of glibenclamide and metformin hydrochloride.

Pharmacodynamics

1. Glibenclamide:

   • Insulin stimulation: Glibenclamide is a member of the sulfonylurea class and works by stimulating the release of insulin from pancreatic β cells. This mechanism helps lower blood glucose levels by increasing insulin-dependent glucose uptake into tissues and decreasing glucose release from the liver.
   • Increasing insulin sensitivity: Glibenclamide may also improve tissue sensitivity to the action of insulin, which also helps reduce blood glucose levels.

2. Metformin:

   • Reduced gluconeogenesis: Metformin reduces the production of glucose in the liver by inhibiting the processes of gluconeogenesis and glycogenolysis.
   • Increasing insulin sensitivity: Metformin improves tissue sensitivity to insulin by increasing peripheral glucose uptake and decreasing blood glucose levels.

Pharmacokinetics

1. Glibenclamide:

   • Absorption: Glibenclamide is usually well absorbed from the gastrointestinal tract after oral administration.
   • Metabolism: Metabolism occurs in the liver with the formation of active metabolites.
   • Excretion: Glibenclamide is excreted mainly through the kidneys and also with bile.
   • Half time: About 10 hours.

2. Metformin hydrochloride:

   • Absorption: Metformin hydrochloride is almost completely and rapidly absorbed from the gastrointestinal tract after oral administration.
   • Metabolism: Metformin is not metabolized in the body; it is excreted virtually unchanged through the kidneys.
   • Excretion: Excreted primarily in urine.
   • Half-time: About 6 hours.

Dosing and administration

The dosage of Glucovance is individual and should be determined by the physician based on the needs and response of each patient. Here are general recommendations:

1. Starting dose: The usual starting dose is 250 mg glibenclamide and 250 mg metformin once or twice daily depending on current blood glucose levels and previous diabetes treatment.
2. Dose Adjustment: The dose may be gradually increased at intervals of several weeks to minimize side effects and determine the minimum effective dose for glucose control.
3. Maximum dose: The maximum recommended dose should generally not exceed 20 mg of glibenclamide and 2000 mg of metformin per day.

Use Glucovance during pregnancy

The use of Glucovance (a combination of glibenclamide and metformin) during pregnancy is generally not recommended. Both components of this combination drug may pose potential risks to the developing fetus.

• Glibenclamide

Glibenclamide belongs to the sulfonylurea class and can cause hypoglycemia in both the mother and fetus. Although some older studies have suggested the use of glibenclamide during pregnancy, there are concerns about its safety, including possible effects on the fetus and the risk of neonatal hypoglycemia.

• Metformin

Metformin is often considered relatively safe for use during pregnancy compared to other oral antidiabetic drugs and may be used to treat women with polycystic ovary syndrome or gestational diabetes. However, its use should be closely monitored by a physician.

Contraindications

1. Type 1 diabetes mellitus: Glucovance is contraindicated for the treatment of type 1 diabetes mellitus, which is characterized by a lack of insulin in the body. This drug is intended only for the treatment of type 2 diabetes.
2. Ketoacidosis: Glucovance is also contraindicated in the presence of ketoacidosis, an acute and severe complication of diabetes mellitus, which is characterized by high levels of ketone bodies in the blood. This is a serious condition that requires immediate medical attention.
3. Liver failure: In patients with severe liver failure, the use of Glucovance may be contraindicated due to the risk of toxic accumulation of drugs in the body.
4. Renal failure: In the presence of severe renal failure, Glucovance may be contraindicated, since metformin, one of the components of the drug, is excreted through the kidneys.
5. Pregnancy and breastfeeding: The use of Glucovance during pregnancy and breastfeeding may require special attention and consultation with a doctor.
6. Known allergic reaction: Patients with a known allergy to glibenclamide, metformin or other components of the drug should avoid its use.

Side effects Glucovance

1. Hypoglycemia (low blood sugar levels) - especially if the dosage recommendations are not followed or doses are missed.
2. Gastrointestinal disorders such as diarrhea, nausea, vomiting, constipation, dyspepsia.
3. Rarely, allergic reactions such as skin rash, itching, urticaria may occur.
4. Changes in liver function tests may occur.
5. Changes in blood composition such as anemia or leukopenia may occur.

Overdose

1. Hypoglycemia: Glibenclamide, as a sulfonylurea, can cause a significant decrease in blood glucose levels in overdose. This can lead to various symptoms of hypoglycemia, such as hunger, sweating, shaking, irregular heartbeat, as well as headaches and irritability. In cases of severe hypoglycemia, loss of consciousness or even seizures may occur.
2. Lactic acidosis: Metformin can cause a rare but serious complication called metformic acidosis. This condition is characterized by the accumulation of lactic acid in the body, which can lead to serious problems with the heart, breathing, and other organs. Symptoms of metformin acidosis may include nausea, vomiting, abdominal pain, faster or slower respiratory rates, weakness and drowsiness.
3. Other undesirable effects: In addition, overdose may cause other undesirable effects associated with the action of glibenclamide and metformin, such as gastrointestinal disorders, headache, dizziness, drowsiness and others.

Interactions with other drugs

1. Hypoglycemic agents: Combination with other hypoglycemic agents such as sulfonylurea, insulin or α-glucosidase inhibitors may increase the risk of hypoglycemia. Careful monitoring of blood glucose levels is necessary during concomitant use.
2. Medicines affecting renal function: Drugs such as certain antibiotics (eg, aminoglycosides), indirect anticoagulants (eg, warfarin) or iodinated contrast media may increase the risk of lactic acidosis, especially in patients with impaired renal function. Caution is required when using them together.
3. Medicines affecting metformin absorption: Some drugs such as antacids may reduce the absorption of metformin, which may lead to a decrease in its effectiveness. It is recommended to take metformin at least 2 hours before or after taking antacids.
4. Medicines that increase the risk of hypoglycemia: Some drugs, such as ACE inhibitors, calcium channel blockers, beta-blockers, can enhance the hypoglycemic effect of glucose-lowering agents.
5. Medicines that affect the metabolism of glibenclamide: Some drugs, such as cytochrome P450 inhibitors, can increase the concentration of glibenclamide in the blood, which can enhance its hypoglycemic effect and increase the risk of hypoglycemia.

Storage conditions

Glucovance containing glibenclamide and metformin hydrochloride, like many other medications, should be stored in accordance with the directions on the packaging and instructions for use. It is generally recommended to store it in a dry place at a temperature not exceeding 25°C, away from direct sunlight and moisture. Storage conditions may vary slightly depending on the manufacturer and the form of the drug (tablets, capsules, etc.), so it is recommended that you read the instructions and follow the directions on the package.

In addition, Glucovance should be kept out of the reach of children to prevent accidental use. If the product is expired or shows signs of deterioration (such as changes in color, odor, or texture), it should not be used and should be disposed of in accordance with local regulations.