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[Pharmacology](https://durgical.com/en/pharmacology/) · [Sulfonylureas](https://durgical.com/en/pharmacology/classes/sulfonylureas/)

# Glibenclamide

A potent, long-acting sulfonylurea: it forces the pancreas to release insulin and carries the highest risk of hypoglycemia in its class.

Updated 2026-11-01

- Class: [Sulfonylureas](https://durgical.com/en/pharmacology/classes/sulfonylureas/)
- Ion channel: Sulfonylurea receptor 1 (SUR1) of the KATP channel
- ATC code: A10BB01

## ⚠ High-alert medication

An error with this medicine can cause serious harm: double checks and protocols are used.

Also called: glyburide

⇅**Sulfonylurea receptor 1 (SUR1) of the KATP channel**Glibenclamide

ⓘ The figure shows glibenclamide bound to SUR1 in the complete KATP channel (hamster SUR1 with rat Kir6.2, proteins very similar to the human ones).

**Target in 3D:** Sulfonylurea receptor 1 (SUR1) of the KATP channel. PDB structure 6BAA (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6BAA) · Drag to rotate · pinch to zoom

## Mechanism of action

Glibenclamide binds SUR1 with high affinity and closes the KATP channel of the beta cell. The membrane depolarizes, L-type calcium channels open and insulin is released whatever the glucose level. Its active metabolites and tight binding make the effect long, which is why hypoglycemia with glibenclamide can be severe and recurrent.

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

## Pharmacokinetics

**Absorption**
Oral, well absorbed.

**Distribution**
Highly bound to plasma proteins.

**Metabolism**
In the liver to metabolites that keep some activity.

**Elimination**
Bile and urine; kidney or liver failure raises levels and hypoglycemia risk.

## Indications

- Type 2 diabetes, with diet and exercise [Type 2 diabetes mellitus →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

## Adverse effects

### Common

- Hypoglycemia
- Weight gain
- Nausea, heartburn, fullness
- Rash, itching, hives

### Serious (rare, important)

- Severe, prolonged or recurrent hypoglycemia, especially in older adults and in kidney failure
- Hemolytic anemia in G6PD deficiency
- Disulfiram-like reaction with alcohol (very rare)

## Contraindications

- Type 1 diabetes
- Diabetic ketoacidosis
- Use together with bosentan
- Hypersensitivity to the drug

## 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.

**Bosentan**
Contraindicated: liver enzyme rises when combined.

## What is monitored

- Capillary glucose, especially at the start and in older adults
- HbA1c
- Kidney and liver 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.

## Memory aid

Glibenclamide is the 'heavy hammer' of the sulfonylureas: it hits SUR1 hard and long. The longer the hammer swings, the longer the low sugar lasts.

## Test yourself

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

## Why is glibenclamide avoided in frail older adults?

Its long action and active metabolites, plus reduced kidney function with age, make severe and prolonged hypoglycemia more likely.

## What blood disorder can sulfonylureas trigger in G6PD deficiency?

Hemolytic anemia.

## A patient on glibenclamide is treated for hypoglycemia and wakes up. Can the team relax?

No. Hypoglycemia can return for many hours as the drug keeps acting, so glucose is rechecked repeatedly and glucose support may be needed.

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## Related drugs

- [Gliclazide](https://durgical.com/en/pharmacology/gliclazide/)
- [Glimepiride](https://durgical.com/en/pharmacology/glimepiride/)
- [Glipizide](https://durgical.com/en/pharmacology/glipizide/)
- [Diazoxide](https://durgical.com/en/pharmacology/diazoxide/)

## Related conditions

- [Type 2 diabetes mellitus](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

[← Back to the class: Sulfonylureas](https://durgical.com/en/pharmacology/classes/sulfonylureas/)

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

Sources: [Glyburide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a684058.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - GLYBURIDE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a56f100f-0f42-4188-81ab-04644b824040) (DailyMed (U.S. National Library of Medicine), 2026); [Cryo-EM structure of the pancreatic beta-cell KATP channel bound to ATP and glibenclamide](https://www.rcsb.org/structure/6BAA) (RCSB Protein Data Bank, 2017); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BB01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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