1. Glimepiride
2. Pharmacological Class: Second/Third-Generation Sulfonylurea; Pancreatic Beta-Cell Insulin Secretagogue • 3. Therapeutic Category: Antidiabetic Medicines, Insulins & GLP-1 Agonists (Ch 04)
4. Clinical Overview & Verified Formulation Identity
Glimepiride
Code: [4.5] | Stable ID: TIP-MED-000049
Representative Indian Market Examples (Edition 2.7 Ch 04 [4.5], p. 47): Amaryl (Sanofi), Glimestar (Mankind), Glimy (Dr. Reddy's), Azulix (Torrent), Zoryl (Intas), GP (USV); In FDC with Metformin: Glycomet-GP 1/2, Amaryl-M, Glimestar-M ā Strengths & Forms: Oral Uncoated Scored Tablets: 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
Oral Uncoated Scored Tablets: 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
Route: Oral / Parenteral / Topical as specified by formulation
Schedule H Prescription Drug ā¢ NLEM 2022 Core Essential Medicine
True
5 & 6. Mechanism of Action & Pharmacodynamics
Binds to the 65-kDa site on the Sulfonylurea Receptor 1 (SUR1) regulatory subunit of the ATP-sensitive potassium (K_ATP / Kir6.2) channel on pancreatic islet beta-cell membranes. Channel closure prevents K+ efflux, depolarizing the beta-cell membrane, opening voltage-gated L-type Ca2+ channels, and triggering Ca2+-dependent exocytosis of preformed insulin granules.
8. Therapeutic Indications
- Type 2 Diabetes Mellitus (as adjunct to Metformin, diet, and exercise when glycaemic targets are not achieved)
10. Dosage and Administration (Educational Reference Summary)
Administration & Timing: Oral; administer immediately before or during the first substantial meal of the day. Never take if skipping a meal.
11 & 13. Contraindications, Precautions and Warnings
- Type 1 Diabetes Mellitus or Diabetic Ketoacidosis (DKA)
- Severe renal or severe hepatic impairment
- Pregnancy and lactation
- Hypersensitivity to sulfonylureas or sulfonamides
Contraindicated in severe hepatic insufficiency (impaired gluconeogenic counter-regulation).
7, 12, 14ā18. Detailed Pharmacokinetics, Interactions, Special Populations & Counselling
7 & 16. Pharmacokinetics (ADME) & Renal / Hepatic Considerations
7. Pharmacokinetics (Absorption, Distribution, Metabolism, Excretion): Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
16a. Renal Considerations: Initiate conservatively at 1 mg/day in CKD due to renal clearance of active M1 metabolite and heightened prolonged hypoglycaemia risk; avoid in severe renal failure (eGFR < 30 mL/min).
16b. Hepatic Considerations: Contraindicated in severe hepatic insufficiency (impaired gluconeogenic counter-regulation).
12 & 14. Adverse Effects & Drug Interactions
- Hypoglycaemia (sweating, tremor, palpitations, confusion, neuroglycopenia ā lower risk than Glibenclamide but still ISMP High-Alert)
- Modest weight gain (1.5ā3 kg)
- Rare cholestatic jaundice, hyponatraemia, or blood dyscrasias
- CYP2C9 inhibitors (Fluconazole, Voriconazole, Sulfamethoxazole-Trimethoprim, Metronidazole, Amiodarone): precipitate severe, prolonged hypoglycaemia
- Beta-blockers (Propranolol, Metoprolol): mask adrenergic warning signs of hypoglycaemia and impair glycogenolysis
- Alcohol: inhibits hepatic gluconeogenesis and causes severe hypoglycaemia
15, 17 & 18. Special Populations, Clinical Monitoring & Patient Counselling
15. Use in Special Populations (Pregnancy, Lactation, Paediatrics, Geriatrics): Evaluate maternal-foetal benefit-risk ratio, paediatric mg/kg ceiling, and geriatric renal function prior to prescribing.
17. Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.
18. Patient Counselling & Storage:- Take with breakfast; NEVER take Glimepiride if you plan to fast or skip a meal.
- Always carry fast-acting glucose (15 g glucose tablets or 3 teaspoons of sugar) to treat symptoms of low blood sugar (Rule of 15).
- Inform physician before taking antifungals (Fluconazole) or antibiotics (Cotrimoxazole).
Storage & Dispensing Notes: Store below 30Ā°C in a dry place.
Visual Pharmacology Illustration (PLATE-8.11)
19. Authoritative References & Source Traceability
Primary Reference Record: Indian Pharmacopoeia (IP 2026) ā¢ NLEM 2022 (MoHFW) ā¢ CDSCO Approved Prescribing Information
Verification Portals: Indian Pharmacopoeia Commission (IPC) • CDSCO (India Jurisdiction) • NCBI Bookshelf • DailyMed (US FDA Label Reference)
Last Reviewed Date: 2026-11-08 • Related Study Guide: Type 2 Diabetes Mellitus Pharmacotherapy Guide →