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Pharmacology · Sulfonylureas

Glimepiride !

A once-daily sulfonylurea for type 2 diabetes: it increases insulin release and can cause hypoglycemia and weight gain.

Updated 2026-11-01

  • Class: Sulfonylureas
  • Ion channel: Sulfonylurea receptor 1 (SUR1) of the KATP channel
  • ATC code: A10BB12

No structure with this drug is available; the figure shows glibenclamide, another sulfonylurea that binds the same SUR1 pocket of the KATP channel (hamster SUR1, rat Kir6.2).

Target in 3D: Sulfonylurea receptor 1 (SUR1) of the KATP channel. PDB structure 6BAA (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Glimepiride binds SUR1 and closes the beta-cell KATP channel; depolarization opens calcium channels and insulin is released, regardless of the glucose level. Its long action allows once-daily use.

  1. Binds SUR1 on the beta-cell KATP channel
  2. The channel closes and the membrane depolarizes
  3. Calcium channels open and insulin granules are released
  4. Glucose falls, even when it is already low

Pharmacokinetics

Absorption
Oral, well absorbed.
Metabolism
In the liver by CYP2C9.
Elimination
Urine and feces as metabolites; kidney impairment raises hypoglycemia risk.

Indications

Adverse effects

Common

  • Hypoglycemia
  • Weight gain
  • Dizziness, nausea, headache

Contraindications

  • Hypersensitivity to glimepiride
  • Hypersensitivity to sulfonamide derivatives
  • Type 1 diabetes and ketoacidosis (not effective)

Key interactions

Insulin and other glucose-lowering drugs
Add to hypoglycemia.
Beta-blockers
Can increase the effect and blunt the warning signs of hypoglycemia.
NSAIDs and salicylates, sulfonamides, fluoroquinolones, oral azole antifungals (miconazole)
Can increase the glucose-lowering effect and cause severe hypoglycemia.
Alcohol
Raises the risk of hypoglycemia.
Colesevelam
Reduces glimepiride absorption, so they are given hours apart.

What is monitored

  • Capillary glucose
  • HbA1c
  • Kidney function

Administration and safety

  • Oral tablet, given with a meal (usually breakfast); a skipped meal raises hypoglycemia risk.
  • Look-alike names: glipizide, glyburide (glibenclamide) and glimepiride are easily confused.
  • Often held while the patient is fasting (nil by mouth) in hospital.

Nursing care

  • Before: capillary glucose, kidney and liver function, meal intake, age.
  • During: signs of hypoglycemia (sweating, tremor, confusion); beta-blockers can mask them.
  • After a hypoglycemia episode: glucose is rechecked for many hours, because it can come back.
  • Teach: carry fast sugar, avoid skipping meals, limit alcohol.

Pregnancy and breastfeeding

Insulin is the usual choice. A sulfonylurea taken near delivery can cause prolonged hypoglycemia in the newborn.

Test yourself

Think of the answer, then tap the question to see it.

Which drug allergy is a contraindication to glimepiride?

Hypersensitivity to sulfonamide derivatives.

Which enzyme metabolizes glimepiride?

CYP2C9 in the liver; its inhibitors can raise levels and hypoglycemia risk.

Why are colesevelam and glimepiride given hours apart?

Colesevelam binds glimepiride in the gut and reduces its absorption.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Glimepiride: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - GLIMEPIRIDE- glimepiride tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.