Ergotamine

Contraindicated.

Contraindicated.

Ergotamine May be taken with or without food.

Peripheral vascular disease, coronary artery disease, hypertension, sepsis. Renal or hepatic impairment. Pregnancy. Concomitant use with potent CYP3A4 inhibitors (e.g. protease inhibitors, azole antifungals, macrolide antibiotics).

Avoid use within 24 hours of taking selective serotonin (5-HT₁) agonists. Not indicated for chronic daily administration. Elderly. Lactation.

Significant: Cardiac valvular fibrosis (chronic use); CV effects, particularly vasospasm or vasoconstriction, which may lead to hypertension, ECG changes or reduced cerebral blood flow. Rarely, pleural or retroperitoneal fibrosis (prolonged use).
Cardiac disorders: Bradycardia, tachycardia, precordial distress or pain.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Nausea, vomiting, abdominal pain.
General disorders and administration site conditions: Weakness, cold extremities, localised oedema.
Musculoskeletal and connective tissue disorders: Myalgia.
Nervous system disorders: Paraesthesia, numbness.
Skin and subcutaneous tissue disorders: Pruritus, cyanosis.
Potentially Fatal: Ergotism (intense vasoconstriction), resulting in peripheral vascular ischaemia or possible gangrene.

PO/Rectal/SL: X

Monitor for signs of hypertension, cardiac events, or ergotism (e.g. headache, muscle pain, pallor, numbness or coldness of digits).

Symptoms: Nausea, vomiting, drowsiness, numbness, hypertension or hypotension, tingling, pain or cyanosis of the extremities (associated with diminished or absent peripheral pulses), stupor, shock, convulsions and coma. Management: Symptomatic or supportive treatment. Correct hypotension, maintain adequate pulmonary ventilation and control convulsions. For peripheral vasospasms, apply warmth and protect the ischaemic limbs. Administration of vasodilators may be considered, but caution in case of exacerbating existing hypotension.

Increased risk of prolonged vasospastic reactions with selective serotonin agonists (e.g. sumatriptan). Enhanced vasoconstricting effects with other ergot alkaloid derivatives (e.g. dihydroergotamine), β-blockers (e.g. propranolol), nicotine, or other vasoconstrictors. May increase the risk of vasospasm with less potent CYP3A4 inhibitors (e.g. saquinavir, nefazodone, fluconazole, clotrimazole, fluoxetine, zileuton). May result in significant blood pressure elevation with sympathomimetics (e.g. epinephrine).
Potentially Fatal: Increased serum levels resulting in increased risk of ergotism (characterised by vasospasm and cerebral/peripheral ischaemia) with potent CYP3A4 inhibitors, such as protease inhibitors (e.g. ritonavir, indinavir), azole antifungals (e.g. ketoconazole, itraconazole), or macrolides (e.g. erythromycin, clarithromycin).

May increase serum levels and risk of toxicity with grapefruit juice.

Description:
Mechanism of Action: Ergotamine, an ergot alkaloid derivative, has partial agonist and/or antagonist activity on α-adrenergic, serotonergic and dopaminergic receptors depending on the action site. It causes direct vasoconstriction of peripheral and cranial blood vessels and produces depression of the central vasomotor centre.
Pharmacokinetics:
Absorption: Poorly absorbed (sublingual).
Distribution: Crosses the placenta and enters breast milk. Volume of distribution: 1.85 L/kg.
Metabolism: Extensively metabolised in the liver primarily by CYP3A4; undergoes extensive first-pass metabolism.
Excretion: Via faeces (90%, mainly as metabolites); urine (approx 4%). Elimination half-life: 2-2.5 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 8223, Ergotamine. https://pubchem.ncbi.nlm.nih.gov/compound/Ergotamine. Accessed Mar. 29, 2023.

Store between 20-25°C. Protect from heat and light.

Antimigraine Preparations

N02CA02 - ergotamine ; Belongs to the class of ergot alkaloids preparations. Used to relieve migraine.

Brayfield A, Cadart C (eds). Ergotamine Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2025.

Ergomar Sublingual Tablet (Pangea Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/07/2025.

Ergotamine Tartrate. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/07/2025.

Ergotamine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 07/07/2025.

Ergotamine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/07/2025.