[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [GLP-1 receptor agonists](https://durgical.com/en/pharmacology/classes/glp-1-receptor-agonists/) › Exenatide [Pharmacology](https://durgical.com/en/pharmacology/) · [GLP-1 receptor agonists](https://durgical.com/en/pharmacology/classes/glp-1-receptor-agonists/) # Exenatide The first GLP-1 agonist: a synthetic copy of exendin-4, a peptide from Gila monster saliva. Injected twice a day, or weekly as a slow-release form. Updated 2026-11-01 - Class: [GLP-1 receptor agonists](https://durgical.com/en/pharmacology/classes/glp-1-receptor-agonists/) - Receptor: GLP-1 receptor (GLP1R) - ATC code: A10BJ01 ◎**GLP-1 receptor (GLP1R)**Exenatide ⓘ The figure shows exendin-4 (the natural peptide whose synthetic form is exenatide) bound to the human GLP-1 receptor with its Gs protein. **Target in 3D:** GLP-1 receptor (GLP1R). PDB structure 7LLL (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/7LLL) · Drag to rotate · pinch to zoom ## Mechanism of action Exenatide is synthetic exendin-4, a reptile peptide that shares about half of its sequence with human GLP-1 and is not cut by DPP-4. It activates the GLP-1 receptor: glucose-dependent insulin release rises, glucagon falls after meals, the stomach empties more slowly and appetite falls. - Activates the GLP-1 receptor (Gs, cAMP) - Beta cells release more insulin when glucose is high - Glucagon falls and the stomach empties more slowly - Appetite falls: lower glucose and weight ## Pharmacokinetics **Absorption** Subcutaneous injection; the short form is given before meals, the extended-release form weekly. **Elimination** Mainly by the kidney (filtration and breakdown), so it is avoided in severe kidney failure. ## Indications - Type 2 diabetes, with diet and exercise, alone or combined [Type 2 diabetes mellitus →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/) ## Adverse effects ### Common - Nausea, vomiting, diarrhea, constipation, abdominal pain (most common, mostly at the start) - Reduced appetite - Injection-site reactions - Slightly faster heart rate ### Serious (rare, important) - Acute pancreatitis - Kidney injury, mostly from dehydration - Gallbladder disease - Hypoglycemia with sulfonylureas or insulin ## Contraindications - Severe kidney failure - Serious hypersensitivity to exenatide - Medullary thyroid carcinoma or MEN 2 (GLP-1 class caution) ## Key interactions **Insulin or sulfonylureas** Higher risk of hypoglycemia; their dose is often reduced. **Oral drugs in general** Slower gastric emptying can change their absorption. **Oral contraceptives and antibiotics** Usually taken well before the injection, so slowed gastric emptying does not reduce their absorption. ## What is monitored - HbA1c and weight - Kidney function - Symptoms of pancreatitis ## Administration and safety - Subcutaneous injection in the abdomen, thigh or upper arm, rotating sites. - Pens are for one person only and are never shared, even with a new needle. - The short-acting form is injected before meals, not after them. - Unopened pens are kept in the refrigerator, not frozen. ## Nursing care - Before: thyroid history (medullary carcinoma, MEN 2), pancreatitis history, kidney function. - During: severe abdominal pain spreading to the back (pancreatitis), vomiting and dehydration. - Teach to report a neck lump, hoarseness or trouble swallowing. - The anesthesia team is told before surgery or endoscopy. ## Pregnancy and breastfeeding Not used in pregnancy (weight loss is not a goal and animal data showed harm); it is stopped ahead of a planned pregnancy. ## Memory aid Exenatide came from a lizard: the Gila monster's 'exendin' resists DPP-4 naturally. Lizard peptide, human receptor. ## Test yourself Think of the answer, then tap the question to see it. ## Where does exenatide come from? It is a synthetic copy of exendin-4, a peptide found in the saliva of the Gila monster (Heloderma suspectum). ## Why is exenatide avoided in severe kidney failure? It is cleared mainly by the kidney, so it accumulates and side effects increase. ## Why is exenatide not broken down by DPP-4? Its sequence differs from GLP-1 at the N-terminal cutting site, so the enzyme cannot inactivate it. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/exenatide/) ## Related drugs - [Liraglutide](https://durgical.com/en/pharmacology/liraglutide/) - [Semaglutide](https://durgical.com/en/pharmacology/semaglutide/) - [Dulaglutide](https://durgical.com/en/pharmacology/dulaglutide/) ## Related conditions - [Type 2 diabetes mellitus](https://durgical.com/en/conditions/type-2-diabetes-mellitus/) [← Back to the class: GLP-1 receptor agonists](https://durgical.com/en/pharmacology/classes/glp-1-receptor-agonists/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [Exenatide Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a605034.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Exendin-4-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein](https://www.rcsb.org/structure/7LLL) (RCSB Protein Data Bank, 2022); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 51 (McGraw Hill, 2023); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BJ01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/exenatide/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/exenatide/