Glucophage

Glucophage is the trade name for metformin, a widely used oral drug to treat type 2 diabetes. Metformin belongs to a class of drugs known as biguanides, and it works by helping control blood glucose levels. It is especially popular because of its ability to improve glucose control without causing hypoglycemia (blood glucose levels that are too low), which is a common side effect of many other antidiabetic drugs.

Mechanism of action of metformin:

1. Decreased glucose production in the liver - Metformin reduces the amount of glucose produced by the liver.
2. Improved insulin sensitivity - enhances the body's ability to use available insulin to manage blood glucose levels more effectively.
3. Reducing blood glucose levels - metformin helps reduce the absorption of glucose from food in the intestines.

Indications Glucophage

Glucophage is commonly used to treat type 2 diabetes mellitus. It can be used as monotherapy or in combination with other glucose-lowering drugs or insulin. Glucophage is also indicated to prevent the development of diabetes mellitus in individuals with prediabetic conditions and to improve insulin sensitivity in patients with polycystic ovary syndrome.

Release form

Glucophage (metformin) is usually available in tablet form.

Pharmacodynamics

1. Reduced gluconeogenesis: Glucophage reduces the production of glucose in the liver (gluconeogenesis), which is the main mechanism of its antihyperglycemic action. It inhibits enzymes involved in the process of gluconeogenesis, such as phosphoenolpyruvate carboxykinase (PEPCK) and gluconeogenesis-11.
2. Increasing tissue sensitivity to insulin: Metformin increases tissue sensitivity to the action of insulin, which allows them to better utilize glucose from the blood. This is especially important for muscles, which become more sensitive to insulin, which improves peripheral glucose uptake.
3. Reduced absorption of glucose from the intestine: Glucophage may reduce the absorption of glucose from food in the intestine, resulting in a decrease in peak postprandial glucose concentrations and a decrease in postprandial hyperglycemia.
4. Reducing blood lipids: Glucophage may also have beneficial effects on blood lipids, including reducing triglycerides and total cholesterol.
5. Oxidative stress and antioxidant activity: There is evidence that metformin may reduce oxidative stress and have antioxidant properties, which may be associated with its protective effect against cardiovascular complications.

Pharmacokinetics

1. Absorption: Metformin is absorbed from the gastrointestinal tract, mainly in the upper parts of the intestine. Absorption occurs slowly, and peak concentrations are usually reached approximately 2.5 to 3 hours after ingestion.
2. Metabolism: Metformin is practically not metabolized in the body. It is excreted unchanged through the kidneys.
3. Elimination: The main route of excretion of metformin is renal. Most of the drug is excreted unchanged from the body through the kidneys. In patients with impaired renal function, metformin may be retained in the body, requiring dosage adjustment or discontinuation of the drug.
4. Half-life: The half-life of metformin is approximately 6.2 hours, which allows its use two or three times a day, depending on the doctor's recommendations.
5. Food effects: Food can affect the rate and extent of absorption of metformin, so the drug is usually taken with or immediately after meals.

Dosing and administration

Method of application:

1. Taken with food: Glucophage should be taken with or after a meal to minimize gastrointestinal side effects such as nausea and diarrhea.
2. Regularity: The drug should be taken regularly, according to the schedule established by the doctor, to maintain stable blood glucose levels.

Dosage:

The dosage of Glucophage depends on the individual needs of the patient, his response to treatment and target blood glucose levels.

1. Starting dose: The usual starting dose is 500 mg once or twice daily or 850 mg once daily. Your doctor may increase your dose gradually to improve blood glucose control.
2. Maintenance dose: The usual maintenance dose may range from 1500 to 2000 mg per day, divided into two or three doses.
3. Maximum Dose: The maximum recommended dose is 2550 mg per day for adults. For long-term release forms of metformin, the maximum dose may be up to 2000 mg per day.

Special instructions:

• Gradually increase the dose: To minimize side effects, it is advisable to gradually increase the dose.
• Monitoring: Regular monitoring of renal function is necessary, especially before starting treatment and periodically during the course, since metformin is excreted by the kidneys.
• Discontinuation: Metformin should be temporarily discontinued before certain medical procedures or when conditions develop that may increase the risk of lactic acidosis (eg, severe dehydration or hypoxia).

Use Glucophage during pregnancy

Metformin Use Guidelines During Pregnancy:

1. Type 2 Diabetes:

   • Glucophage may be recommended during pregnancy to manage type 2 diabetes. Some studies have shown that it may be safe and effective during this period, helping control blood glucose levels without a significant risk of hypoglycemia.
   • However, the standard treatment for gestational diabetes is insulin, and metformin should only be used under strict indications and under medical supervision.

2. Polycystic ovary syndrome (PCOS):

   • Glucophage is used to improve insulin resistance in women with PCOS, which may promote regular menstruation and improve ovulation. This may be useful for women trying to get pregnant.

3. Safety and efficiency:

   • Research suggests that metformin may be relatively safe for use during pregnancy, but more data is still needed to confirm its complete safety. It is important to consider that metformin crosses the placenta and its effects on the fetus require further study.

4. Monitoring and control:

   • If Glucophage is prescribed during pregnancy, careful monitoring of maternal health and fetal development is necessary. This includes regular blood glucose checks, as well as possible ultrasound examinations to assess the condition of the fetus.

Contraindications

1. Kidney failure: Metformin is excreted through the kidneys, and its accumulation in the body can lead to the development of lactic acidosis (lactic acidosis) in patients with poorly functioning kidneys. Therefore, Glucophage is contraindicated in patients with severe renal failure (glomerular filtration rate less than 30 ml/min) or moderate renal failure in the presence of other risk factors.
2. Liver impairment: In patients with severe hepatic impairment, Glucophage may be contraindicated due to the potential for impaired metabolism and excretion of metformin.
3. Alcoholism: If you abuse alcohol, metformin may increase the risk of developing lactic acidosis. Therefore, patients with alcohol dependence or severe alcohol abuse are not recommended to use Glucophage.
4. Ketoacidosis: Glucophage is also contraindicated in the presence of ketoacidosis, a serious complication of diabetes characterized by high levels of ketone bodies in the blood.
5. Allergy: Patients with a known allergy to metformin or other components of the drug should avoid its use.
6. Pregnancy and breastfeeding: Use of Glucophage during pregnancy and breastfeeding requires consultation with a physician due to limited information about its safety in such situations.

Side effects Glucophage

1. Gastrointestinal problems: diarrhea, nausea, vomiting, abdominal pain, decreased appetite.
2. Metallic taste in the mouth.
3. Lactic acidosis (a rare but serious complication characterized by increased levels of lactate in the blood).
4. Allergic reactions, including hives and itching, are rare.

Overdose

1. Lactate acidosis: This is a serious complication that can occur with an overdose of metformin. Lactic acidosis is characterized by a buildup of lactic acid in the body. Symptoms may include nausea, vomiting, abdominal pain, muscle weakness, fatigue, difficulty breathing, decreased body temperature, and changes in state of consciousness. Treatment includes fluid administration and correction of acid-base balance.
2. Hypoglycemia: In rare cases, metformin may cause hypoglycemia (low blood glucose), especially in people with impaired kidney function or other conditions that may impair the metabolism of metformin. Treatment includes taking carbohydrates and monitoring blood glucose levels.
3. Other undesirable effects: Other undesirable effects associated with metformin overdose are also possible, such as gastrointestinal disorders, headache, hypovitaminosis B12 and others.

Interactions with other drugs

1. Antidiabetic drugs: The combination of metformin with other antidiabetic drugs such as sulfonylurea or insulin may lead to an increased hypoglycemic effect. This may require dosage adjustments.
2. Medicines that affect kidney function: Medicines such as some nonsteroidal anti-inflammatory drugs (NSAIDs), antihypertensives, or diuretics may affect kidney function and the levels of metformin in the body.
3. Medicines that affect acid-base balance: Medicines including carbonates, acetazolamide, and others that can change the acid-base balance in the body may affect the levels of metformin in the blood.
4. Medicines that affect digestion: Medicines that decrease or improve digestion, such as antiemetics or antacids, may affect the absorption of metformin.
5. Alcohol: Drinking alcohol may increase the risk of lactic acidosis when taking metformin.
6. Other medicines: Before starting a new medicine in combination with Glucophage, it is important to consult a physician to evaluate potential interactions and adjust dosage if necessary.