Description
Gliclazide MR Pharmacodynamics
Gliclazide is a sulfonylurea derivative, hypoglycemic drug for oral administration, which differs from similar drugs by the presence of N-containing heterocyclic ring with endocyclic bond.
Gliclazide reduces blood glucose concentration by stimulating insulin secretion by β-cells of Langerhans islets. Increased concentration of postprandial insulin and C-peptide persists after 2 years of therapy.
In addition to its effect on carbohydrate metabolism, gliclazide has hemovascular effects.
Effects on insulin secretion
In type 2 diabetes, 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
Gliclazid decreases the risk of small vessel thrombosis by acting on the mechanisms which may contribute to the development of complications in diabetes: partial inhibition of platelet aggregation and adhesion and reduction of platelet-activating factors (beta-thromboglobulin, thromboxane B2), restoration of fibrinolytic activity of vascular endothelium and increase of tissue plasminogen activator activity. Intensive glycemic control based on the use of gliclazide with modified release (target glycosylated hemoglobin (HbAlc) < 6.5%) significantly reduces the risk of micro- and macrovascular complications of type 2 diabetes compared with standard glycemic control (ADVANCE study).
Indications
Diabetes mellitus type 2 with insufficient effectiveness of diet therapy, physical activity and body weight reduction.
Prevention of diabetes complications: reduction of risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke) in patients with type 2 diabetes by intensive glycemic control.
Contraindications
Hypersensitivity to gliclazide or any of the excipients of the drug, other sulfonylurea derivatives, sulfonamides;
diabetes mellitus type 1;
diabetic ketoacidosis, diabetic precoma, diabetic coma;
Severe renal or hepatic insufficiency;
taking miconazole;
Pregnancy and lactation;
Age under 18 years old.
It is not recommended to use the drug simultaneously in combination with phenylbutazone or dan azole.
Caution:
Elderly age, irregular and/or unbalanced diet, severe cardiovascular diseases (including coronary heart disease, atherosclerosis), hypothyroidism, adrenal or pituitary insufficiency, hypopituitarism, renal and/or liver failure, long-term therapy with glucocorticosteroids (GCS), alcoholism, glucose-6-phosphate dehydrogenase deficiency.
Pregnancy and lactation:
There is no experience with the use of gliclazide during pregnancy.
Data on the use of other sulfonylurea derivatives during pregnancy are limited.
Teratogenic effects of gliclazide have not been identified in studies on laboratory animals.
Oral hypoglycemic drugs are not used during pregnancy. The drug of choice for the therapy of diabetes mellitus in pregnant women is insulin. It is recommended to replace gliclazide with insulin therapy both in case of a planned pregnancy, and if pregnancy occurs against the background of taking the drug.
Breastfeeding period
Taking into account the lack of data on the intake of gliclazide in breast milk and the risk of neonatal hypoglycemia, breastfeeding is contraindicated during therapy with the drug.
Dosage and administration
- The drug is intended for adults only.
The recommended dose of the drug should be taken orally, 1 time per day, preferably during breakfast. - The daily dose is 30-120 mg (1-4 tablets) at 1 sitting. It is recommended to swallow the tablet whole, without chewing and crushing.
- If you miss one or more doses of the drug, you should not take a higher dose at the next appointment, the missed dose should be taken the next day. As with other hypoglycemic drugs, the drug dose in each case should be adjusted individually, depending on the blood glucose concentration and glycosylated hemoglobin (HbAlc).
- Initial dose
Recommended initial dose in adults who have not been treated earlier (including elderly patients >65 years old) – 30 mg/day (1 tablet), then the dose is adjusted individually in order to achieve the desired result.
When replacing Gliclazide MB with another hypoglycemic drug, no transition time is required. It is necessary to stop taking this drug first and only then take Gliclazide MB. - Dose adjustment
Dosage adjustment should be made according to the blood glucose concentration after the start of treatment. Each subsequent dose adjustment can be made after a minimum of two weeks. - Maintenance Therapy
The maintenance daily dose is 1 to 3 to 4 tablets and should not exceed 120 mg. Gliclazide MB may be used in combination with biguanidines, alpha-glucosidase inhibitors, or insulin. - Elderly Persons
Recommended dosages for the elderly are identical to those for adults under 65 years of age. - Renal failure
Recommended drug doses in mild to moderate renal insufficiency are identical with those in individuals with normal renal function. - Patients at risk of hypoglycemia
In patients belonging to a group of risk of hypoglycemia (insufficient or unbalanced nutrition; severe or poorly compensated endocrine disorders – pituitary and adrenal insufficiency, hypothyroidism; withdrawal of GCS after their long period of use and/or administration in high doses; severe diseases of cardiovascular system (severe coronary heart disease, severe atherosclerosis of carotid arteries, widespread atherosclerosis) the minimum dose (30 mg) of GliClazide MB is recommended. - Prevention of diabetes complications
To achieve intensive glycemic control, the dose of Gliclazide MB can be gradually increased to 120 mg/day in addition to diet and exercise until the target HbAlc level is achieved. The risk of hypoglycemia should be kept in mind. In addition, other hypoglycemic drugs such as metformin, alpha-glucosidase inhibitor, thiazolidinedione derivative, or insulin may be added to therapy.
