[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/) › Tirzepatide [Pharmacology](https://durgical.com/en/pharmacology/) · [GLP-1 receptor agonists](https://durgical.com/en/pharmacology/classes/glp-1-receptor-agonists/) # Tirzepatide A weekly injection that activates both GIP and GLP-1 receptors: large falls in glucose and weight. Used in type 2 diabetes and obesity. Updated 2026-11-01 - Class: [GLP-1 receptor agonists](https://durgical.com/en/pharmacology/classes/glp-1-receptor-agonists/) - Receptor: GIP receptor and GLP-1 receptor (dual agonist) - ATC code: A10BX16 - WHO Model List of Essential Medicines ◎**GIP receptor and GLP-1 receptor (dual agonist)**Tirzepatide ⓘ The figure shows tirzepatide bound to the human GIP receptor coupled to its Gs protein; tirzepatide also activates the GLP-1 receptor. **Target in 3D:** GIP receptor and GLP-1 receptor (dual agonist). PDB structure 7FIY (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/7FIY) · Drag to rotate · pinch to zoom ## Mechanism of action Tirzepatide is a single peptide built on the GIP sequence with a fatty diacid chain that binds albumin. It activates the GIP receptor and the GLP-1 receptor, both Gs-coupled. Together they increase glucose-dependent insulin release, lower glucagon, slow gastric emptying and reduce food intake, producing larger weight loss than GLP-1 agonism alone in trials. - Activates GIP and GLP-1 receptors (Gs, cAMP) - More insulin when glucose is high, less glucagon - Stomach empties slowly; appetite and intake fall - Large falls in HbA1c and body weight ## Pharmacokinetics **Absorption** Weekly subcutaneous injection. **Distribution** Highly bound to albumin. **Metabolism** Broken down by peptidases and fatty-acid oxidation. **Half-life** Long, which allows once-weekly injection. ## Indications - Type 2 diabetes, with diet and exercise [Type 2 diabetes mellitus →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/) - Chronic weight management in obesity or overweight with weight-related conditions [Obesity →](https://durgical.com/en/conditions/obesity/) - Obstructive sleep apnea in adults with obesity [Obstructive sleep apnoea →](https://durgical.com/en/conditions/obstructive-sleep-apnoea/) ## 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 - Gallbladder disease (gallstones, cholecystitis) - Acute kidney injury from dehydration after vomiting or diarrhea - Thyroid C-cell tumors (seen in rodents; risk in humans unknown) - Pulmonary aspiration during anesthesia or deep sedation, because the stomach empties slowly ## Contraindications - Personal or family history of medullary thyroid carcinoma - Multiple endocrine neoplasia type 2 (MEN 2) - Serious hypersensitivity to the drug ## 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 hormonal contraceptives** Can be less effective, mostly after starting or raising the dose; another or added method is advised. ## What is monitored - HbA1c and weight - Kidney function if vomiting or diarrhea - Symptoms of pancreatitis or gallbladder disease ## 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 dose is raised step by step to limit nausea. - 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. - Ask about oral contraceptives and discuss a backup method. ## 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 Tirzepatide is the 'twincretin': two incretin keys (GIP and GLP-1) on one peptide, so it opens two doors at once. ## Test yourself Think of the answer, then tap the question to see it. ## Which two receptors does tirzepatide activate? The GIP receptor and the GLP-1 receptor. ## Why may a woman on tirzepatide need a backup contraceptive method? Slowed gastric emptying can reduce absorption of oral hormonal contraceptives, especially after starting or raising the dose. ## Besides diabetes and obesity, which condition is tirzepatide used for? Obstructive sleep apnea in adults with obesity. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/tirzepatide/) ## Related drugs - [Semaglutide](https://durgical.com/en/pharmacology/semaglutide/) - [Liraglutide](https://durgical.com/en/pharmacology/liraglutide/) ## Related conditions - [Type 2 diabetes mellitus](https://durgical.com/en/conditions/type-2-diabetes-mellitus/) - [Obesity](https://durgical.com/en/conditions/obesity/) - [Obstructive sleep apnoea](https://durgical.com/en/conditions/obstructive-sleep-apnoea/) [← 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: [Tirzepatide injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a622044.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Cryo-EM structure of the tirzepatide-bound human GIPR-Gs complex](https://www.rcsb.org/structure/7FIY) (RCSB Protein Data Bank, 2022); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BX16) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/) (World Health Organization, 2025). ## **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/tirzepatide/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/tirzepatide/