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NERVOUS SYSTEM › ANALGESICS › ANTIMIGRAINE PREPARATIONS › Ergot alkaloids
ergotamine
N02CA02
Forms & Strengths
- Sublingual tablet: 2 mg ergotamine tartrate with 100 mg caffeine
Adult Dosing
- Acute migraine: 1 tablet sublingually at onset
- May repeat every 30 minutes if needed
- Maximum dose: 3 tablets per attack
- Maximum weekly dose: 10 tablets
Pediatric Dosing
- Safety and efficacy not established in pediatric patients
Indications
- Abortive treatment of vascular headaches, such as migraine or migraine variants
Mechanism of Action
- Constricts peripheral and cranial blood vessels
- Partial agonist and antagonist activity at 5-HT1D/1B receptors and alpha-adrenergic receptors
Contraindications
- Hypersensitivity to ergot alkaloids
- Ischemic heart disease, angina pectoris, myocardial infarction
- Peripheral vascular disease, Raynaud's syndrome
- Uncontrolled hypertension
- Hemiplegic or basilar migraine
- Sepsis
- Severe hepatic or renal impairment
- Concurrent use of potent CYP3A4 inhibitors (e.g., protease inhibitors, macrolide antibiotics)
- Pregnancy and lactation
Adverse Reactions
- Nausea and vomiting
- Paresthesias, numbness, and tingling in extremities
- Peripheral ischemia, cold extremities, diminished pulses
- Transient tachycardia or bradycardia
- Precordial distress, chest pain
- Ergotism with chronic use (vasospasm, gangrene)
Drug Interactions
- Potent CYP3A4 inhibitors (e.g., ritonavir, ketoconazole, erythromycin) cause severe vasospasm and ischemia
- Triptans or other 5-HT agonists increase risk of prolonged vasoconstriction; separate by at least 24 hours
- Beta-blockers can cause peripheral vasoconstriction
- Nicotine promotes vasoconstriction and increases risk of ergotism
- Vasoconstrictors (sympathomimetics) lead to additive hypertensive effects
Curated Content: Needs Vetting Before Put to Clinical Use