Glimepiride
A sulfonylurea taken once daily with breakfast to boost insulin release in type 2 diabetes.
Drug card
- Class
- Sulfonylurea
- How it works
- Closing KATP channels on beta cells, so the pancreas releases insulin
- Used for
- Type 2 diabetes
- Known for
- Low blood sugar (hypoglycemia)
- Weight gain
- Its name
- gli- means a glucose-lowering drug, often a sulfonylurea
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does glimepiride work?
Glimepiride binds the sulfonylurea receptor on beta cells and closes ATP-sensitive potassium channels, so insulin is released. Levels peak 2 to 3 hours after a dose; it is over 99.5% bound to plasma proteins and is fully metabolized in the liver, where CYP2C9 is involved, so CYP2C9 inhibitors and inducers alter its effect.
Like other sulfonylureas: Sulfonylureas bind the SUR1 subunit of ATP-sensitive potassium (KATP) channels on pancreatic beta cells and close them. Calcium then enters through voltage-gated channels and triggers the release of stored insulin. They need working beta cells, so they do not help type 1 diabetes, and a missed meal while taking them can cause hypoglycemia.
Uses
What is glimepiride used for?
- Type 2 diabetes
Side effects
Side effects of glimepiride
- Low blood sugar (hypoglycemia)Known forSerious
- Weight gainKnown for
- Headache
- Nausea
- Severe allergic reaction (anaphylaxis, angioedema)Serious
- Stevens-Johnson syndromeSerious
- Hemolytic anemia, with or without G6PD deficiencySerious
- Hepatitis or cholestatic jaundice, rarely liver failureSerious
- Blood disorders such as agranulocytosis (rare)Serious
- Low sodium (hyponatremia)Serious
- Sun sensitivity (photosensitivity)
- Possible rise in cardiovascular deaths (label warning)Serious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Contraindicated in people allergic to glimepiride or to sulfonamide derivatives.
- Start low in older people and those with kidney impairment, who are most prone to hypoglycemia.
- Oral miconazole can cause severe hypoglycemia; fluconazole and other CYP2C9 inhibitors raise its effect.
- Give it at least 4 hours before colesevelam, which reduces its absorption.
Good to know: Taken once a day with the first meal; like all sulfonylureas it causes weight gain.
Remember it
A way to remember it
Sulfonylureas squeeze insulin out of the beta cell: skip a meal and you get a hypo, and the extra insulin adds weight.
They close KATP channels so beta cells release insulin. Hypoglycemia, worst when meals are missed, and weight gain are the two classic side effects.
Written for biofideX
Its name
gli- means glucose-lowering drug, often a sulfonylurea
At the start of a name it mostly marks sulfonylureas: gliclazide, glimepiride, glibenclamide (US glyburide). The same letters sit inside -gliptin, -gliflozin and -glitazone.
- Every drug name stem
Its class
Sulfonylureas
Other sulfonylureas with a card:
Easily mixed up with DPP-4 inhibitors and SGLT2 inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Diabetes
Glimepiride is one of 14 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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