[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Ergot alkaloids](https://durgical.com/en/pharmacology/classes/ergot-alkaloids/) › Ergotamine [Pharmacology](https://durgical.com/en/pharmacology/) · [Ergot alkaloids](https://durgical.com/en/pharmacology/classes/ergot-alkaloids/) # Ergotamine Ergot alkaloid that narrows cranial blood vessels to stop migraine attacks. Dangerous with CYP3A4 inhibitors and forbidden in pregnancy. Updated 2026-11-01 - Class: [Ergot alkaloids](https://durgical.com/en/pharmacology/classes/ergot-alkaloids/) - Receptor: Serotonin 5-HT1B/1D receptors (and alpha-adrenergic receptors) - ATC code: N02CA02 ◎**Serotonin 5-HT1B/1D receptors (and alpha-adrenergic receptors)**Ergotamine ⓘ Crystal structure of the human serotonin 5-HT1B receptor with ergotamine bound. **Target in 3D:** Serotonin 5-HT1B/1D receptors (and alpha-adrenergic receptors). PDB structure 4IAR (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/4IAR) · Drag to rotate · pinch to zoom ## Mechanism of action Ergotamine acts on serotonin receptors (especially 5-HT1B/1D) and alpha-adrenergic receptors. It constricts dilated cranial and peripheral blood vessels and depresses central vasomotor centres, which stops a migraine attack. Caffeine is often combined with it to add vasoconstriction. It also contracts the uterus. - It binds 5-HT1B/1D and alpha-adrenergic receptors - Dilated cranial vessels constrict - The migraine attack is aborted; peripheral vessels also narrow ## Pharmacokinetics **Absorption** By mouth, often with caffeine; also rectal when nausea is severe **Metabolism** Liver, through CYP3A4; it also inhibits CYP3A itself ## Indications - Treatment of migraine attacks and other vascular headaches [Migraine →](https://durgical.com/en/conditions/migraine/) - Cluster headache (vascular headache variant) [Cluster headache →](https://durgical.com/en/conditions/cluster-headache/) ## Adverse effects ### Common - Nausea and vomiting - Numbness, tingling and weakness of limbs - Cold hands and feet - Fast or slow heart rate and raised blood pressure ### Serious (rare, important) - Ergotism: intense vasoconstriction that can progress to gangrene - Severe peripheral ischaemia with strong CYP3A4 inhibitors - Chest pain and myocardial ischaemia - Fibrosis of heart valves, pleura or retroperitoneum with long-term use - Rebound headache and dependence with overuse ## Contraindications - Pregnancy, labour and delivery - Peripheral vascular disease, coronary heart disease and hypertension - Liver or kidney impairment, and sepsis - Use with strong CYP3A4 inhibitors (protease inhibitors, macrolides, ketoconazole, itraconazole) ## Key interactions **Strong CYP3A4 inhibitors (protease inhibitors, clarithromycin, erythromycin, ketoconazole, itraconazole)** Life-threatening peripheral ischaemia; contraindicated **Weaker CYP3A4 inhibitors (fluconazole, fluoxetine, grapefruit juice)** Higher levels; caution **Other vasoconstrictors or sympathomimetics** Additive vasoconstriction **Propranolol** May potentiate vasoconstriction ## What is monitored - Pulses, colour and temperature of the limbs - Blood pressure and chest pain - Frequency of use (risk of rebound headache and fibrosis) ## Administration and safety - Used at the start of an attack; chronic daily use is avoided. - Check the full medicine list for CYP3A4 inhibitors before each new prescription. - Contains tartrazine in some tablets: possible allergic reactions in people sensitive to aspirin. ## Nursing care - Ask about pregnancy, heart disease, hypertension and peripheral vascular disease before use. - Teach the patient to report numbness, tingling, cold or pale fingers and chest pain at once. - Review new antibiotics, antifungals or HIV medicines for interactions. - Teach that overuse causes rebound headache. ## Pregnancy and breastfeeding Contraindicated: its oxytocic and vasoconstrictor effects can harm the fetus. ## Memory aid «Ergotamine + macrolide = Ergotism»: cold, pale, painful limbs. ## Test yourself Think of the answer, then tap the question to see it. ## Which serious reaction occurs when ergotamine is combined with a strong CYP3A4 inhibitor? Life-threatening peripheral ischaemia (ergotism) from intense vasoconstriction. ## Why is ergotamine contraindicated in pregnancy? It contracts the uterus and constricts vessels, which can harm the fetus. ## Which complication appears with long-term ergotamine use? Fibrosis: retroperitoneal, pleuropulmonary or of the heart valves. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/ergotamine/) ## Related drugs - [Methylergometrine](https://durgical.com/en/pharmacology/methylergometrine/) - [Ergometrine](https://durgical.com/en/pharmacology/ergometrine/) ## Related conditions - [Migraine](https://durgical.com/en/conditions/migraine/) - [Cluster headache](https://durgical.com/en/conditions/cluster-headache/) [← Back to the class: Ergot alkaloids](https://durgical.com/en/pharmacology/classes/ergot-alkaloids/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [DailyMed - ERGOTAMINE TARTRATE AND CAFFEINE tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=41f88ae7-c124-5b9c-e054-00144ff88e88) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N02CA) (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/ergotamine/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/ergotamine/