Glimesyn

Glimepiride.

Each Film-coated Tablet contains: Glimepiride, USP 2 mg and Glimepiride, USP 3 mg.

Pharmacology: Pharmacodynamics: Glimepiride acts mainly by stimulating insulin release from pancreatic beta cells. As with other sulphonylureas, this effect is based on an increase of responsiveness of the pancreatic beta cells to the physiological glucose stimulus. Glimepiride increases the activity of the glycosylphosphatidyl inositol specific phospholipase C which may be correlated with the drug induced lipogenesis and glycogenesis in isolated fat and muscle cells.
Pharmacokinetics: Glimepiride is completely absorbed from the gastrointestinal tract, with peak plasma concentration occurring within 2 to 3 hours. It is highly bound to plasma proteins. The drug is extensively metabolized to two main metabolites, a hydroxyl derivative and a carboxyl derivative. The half-life after multiple doses is about 9 hours. Approximately 60% of a dose is being eliminated in the urine and 40% in the feces.

Glimepiride is used for the treatment of non-insulin-dependent diabetes mellitus (Type 2 diabetes mellitus).

Adult: The usual starting dose is 1 mg or 2 mg once daily with breakfast or the first main meal. Usual maintaining dose is 1 mg to 4 mg once daily. The maximum recommended dose is 6 mg once daily. Or as prescribed by the physician.

Like other sulfonylureas, glimepiride overdose may manifest as hypoglycemia which may last for 7-12 hours and may recur after an initial recovery. Symptoms may not be present for up to 24 hours after ingestion. Aggressively treat mild hypoglycemic symptoms with oral glucose and adjust drug dosage and/or meal patterns. Continue close monitoring until the patient is out of danger. Prevent absorption of glimepiride by inducing vomiting and then drinking water or lemonade with activated charcoal (adsorbent) and sodium sulfate (laxative). Gastric lavage followed by activated charcoal and sodium sulfate is recommended in case of large ingestions of glimepiride. In case of severe hypoglycemic reactions including coma, seizure or other neurological impairment, immediate hospitalization is required. In patients with diagnosed or suspected hypoglycemic coma, rapid intravenous injection of concentrated (50%) glucose solution followed by a continuous infusion of 10% glucose solution at a rate that will maintain blood glucose level at 100 mg/dL and above should be given. Monitor patients for 24 to 48 hours to prevent recurrence of hypoglycemia. In case of accidental ingestion of glimepiride in infants and children, treat hypoglycemic symptoms by giving a carefully controlled dose of glucose (to avoid the possibility of producing hyperglycemia) and close monitoring of blood glucose until the patient is out of danger.

Use in noninsulin-dependent diabetes mellitus is contraindicated in patients with ketoacidosis and in those with severe infection, stress, trauma and other severe conditions where it is unlikely to control hyperglycemia.

Glimepiride should not be used in insulin-dependent diabetes mellitus. Hepatic and haematological monitoring is recommended in patients receiving glimepiride.

Glimepiride should not be given to pregnant or lactating woman since it is excreted in breast milk.

Gastrointestinal disorders: nausea, vomiting, heartburn, anorexia, diarrhea.
Skin disorders: Skin rashes, pruritus, photosensitivity.
Liver disorders: Altered liver enzyme values, cholestatic jaundice.
Blood and lymphatic system disorders: Leukopenia, thrombocytopenia, aplastic anemia, agranulocytosis, hemolytic anemia, erythema multiforme, exfoliative dermatitis, erythema nosodum.

Drugs which may diminish the hypoglycaemic effects of sulphonylureas. Adrenaline [epinephrine], aminoglutethimide, chlorpromazine, corticosteroids, diazoxide, oral contraceptives, rifamycins and thiazide diuretics. Drugs which increase the hypoglycaemic effect of sulphonylureas. ACE inhibitors, alcohol, allopurinol, some analgesics (azapropazone, phenylbutazone and the salicylates), azole antifungals (fluconazole, ketoconazole and miconazole), chloramphenicol, cimetidine, clofibrate and related compounds, coumarin anticoagulants, halofenate, heparin, MAOIs, octreotide, ranitidine, sulfinpyrazone, sulfonamides (including co-trimoxazole), tetracyclines, tricyclic antidepressants, and thyroid hormones. Also, beta-blockers have been reported both to increase hypoglycaemia and to mask the typical sympathetic warning signs.

Store at temperatures not exceeding 30°C.

Antidiabetic Agents

A10BB12 - glimepiride ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.

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