Gliclazide

Gliclazide is an oral hypoglycemic drug of the sulfonylurea class that is used to treat type 2 diabetes. This drug helps control blood glucose levels by stimulating the pancreas to produce insulin. Gliclazide is effective for patients who have not achieved adequate glycemic control through diet, exercise, or other medications.

Gliclazide works by stimulating the beta cells of the pancreas to produce more insulin. Insulin is needed to help the body's cells take up glucose from the blood and use it as energy, which ultimately lowers blood glucose levels.

Indications Gliclazide

Diabetes mellitus type 2: The drug may be prescribed as monotherapy or in combination with other hypoglycemic agents such as metformin or insulin to achieve optimal blood glucose control.

Release form

Gliclazide is usually available as a tablet for oral administration. The tablets may have different dosages depending on the doctor's prescription and the patient's needs.

Pharmacodynamics

1. Stimulation of insulin release: Gliclazide acts on the beta cells of the pancreas, stimulating them to release insulin. This occurs by blocking potassium channels in the beta cells, which leads to depolarization of the cells and subsequent release of insulin.
2. Improving tissue sensitivity to insulin: Gliclazide may also increase the sensitivity of peripheral tissues to insulin, which means that the tissues respond better to insulin, enhancing its action and reducing blood sugar levels.
3. Lowering blood pressure: Some studies suggest that gliclazide may have a hypotensive effect, i.e. it may help lower blood pressure in patients with diabetes. This is due to its ability to dilate blood vessels and improve blood flow.
4. Anti-inflammatory action: Some studies also suggest that gliclazide may have anti-inflammatory properties, which may be useful in preventing or reducing inflammation associated with diabetes.

Pharmacokinetics

1. Absorption: Gliclazide is generally well absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are usually achieved 4-6 hours after administration.
2. Metabolism: The drug is metabolized in the liver to form active and inactive metabolites. The main active metabolite of gliclazide is M1, which also has a hypoglycemic effect.
3. Elimination: Gliclazide and its metabolites are eliminated primarily via the kidneys. The elimination half-life is approximately 6-12 hours.
4. Interactions: Gliclazide may interact with other medications, including anticoagulants, beta-blockers, and some antibiotics. Some medications may increase or decrease the hypoglycemic effect of gliclazide, so it is important to tell your doctor about all the medications you are taking.

Dosing and administration

The dosage and route of administration of Gliclazide may vary depending on the doctor's recommendations, the patient's health condition, and other factors. Gliclazide is usually taken orally during or immediately after meals to reduce the risk of hypoglycemia (low blood sugar).

The dosage is usually determined individually by the doctor depending on the blood glucose level and other factors. The usual starting dose for adults is 30 to 120 mg once or twice a day. The maximum daily dose can be up to 320 mg, but it is important to follow the doctor's recommendations.

Use Gliclazide during pregnancy

The use of gliclazide during pregnancy is generally not recommended. Gliclazide is a sulfonylurea drug used to treat type 2 diabetes mellitus, and its effects on pregnancy and the fetus have not been fully studied. During pregnancy, blood glucose control is essential, but other methods and drugs are usually preferred because of concerns about the safety of gliclazide and other oral hypoglycemic agents.

Risks of using gliclazide during pregnancy:

1. Hypoglycemia: Gliclazide can cause hypoglycemia, which is dangerous to both the mother and the developing fetus.
2. Effects on the fetus: Like other sulfonylurea drugs, gliclazide can cross the placenta, which could theoretically affect the fetus, although specific studies in this area are limited.

Recommendations for pregnant women:

• Alternative treatments: During pregnancy, insulin is generally recommended to control blood glucose levels because it does not cross the placenta and is considered safe for the fetus.
• Close monitoring: Women with type 2 diabetes who are planning to become pregnant or who are already pregnant should closely monitor their blood glucose levels under the guidance of their doctor. The doctor may adjust their treatment to ensure optimal diabetes control during pregnancy.
• Consulting with a doctor: Before changing or stopping any medications during pregnancy, you should consult with your doctor.

Contraindications

1. Type 1 diabetes: Gliclazide 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: Gliclazide may lower blood sugar levels, which may cause hypoglycemia (very low blood sugar). Patients at increased risk of hypoglycemia, such as the elderly or those with poor nutrition, should use gliclazide with caution.
3. Renal impairment: The use of gliclazide may be contraindicated in patients with severe renal impairment since its metabolism and elimination from the body may be impaired.
4. Liver failure: The liver plays an important role in the metabolism of gliclazide. Therefore, its use may be contraindicated or require dosage adjustment in patients with severe liver failure.
5. Pregnancy and breastfeeding: Use of gliclazide during pregnancy and breastfeeding requires special caution and consultation with a doctor.
6. Cardiovascular disease: Gliclazide may affect the cardiovascular system, so its use may be contraindicated in patients with cardiovascular disease or at risk for developing it.
7. Allergic reaction: People with a known allergy to gliclazide or other sulfonylurea drugs should avoid its use.

Side effects Gliclazide

1. Hypoglycemia: This is the most serious side effect of gliclazide. Hypoglycemia can be caused by too much low blood sugar. Symptoms of hypoglycemia include dizziness, hunger, tremors, sweating, weakness, irregular heartbeat, and even loss of consciousness.
2. Digestive disturbances: May include nausea, vomiting, diarrhea, constipation, or abdominal discomfort.
3. Allergic reactions: Some people may be allergic to gliclazide and experience skin rash, itching, swelling of the throat or face, difficulty breathing, and other signs of allergy.
4. Possible changes in liver or kidney function tests: In some cases, changes in blood tests may occur that indicate problems with the liver or kidneys.
5. Rare: Other side effects such as headache, tiredness, drowsiness, irritability, or changes in blood pressure may occur.

Overdose

1. Hypoglycemia: This is the most serious and common complication of gliclazide overdose. Overdose results in extremely low blood glucose levels, which can cause dizziness, weakness, hunger, loss of consciousness, and serious cardiac symptoms such as arrhythmias.
2. Cardiac arrhythmias: Overdose of gliclazide may cause various cardiac arrhythmias such as tachycardia, bradycardia or atrial fibrillation.
3. Arterial hypotension: Excessive drug action may lead to a decrease in blood pressure, which may cause dizziness, fainting or even collapse.
4. Other symptoms: Overdose may also cause nausea, vomiting, stomach upset, drowsiness, headache and other unwanted effects.

Interactions with other drugs

1. Hypoglycaemic agents: The use of gliclazide with other hypoglycaemic agents such as sulfonylureas or insulin may enhance the hypoglycaemic effect and increase the risk of hypoglycaemia.
2. Beta-blockers: Beta-blockers may mask symptoms of hypoglycemia such as increased heart rate or sweating, which may make it difficult to diagnose hypoglycemia in patients taking gliclazide.
3. Anticoagulants: Gliclazide may enhance the effect of anticoagulants such as warfarin, which may lead to an increased risk of bleeding. Regular monitoring of prothrombin time is necessary.
4. Antibiotics: Some antibiotics can alter blood glucose levels, which may require adjustment of the gliclazide dose.
5. Antifungals: Antifungals such as fluconazole may increase blood levels of gliclazide, requiring caution and possible dosage adjustment.