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GLP-1 Receptor Agonist

Semaglutide

A long-acting GLP-1 receptor agonist, given by weekly injection or as a daily tablet, for type 2 diabetes and weight management.

Drug card

How it works
Activating GLP-1 receptors, raising insulin and curbing appetite
Used for
  • Type 2 diabetes
  • Weight management in obesity or overweight
  • Cutting heart attack and stroke risk in heart disease
  • Slowing kidney decline in type 2 diabetes
Known for
  • Nausea
  • Inflammation of the pancreas (pancreatitis)
  • Thyroid C-cell tumors in rodents (human risk unknown)
Its name
-glutide means a GLP analogue (mostly GLP-1 agonists)

Study it as a flashcard, and it comes back before you forget it.

Mechanism of action

How does semaglutide work?

Semaglutide is a modified GLP-1 that shares 94% of its sequence with the human hormone and resists DPP-4. It binds albumin, which slows its clearance by the kidney and gives a half-life of about a week, so injections are weekly. It raises glucose-dependent insulin release, lowers glucagon, slightly delays stomach emptying and acts on the brain to reduce appetite.

Like other GLP-1 receptor agonists: GLP-1 receptor agonists activate the receptor for glucagon-like peptide-1, a Gs-coupled receptor that raises cAMP in beta cells. Insulin release rises and glucagon falls only when glucose is high, the stomach empties more slowly, and receptors in the brain cut appetite, so glucose and body weight fall. Unlike natural GLP-1, which DPP-4 inactivates within minutes, they resist breakdown and last hours to days.

Uses

What is semaglutide used for?

  • Type 2 diabetes
  • Weight management in obesity or overweight
  • Cutting heart attack and stroke risk in heart disease
  • Slowing kidney decline in type 2 diabetes

Side effects

Side effects of semaglutide

  • NauseaKnown for
  • Inflammation of the pancreas (pancreatitis)Known forSerious
  • Thyroid C-cell tumors in rodents (human risk unknown)Known forSerious
  • Vomiting
  • Diarrhea
  • Constipation
  • Gallstones and gallbladder inflammationSerious
  • Worse diabetic retinopathySerious
  • Sudden loss of vision in one eye (very rare)Serious
  • Kidney injury from dehydrationSerious
  • Hair loss
  • Swelling of face and throat (angioedema)Serious

Known for marks what an exam expects you to know it for.

Watch for

Cautions and what sets it apart

  • Contraindicated if the person or a close relative has had medullary thyroid cancer, and in MEN 2.
  • Watch people with diabetic retinopathy: a rapid fall in glucose can make it worse for a time.
  • Do not combine it with other semaglutide products or other GLP-1 receptor agonists.
  • Stop it if pancreatitis is suspected, and never restart it once pancreatitis is confirmed.

Good to know: Its half-life of about a week allows weekly injections; it is also made as a daily tablet for type 2 diabetes.

Remember it

A way to remember it

GLP-1 agonists put the brakes on the stomach.

Slower stomach emptying and a fuller feeling cut appetite and weight, and the same effect explains the nausea and vomiting and the risk of aspiration under anesthesia.

Written for biofideX

Its name

  • -glutide means GLP analogue (mostly GLP-1 agonists)

    Semaglutide, liraglutide and dulaglutide are GLP-1 receptor agonists; WHO files the stem under -tide (peptides). Exenatide and lixisenatide end in -enatide instead.

  • Every drug name stem

Its class

GLP-1 receptor agonists

Other GLP-1 receptor agonists with a card:

Easily mixed up with DPP-4 inhibitors and insulins.

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.

Practice it

Diabetes

Semaglutide 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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