Glimekomb

Glimekomb Uses, Dosage, Side Effects, Food Interaction and all others data.

Gliclazide stimulates the release of insulin from pancreatic beta-cells by facilitating Ca++ transport across the beta-cell membranes. It lowers blood glucose by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. Extrapancreatic effects also may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. Two extrapancreatic effects shown to be important in the action of Gliclazide are an increase in insulin sensitivity and a decrease in hepatic glucose production. The anti-oxidant, platelet inhibiting and fibrinolytic actions of Gliclazide involve processes which have been implicated in the pathogenesis of vascular complications of type 2 diabetes.

Based on the pharmacological properties, gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall, it potentiates insulin release and improves insulin dynamics.

Glimekomb
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Glimekomb
Generic	Gliclazide + Metformin Hydrochloride
Type
Therapeutic Class
Manufacturer
Available Country	Russia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Gliclazide is used for control of blood glucose in patients with non-insulin dependent diabetes mellitus (Type-II, maturity onset diabetes mellitus) whose hyperglycemia cannot be controlled by diet alone.

Glimekomb is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus

How Glimekomb works

Gliclazide binds to the β cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the β cells. This opens voltage-dependent calcium channels in the β cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules.

Dosage

Glimekomb dosage

Adult: The usual initial dose of Gliclazideis 40 to 80 mg daily, gradually increased, if necessary up to 320 mg daily until adequate control is achieved. A single dose should not exceed 160 mg. When higher doses are required it should be taken twice daily, according to the main meals of the day. For extended release tablet the initial recommended dose is 30 mg daily, even in elderly patients (>65 years); the daily dose may vary from 30 to 120 mg taken orally, once daily.

Gliclazide extend release tablet should be taken with food because there is increased risk of hypoglycemia if a meal is taken late. It is recommended that the medication be taken at breakfast time. If a dose is forgotten, the dose taken on the next day should not be increased. Dose titration should be carried out in steps of 30 mg, according to the fasting blood glucose response. Each step should last for at least two weeks. Gliclazide extend release tabletshould be neither broken nor chewed. Gliclazide extend release tablet30 mg, can replace Gliclazide 80 mg tabletsfor doses of 1 to 4 tablets per day.

Elderly: Plasma clearance of Gliclazide is not altered in the elderly and steady state plasma levels are similar to those in adults under 65 years. Clinical experience in the elderly shows that it is effective and well tolerated.

Children: Gliclazide as with other sulfonylureas is not indicated for the treatment of juvenile onset diabetes mellitus.

Side Effects

Hypoglycemia may occur in concurrent conditions such as hepatic & renal diseases, alcohol intoxication and adrenal and pituitary insufficiency. Mild gastro-intestinal disturbances including nausea, dyspepsia, diarrhea, and constipation have been reported but these types of adverse reactions can be avoided if Gliclazide is taken during a meal. Allergic dermatological reactions including rash, prurits, erythema, bullous eruption have been reported during treatment with the drug but are not known to be directly attributable to it. More serious reactions like leucopenia, thrombocytopenia, agranulocytosis, pancytopenia, hemolytic anemia, cholestatic jaundice, GI hemorrhage have not been reported with Gliclazide.

Toxicity

LD₅₀=3000 mg/kg (orally in mice). Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.

Precaution

Gliclazide should be used carefully in patients with hepatic impairment. If there is definite hepatic disease then gliclazide should not be used. Consucon (Gliclazide) can be used safely in patients with renal insufficiency as it is extensively metabolized. Consucon has less sudden hypoglycaemic episode than other sulfonylurea group of drugs.

Interaction

The hypoglycemic effect of Gliclazide may be potentiated by NSAID (in particular aspirin), phenylbutazone, sulfonamides, coumarin derivatives, MAOIs, beta-adrenergic blockers, tetracyclines, chloramphenicol, clofibrate, cimetidine and miconazole tablets. Ingestion of alcohol may also increase the hypoglycemic effect of Gliclazide. Some drugs may on the contrary, reduce its activity e.g. barbiturates, corticosteroides, thiazide diuretics, thyroid hormones, laxatives and oral contraceptives.

Elimination Route

Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.

Half Life

10.4 hours. Duration of action is 10-24 hours.

Elimination Route

Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).

Pregnancy & Breastfeeding use

Pregnant Women: Gliclazide should not be used in pregnant women although animal studies of Gliclazide have not shown any teratogenic effect.

Nursing Mothers: This drug is contraindicated when breast feeding.

Contraindication

Hypersensitivity to sulfonylurea, diabetes complicated by ketoacidosis with coma, as a sole therapy of insulin-dependent (Type-1) diabetes mellitus, diabetes when complicated by pregnancy & breast-feeding.

Special Warning

Children: Gliclazide as with other sulfonylureas is not indicated for the treatment of juvenile onset diabetes mellitus.

Acute Overdose

Symptoms: Hypoglycaemia with or without coma, convulsions or other neurological disorders.

Management: Carbohydrate intake, dosage adjustment and/or change of diet may be helpful. Admin rapid IV inj of concentrated glucose soln for hypoglycaemic coma.