Glucovance

Glucovance is a combination oral hypoglycemic drug used to treat type 2 diabetes. This drug 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 in 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 class of drugs called bolus anglideases. It works by reducing glucose production in the liver and increasing tissue sensitivity to insulin, which promotes better absorption.

Glucovance is indicated for improving blood glucose control in adult patients with type 2 diabetes mellitus who are not responding effectively to metformin or glibenclamide monotherapy, or who are already taking both drugs separately.

Indications Glucovance

Glucovance is used in the treatment of type 2 diabetes mellitus in adults. It is prescribed when diet and exercise alone are not effective enough to maintain normal blood glucose levels and when metformin or glibenclamide monotherapy is also insufficient.

Release form

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

Pharmacodynamics

1. Glibenclamide:

   • Insulin stimulation: Glibenclamide belongs to the sulfonylurea class and acts by stimulating the release of insulin from pancreatic β-cells. This mechanism helps to lower blood glucose levels by increasing insulin-dependent glucose uptake into tissues and decreasing glucose release from the liver.
   • Insulin Sensitivity Improvement: Glibenclamide can also improve tissue sensitivity to insulin action, which also helps lower blood glucose levels.

2. Metformin:

   • Decreased gluconeogenesis: Metformin reduces hepatic glucose production by inhibiting the processes of gluconeogenesis and glycogenolysis.
   • Increased insulin sensitivity: Metformin improves tissue sensitivity to insulin by increasing peripheral glucose uptake and decreasing blood glucose levels.

Pharmacokinetics

1. Glibenclamide:

   • Absorption: Glibenclamide is generally 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 in the bile.
   • Semi-final deadline: 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 mainly in urine.
   • Semi-final deadline: About 6 hours.

Dosing and administration

The dosage of Glucovance is individual and should be determined by the doctor 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 your current blood glucose levels and previous diabetes treatment.
2. Dose adjustment: The dose may be gradually increased over several weeks to minimize side effects and determine the lowest effective dose for glucose control.
3. Maximum dose: The maximum recommended dose should generally not exceed 20 mg glibenclamide and 2000 mg 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 of drugs and can cause hypoglycemia in both 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 can be used to treat women with polycystic ovary syndrome or gestational diabetes. However, its use should be closely monitored by a doctor.

Contraindications

1. Diabetes mellitus type 1: Glucovance is contraindicated for the treatment of diabetes mellitus type 1, which is characterized by the absence of insulin in the body. This drug is intended only for the treatment of diabetes mellitus type 2.
2. Ketoacidosis: Glucovance is also contraindicated in the presence of ketoacidosis, an acute and severe complication of diabetes mellitus 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 impairment: In the presence of severe renal impairment, Glucovance may be contraindicated, since metformin, one of the components of the drug, is excreted through the kidneys.
5. Pregnancy and breastfeeding: Use of Glucovance during pregnancy and breastfeeding may require special attention and consultation with a doctor.
6. Known Allergy: 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) - especially if 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, and hives may occur.
4. Changes in liver function tests may occur.
5. Changes in blood composition, such as anemia or leukopenia, are possible.

Overdose

1. Hypoglycemia: Glibenclamide, as a sulfonylurea, can cause a significant drop in blood glucose levels in case of overdose. This can lead to various symptoms of hypoglycemia, such as hunger, sweating, trembling, irregular heartbeat, as well as headaches and irritability. In case of severe hypoglycemia, loss of consciousness or even seizures may occur.
2. Lactic acidosis: Metformin can cause a rare but serious complication called metformin acidosis. This condition is characterized by a buildup of lactic acid in the body, which can lead to serious problems with the heart, breathing, and other organ functions. Symptoms of metformin acidosis can include nausea, vomiting, abdominal pain, faster or slower breathing rate, weakness, and drowsiness.
3. Other side effects: In addition, overdose may cause other side 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 when used concomitantly.
2. Drugs 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 in combination.
3. Drugs that affect metformin absorption: Some drugs, such as antacids, may reduce the absorption of metformin, which may reduce its effectiveness. It is recommended that metformin be taken at least 2 hours before or after taking antacids.
4. Drugs that increase the risk of hypoglycemia: Some drugs, such as ACE inhibitors, calcium channel blockers, beta-blockers, may enhance the hypoglycemic effect of glucose-lowering agents.
5. Drugs that affect the metabolism of glibenclamide: Some drugs, such as cytochrome P450 inhibitors, may increase the concentration of glibenclamide in the blood, which may enhance its hypoglycemic effect and increase the risk of hypoglycemia.

Storage conditions

Glucovance, which contains glibenclamide and metformin hydrochloride, like many other drugs, should be stored according to the instructions on the package and the instructions for use. It is generally recommended to store it in a dry place at a temperature not exceeding 25 ° C, protected from direct sunlight and moisture. Storage conditions may vary slightly depending on the manufacturer and the form of release of the drug (tablets, capsules, etc.), so it is recommended to read the instructions and follow the instructions on the package.

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