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# GLP-1 receptor agonists

Injected (and one oral) drugs that copy the gut hormone GLP-1: more insulin after meals, less appetite, weight loss.

Updated 2026-11-01

## What they are

Incretin mimetics resistant to DPP-4. Used in type 2 diabetes, obesity and to lower cardiovascular risk.

## Mechanism of action

They activate the GLP-1 receptor, a class B G-protein-coupled receptor linked to Gs and cAMP. In beta cells this boosts insulin release only when glucose is high (glucose-dependent); in alpha cells it lowers glucagon. They also slow gastric emptying and act on the hypothalamus and brainstem to reduce appetite. Natural GLP-1 lasts minutes because DPP-4 cuts it; the drugs are protected by amino-acid changes, fatty-acid chains or fusion to large proteins.

Target: GLP-1 receptor (GLP1R), class B GPCR

## Key points

- Boxed warning: thyroid C-cell tumors in rodents; contraindicated with a personal or family history of medullary thyroid carcinoma or MEN 2.
- Acute pancreatitis: stop the drug if persistent severe abdominal pain appears.
- Nausea, vomiting and diarrhea are the most common effects; dehydration can injure the kidney.
- Weight loss and, for several agents, fewer heart attacks and strokes in people with type 2 diabetes and cardiovascular disease.
- Alone they rarely cause hypoglycemia, but they add to it with insulin or sulfonylureas; slowed gastric emptying matters before anesthesia.

## Drugs in this class

- [**Semaglutide** A long-acting GLP-1 agonist, weekly by injection or daily by mouth: strong glucose lowering, large weight loss and… GLP-1 receptor (GLP1R)](https://durgical.com/en/pharmacology/semaglutide/)
- [**Liraglutide** A once-daily injected GLP-1 agonist for type 2 diabetes and, at other doses, obesity. It raises insulin after meals… GLP-1 receptor (GLP1R)](https://durgical.com/en/pharmacology/liraglutide/)
- [**Dulaglutide** A weekly injected GLP-1 agonist fused to an antibody fragment. It lowers glucose and cardiovascular events in type 2… GLP-1 receptor (GLP1R)](https://durgical.com/en/pharmacology/dulaglutide/)
- [**Tirzepatide** A weekly injection that activates both GIP and GLP-1 receptors: large falls in glucose and weight. Used in type 2… GIP receptor and GLP-1 receptor (dual agonist)](https://durgical.com/en/pharmacology/tirzepatide/)
- [**Exenatide** The first GLP-1 agonist: a synthetic copy of exendin-4, a peptide from Gila monster saliva. Injected twice a day, or… GLP-1 receptor (GLP1R)](https://durgical.com/en/pharmacology/exenatide/)

## Others in the class

- lixisenatide

## Test yourself

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

## Why do GLP-1 agonists rarely cause hypoglycemia on their own?

Their effect on insulin release is glucose-dependent: when glucose falls toward normal, the extra insulin release stops.

## Which personal or family history rules out a GLP-1 agonist?

Medullary thyroid carcinoma or multiple endocrine neoplasia type 2 (MEN 2).

## How does a GLP-1 agonist differ from a DPP-4 inhibitor?

The agonist gives drug levels far above natural GLP-1 and causes weight loss; a DPP-4 inhibitor only protects the body's own incretins, has a smaller effect and is weight-neutral.

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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: [Semaglutide Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a618008.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [DailyMed - LIRAGLUTIDE injection, solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bb66a46c-9019-4a98-8e5d-581109facfba) (DailyMed (U.S. National Library of Medicine), 2026); [Semaglutide-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in Complex with Gs protein](https://www.rcsb.org/structure/7KI0) (RCSB Protein Data Bank, 2021).

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