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ergotamine, combinations excl. psycholeptics

N02CA52

Forms & Strengths

Ergotamine tartrate 1 mg / Caffeine 100 mg oral tablet
Ergotamine tartrate 2 mg / Caffeine 100 mg rectal suppository

Adult Dosing

Oral: 2 tablets at onset of migraine; then 1 tablet every 30 minutes as needed, up to 6 tablets per attack; max 10 tablets per week
Rectal: 1 suppository at onset of migraine; may repeat after 1 hour if needed, up to 2 suppositories per attack; max 5 suppositories per week

Pediatric Dosing

Safety and efficacy not established in pediatric patients

Indications

Acute treatment of vascular headaches, such as migraine or migrainous headaches

Mechanism of Action

Constricts intracranial extracerebral blood vessels via serotonin 5-HT1B/1D receptor agonism
Reduces transmission in trigeminal sensory pathways
Caffeine added to enhance absorption and promote vasoconstriction

Contraindications

Hypersensitivity to ergot alkaloids
Ischemic heart disease, angina, history of myocardial infarction
Peripheral vascular disease and Raynaud's syndrome
Uncontrolled hypertension
Hemiplegic or basilar migraine
Concurrent use of potent CYP3A4 inhibitors (e.g., protease inhibitors, macrolide antibiotics)
Pregnancy and lactation

Adverse Reactions

Nausea and vomiting
Paresthesias and numbness in extremities
Extremity ischemia and weakness
Tachycardia or bradycardia
Dizziness
Rebound headache with overuse

Drug Interactions

Strong CYP3A4 inhibitors (e.g., ritonavir, erythromycin, ketoconazole) increase risk of severe vasospasm and ischemia
Triptans and other 5-HT1 agonists increase risk of prolonged vasoconstriction; allow at least 6-24 hours between use
Vasoconstrictors and sympathomimetics increase risk of additive hypertension
Beta-blockers may enhance peripheral vasoconstriction

Curated Content: Needs Vetting Before Put to Clinical Use