Brand Name: Glimide
Generic Name: Glimepiride
Preparations: 1/2/3 mg Tablets
Pharmacological Category: Sulphonylurea

Mechanism of Action (MOA)
GLIMIDE (Glimepiride) binds to its receptor on ATP-sensitive potassium channel present on the pancreatic cell surface thereby reducing potassium conductance. This causes depolarization of the membrane leading to increase in insulin production.

GLIMIDE may also decrease rate of hepatic glucose production and increase insulin receptor sensitivity.

Pharmacokinetics
Absorption: Completely absorbed from gastrointestinal tract
Bioavailability: 100%
Initial Effect: 1 hour
Peak Plasma Concentrations: 2 to 3 hours
Protein Binding: 99.5%
Metabolism: Extensively metabolised to a hydroxy derivative and a carboxy derivative
Elimination Half-life: 5-9 hours
Excretion: Urine (60%) and faeces (40%)

Indications and Dosage
Type 2 diabetes mellitus: Initially 1 mg to 2 mg daily after breakfast or with first meal; may be increased by 1 mg to 2 mg every 1 to 2 weeks if necessary for maintenance.

The maximum recommended dose is up to 8 mg.

Side Effects
More than 10%: Hypoglycemia
1-10%: Dizziness, asthenia, headache, nausea
Less than 1%: Allergic skin reactions, erythema, morbilliform or maculopapular eruption, pruritus, urticaria, diarrhea, gastrointestinal pain, vomiting, agranulocytosis, anemia, aplastic anemia, leucopenia, pancytopenia, thrombocytopenia, cholestasis, elevation of liver enzyme levels, hepatic porphyria reactions, jaundice (rare), disulfiram-like reaction, hyponatremia

Contraindications
Hypersensitivity, type 1 diabetes mellitus, diabetic ketoacidosis (with or without coma), complicated gestational diabetic mellitus

Warnings/ Precautions
• Caution in patients with risk of severe hypoglycemia: elderly, debilitated, or malnourished; adrenal or pituitary insufficiency; patients with stress due to infection, fever, trauma, or surgery.
• Caution in hepatic/renal impairment.
• Persons allergic to other sulfonamide derivatives may develop allergic reaction to glimepiride.
• Hemolytic anemia may occur with glucose 6-phosphate dehydrogenase (G6PD) deficiency.
• Fluid retention, which may exacerbate or lead to heart failure, may occur.
• Combination use with insulin and use in congestive heart failure may increase risk of other cardiovascular effects.

Drug Interactions
• A diminished hypoglycaemic effect, possibly requiring an increased dose of sulfonylurea, has been seen with adrenaline, aminoglutethimide, chlorpromazine, corticosteroids, diazoxide, oral contraceptives, rifamycins, thiazide diuretics, and thyroid hormones.
• An increased hypoglycaemic effect has occurred with ACE inhibitors, alcohol, allopurinol, azole antifungals (fluconazole, ketoconazole, and miconazole), chloramphenicol, cimetidine, clofibrate and related compounds, coumarin anticoagulants, fluoroquinolones, heparin, MAOIs, tetracyclines, and tricyclic antidepressants.
• Beta blockers have been reported both to increase hypoglycaemia and to mask the typical sympathetic warning signs.

Pregnancy Category: C

Presentations
GLIMIDE 1: 10 X 15’s
GLIMIDE 2: 10 X 15’s
GLIMIDE 3: 10 X 15’s