Gliclazide

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Clinical Pharmacology

hypoglycemic agent for oral administration of the II generation sulfonylurea group

Gliclazide is a sulfonylurea derivative, a hypoglycemic oral drug that differs from similar drugs by the presence of an N-containing heterocyclic ring with an endocyclic bond.

Gliclazide reduces the concentration of blood glucose by stimulating insulin secretion by beta cells of the islets of Langerhans. An increase in the concentration of postirandial insulin and C-peptide persists after 2 years of therapy. In addition to the effect on carbohydrate metabolism, gliclazide has hemovascular effects.

Effect on insulin secretion

In type 2 diabetes mellitus, gliclazide restores the early peak of insulin secretion in response to glucose intake and enhances the second phase of insulin secretion. A significant increase in insulin secretion is observed in response to stimulation caused by food intake or glucose administration.

Hemovascular effects

Gliclazide reduces the risk of thrombosis of small vessels, affecting the mechanisms that can cause the development of complications in diabetes mellitus: partial inhibition of platelet aggregation and adhesion and a decrease in the concentration of platelet activating factors (beta-thromboglobulin, thromboxane B2), as well as the recovery of fibrinolytic activity of the vessel, and the vessel’s fibrinolytic activity. increased activity of tissue plasminogen activator. Intensive glycemic control based on the use of prolonged-release glycazide (target glycosylated hemoglobin (HbAlc)) reliably reduces the risk of micro- and macrovascular complications of type 2 diabetes compared to standard glycemic control (ADVANCE study).

Pharmacokinetics:

Suction

After oral administration, gliclazide is completely absorbed. Meal does not affect the degree of absorption. The concentration of gliclazide in plasma increases gradually, reaching a maximum and reaching a plateau in 6-12 hours. Individual variability is relatively low. The relationship between the dose taken and the plasma concentration curve is a linear dependence on time.

Distribution

About 95% of the drug is bound to plasma proteins. Gliclazide is metabolized primarily in the liver and is excreted mainly by the kidneys. The volume of distribution is about 30 liters.

Taking the drug in a dose of 30 mg once a day maintains the effective plasma concentration of gliclazide for more than 24 hours.

Metabolism

Gliclazide is metabolized primarily in the liver. Plasma active metabolites are absent.

Removal

Excretion is carried out mainly by the kidneys in the form of metabolites, less than 1% is excreted unchanged. The elimination half-life of gliclazide averages 16 hours (from 12 to 20).

Special populations

In the elderly, clinically significant changes in pharmacokinetic parameters are not observed.

Indications

Diabetes mellitus type 2 with insufficient efficacy of diet, exercise and weight loss.

Prevention of diabetic complications: reducing the risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke) in patients with type 2 diabetes by intensive glycemic control.

Gliclazide is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Gliclazide-MV			pills
Gliclazide	Canonpharma	Russia	pills
Gliclazide	Pharmstandard	Russia	pills
Diabetalong	Synthesis AKOMP	Russia	pills
Diabefarm MV	Pharmacor Production	Russia	pills
Glidiab MB	Akrikhin	Russia	pills
Glidiab	Akrikhin	Russia	pills
Diabeton MR	Servier	France	pills

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Dosage and Administration

The drug is intended for adults only.

The recommended dose of the drug should be taken orally, 1 time / day, preferably at breakfast.

The daily dose is 30-120 mg (1-4 pills) in 1 reception. It is recommended to swallow the tablet whole, without chewing or grinding.

If you skip one or more doses of the drug, you should not take a higher dose in the next dose, the missed dose should be taken the next day. As with other hypoglycemic drugs, the dose of the drug in each case must be selected individually, depending on the concentration of blood glucose and glycated hemoglobin (HbAlc).

Initial dose

The initial recommended dose for adults who have not previously received treatment (including elderly people> 65 years) is 30 mg / day (1 tablet), then the dose is adjusted individually until the desired result is achieved.

When replacing the drug Gliclazide Canon other hypoglycemic agents do not require any transitional period of time. You must first stop taking this drug and only then take the drug Gliclazide Canon.

Dose selection

Increasing the dose is possible not earlier than after 1 month of drug therapy in the previously prescribed dose. Selection of the dose should be carried out in accordance with the indicator of the concentration of glucose in the blood after the start of treatment. Each subsequent dose change can be undertaken after at least a two-week period.

Maintenance therapy

Supporting daily dose ranges from 30 to 90-120 mg (from 1 to
3-4 pills), and should not exceed 120 mg. Gliclazide Canon can be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.

Elderly patients

The dosages recommended for the elderly are identical to those for adults under 65 years of age.

Renal failure

The recommended doses of the drug for mild to moderate renal failure are identical to those for individuals with normal renal function. It is recommended that careful medical monitoring of patients.

Patients at risk of developing hypoglycemia

In patients at risk of developing hypoglycemia (inadequate or unbalanced nutrition; severe or poorly compensated endocrine disorders - pituitary and adrenal insufficiency, hypothyroidism; cancellation of GCS after their long-term administration and / or administration in high doses; severe cardiovascular diseases ( severe ischemic heart disease, severe atherosclerosis of the carotid arteries, common atherosclerosis) is recommended to use the minimum dose (30 mg) of the drug.

Prevention of diabetes complications

To achieve intensive glycemic control, you can gradually increase the dose of Gliclazide Canon 120 mg / day in addition to diet and exercise until the target level of HbAlc is reached. It should be aware of the risk of hypoglycemia. In addition, other hypoglycemic drugs, such as metformin, an alpha-glucosidase inhibitor, a thiazolidinedione derivative or insulin, can be added to the therapy.

Adverse reactions

Hypoglycemia in the case of irregular food intake, and especially if the meal is missed, may be accompanied by the following symptoms: headache, a strong feeling of hunger, nausea, vomiting, fatigue, sleep disturbance, irritability, agitation, decreased concentration, slow reaction, depression, confusion consciousness, impaired vision and speech, aphasia, tremor, paresis, impaired perception, dizziness, weakness, convulsions, bradycardia, delirium, respiratory failure, drowsiness, loss of consciousness with possible development of coma, until death.

Andrenergic reactions may also be noted: increased sweating, sticky skin, anxiety, tachycardia, increased blood pressure, palpitations, arrhythmia, and angina.

Other side effects

On the part of the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, constipation (the severity of these symptoms is reduced when taken during meals).

On the part of the skin and subcutaneous tissue: rash, itching, urticaria, erythema, maculopapular rash, bullous reactions (such as Stevens-Johnson syndrome, toxic epidermal necrolysis).

From the circulatory and lymphatic systems: anemia, thrombocytopenia, leukopenia, granulocytopenia. As a rule, these phenomena are reversible in case of cessation of therapy.

Liver and biliary tract: increased activity of “liver” enzymes (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), alkaline phosphatase), hepatitis (isolated cases). When cholestatic jaundice appears, therapy should be discontinued.

On the part of the organ of vision: transient visual disturbances may occur, caused by changes in blood glucose concentration, especially at the beginning of therapy.

Common side effects of sulfonylurea derivatives: erythropenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia. Also, while taking other sulfonylurea derivatives, there was an increase in the activity of “liver” enzymes, impaired liver function (for example, with the development of cholestasis and jaundice) and hepatitis. These manifestations decreased with time after discontinuation of sulfonylurea drugs, but in some cases resulted in life-threatening liver failure.

Contraindications

It is not recommended to use the drug simultaneously in combination with phenylbutazone or danazol.

Carefully

Older age, irregular and / or unbalanced nutrition, severe diseases of the cardiovascular system (including ischemic heart disease, atherosclerosis), hypothyroidism, adrenal or pituitary insufficiency, hypopituitarism, renal and / or hepatic insufficiency, long-term therapy with glucocorticosteroid gidrosis, and long-term glucocorticosteroid therapy; ), alcoholism, glucose-6-phosphate dehydrogenase deficiency.

Drug interactions

1) Glyclaside-enhancing drugs (increased risk of hypoglycemia):

Contraindications

Miconazole (systemic administration or application of a gel on the mucous membrane of the oral cavity): enhances the hypoglycemic effect of gliclazide (hypoglycemia may develop up to a state of coma).

Not recommended combinations

Phenylbutazone (systemic administration) enhances the hypoglycemic effect of sulfonylurea derivatives (displaces them from binding to plasma proteins and / or slows their elimination from the body). It is preferable to use another anti-inflammatory drug. If taking phenylbutazone is necessary, the patient should be warned about the need to control the concentration of blood glucose. If necessary, the dose of gliclazide should be adjusted during and after phenylbutazone administration.

Ethanol: increases hypoglycemia, inhibiting compensatory reactions, may contribute to the development of hypoglycemic coma. It is necessary to refuse to take medications, which include ethanol, and alcohol consumption.

Combinations requiring precaution

Receiving gliclazide in combination with certain drugs, for example, other hypoglycemic agents - insulin, acarbose, biguanides; beta-blockers, dipeptidyl peptidase-4 inhibitors, glucagon-like peptide-1 receptor agonists, fluconazole; angiotensin-converting enzyme inhibitors - captopril, enalapril; blockers of H2-histamine receptors; monoamine oxidase inhibitors; sulfonamides, clarithromycin and nonsteroidal anti-inflammatory drugs, accompanied by increased hypoglycemic effect and the risk of hypoglycemia.

2) Drugs that weaken the action of gliclazide:

Not recommended combinations.

Danazol: has a diabetogenic effect. If taking this drug is necessary, the patient is advised to carefully monitor the concentration of blood glucose.If necessary, the joint intake of drugs, it is recommended that the selection of the dose of gliclazide as during the reception of danazol, and after its cancellation.

Combinations requiring precautions.

Chlorpromazine: in high doses (more than 100 mg per day) increases the concentration of glucose in the blood, reducing insulin secretion. It is recommended to carefully monitor the concentration of blood glucose. If necessary, the joint intake of drugs, it is recommended that the selection of the dose of gliclazide as during the intake of chlorpromazine, and after its cancellation.

GCS (systemic and local use: intraarticular, external and rectal administration): increase the concentration of glucose in the blood with the possible development of ketoacidosis (reduced tolerance to carbohydrates). It is recommended to carefully monitor the concentration of blood glucose, especially at the beginning of treatment. If necessary, the joint intake of drugs, it may be necessary to adjust the dose of hypoglycemic drugs both during the reception of GCS, and after their cancellation.

Ritodrin, salbutamol, terbutaline (intravenous):

Beta-2 adrenomimetics contribute to an increase in blood glucose concentration.

Special attention must be paid to the importance of self-monitoring of blood glucose concentrations. If necessary, it is recommended to transfer the patient to insulin therapy.

Combinations to be taken into account

Anticoagulants (for example, warfarin): sulfonylurea derivatives may enhance the effect of anticoagulants when taken together. May require dose adjustment of the anticoagulant.

Pregnancy and Lactation

Experience with gliclazide during pregnancy is missing.

Data on the use of other sulfonylurea derivatives during pregnancy is limited.

In studies on laboratory animals, no teratogenic effects of gliclazide were identified.

Oral hypoglycemic drugs during pregnancy are not used. The drug of choice for the treatment of diabetes in pregnant women is insulin. It is recommended to replace taking gliclazide with insulin therapy, both in the case of a planned pregnancy, and if the pregnancy occurred while taking the drug.

Breastfeeding period

Taking into account the lack of data on the entry of gliclazide into breast milk and the risk of neonatal hypoglycemia, breastfeeding is contraindicated during drug therapy.

Special instructions

When taking sulfonylurea derivatives, including gliclazide, hypoglycemia can develop, and in some cases in a severe and prolonged form that requires hospitalization and intravenous administration of a dextrose solution for several days.

The drug Gliclazid Canon can be prescribed only to those patients who regularly eat breakfast. It is very important to maintain adequate intake of carbohydrates from food, because the risk of hypoglycemia increases with irregular or malnutrition, as well as with the consumption of food, poor in carbohydrates. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol, or taking several hypoglycemic drugs at the same time.

As a rule, the symptoms of hypoglycemia disappear after a meal rich in carbohydrates (for example, sugar). It should be borne in mind that taking sweeteners does not contribute to the elimination of hypoglycemic symptoms. Experience with other sulfonylurea derivatives suggests that hypoglycemia can recur, despite effective initial relief of this condition. If the hypoglycemic symptoms have a pronounced nature or are long, even in the case of a temporary improvement after eating a meal rich in carbohydrates, it is necessary to provide emergency medical care, including hospitalization.

In order to avoid the development of hypoglycemia, a careful individual selection of drugs and a dosing regimen is necessary, as well as providing the patient with complete information about the proposed treatment.

An increased risk of hypoglycemia may occur in the following cases:

the refusal or inability of the patient (especially the elderly) to follow the doctor's prescriptions and control his condition;
inadequate and irregular meals, skipping meals, fasting and changing diets;
an imbalance between exercise and the amount of carbohydrates taken;
renal failure;
severe liver failure;
overdose of the drug Gliclazide Canon;
some endocrine disorders (thyroid disease, pituitary and adrenal insufficiency);
simultaneous intake of certain drugs.

Sulfonylurea derivatives can cause hemolytic anemia in patients with glucose-6-phosphate dehydrogenase deficiency. Since gliclazide is a sulfonylurea derivative, care must be taken when prescribing it to patients with glucose-6-phosphate dehydrogenase deficiency. You should evaluate the possibility of prescribing a hypoglycemic drug of another group.

Hepatic / Renal Failure

In patients with severe hepatic and / or renal insufficiency, the pharmacokinetic and / or pharmacodynamic properties of gliclazide may be altered. Hypoglycemia that develops in these patients can be quite long, in such cases it is necessary to immediately conduct appropriate therapy.

Patient Information

It is necessary to inform the patient and his family members about the risk of hypoglycemia, its symptoms and conditions conducive to its development. The patient must be informed of the potential risks and benefits of the proposed treatment. The patient needs to clarify the importance of dieting, the need for regular exercise and regular monitoring of blood glucose concentrations.

Insufficient glycemic control

Glycemic control in patients receiving hypoglycemic therapy may be impaired in the following cases: fever, trauma, infectious diseases, or large surgical interventions. In these conditions, it may be necessary to discontinue therapy with Gliclazide Canon and to prescribe insulin therapy. In many patients, the effectiveness of oral hypoglycemic agents, including gliclazide tends to decrease after a long period of treatment. This effect may be due to both the progression of the disease and a decrease in the therapeutic response to the drug. This phenomenon is known as secondary drug resistance, which must be distinguished from the primary, in which the drug does not give the expected clinical effect at the first appointment. Before diagnosing secondary drug resistance in a patient, it is necessary to assess the adequacy of the dose selection and their compliance with the prescribed diet.

Control of laboratory parameters

To assess the glycemic control, it is recommended to regularly determine the concentration of fasting blood glucose and glycosylated hemoglobin. In addition, it is advisable to regularly monitor blood glucose concentrations.

Influence on the ability to drive vehicles n mechanisms

Patients should be aware of the symptoms of hypoglycemia and use caution when driving or doing work that requires a high rate of psychomotor reactions, especially at the beginning of therapy.

Overdosage

An overdose of sulfonylurea derivatives, including gliclazide, can lead to the development of hypoglycemia, even hypoglycemic coma.

Moderate symptoms of hypoglycemia without impairment of consciousness or neurological symptoms are corrected by taking carbohydrates, taking a dose and / or changing a diet.Careful observation of the patient's condition should continue until there is no certainty that the health of the patient is not in danger.

Perhaps the development of severe hypoglycemic states, accompanied by coma, convulsions or other neurological disorders. If these symptoms appear, emergency medical care and immediate hospitalization are necessary. If a hypoglycemic coma is suspected or diagnosed, 50 ml of a 40% dextrose (glucose) solution is administered by intravenous injection into a patient. Then 5% dextrose solution is administered intravenously to maintain the required concentration of glucose in the blood of about 1 g / l. Careful monitoring of blood glucose concentration and patient monitoring should be carried out for at least
48 next hours. Subsequently, depending on the condition of the patient, the question of the need for further monitoring of the vital functions of the patient should be resolved.

Dialysis is ineffective due to the pronounced binding of gliclazide to plasma proteins.