Section 02 · Monograph
Ergotamine-caffeine
Reviewed Nov 2026FDA label
CafergotErgot alkaloid
- Forms
- Tab: 1mg/100mg caffeine
- Dose
- 1-2mg PRN (max 6mg/day)
- MOA
- 5-HT1 receptor agonism
Indications
- Treatment to abort or prevent vascular headache, including migraine, migraine variants, and cluster headache episodesFDA-labeled
Mechanism of Action
- Ergotamine is a nonselective 5-HT1 receptor agonist with alpha-adrenergic blocking/direct vasoconstrictive activity on peripheral and cranial smooth muscle; caffeine is added to enhance gastrointestinal absorption and potentiate the vasoconstrictive/analgesic effect
Full Dosing
Adult / usual
- Acute attack (oral): 2 tablets (ergotamine 1 mg/caffeine 100 mg per tablet) at onset, then 1 additional tablet every 30 minutes as needed
- Maximum 6 tablets per attack
- Maximum 10 tablets per week
- Not intended for chronic daily or prophylactic use — restrict to intermittent, episodic dosing
Contraindications
- Concomitant use of potent CYP3A4 inhibitors — protease inhibitors and macrolide antibiotics — due to risk of severe vasospasm/ischemia (ergotism)
- Peripheral vascular disease and coronary artery disease
- Uncontrolled hypertension
- Sepsis
- Hepatic or renal impairment
- Pregnancy (oxytocic effects; teratogenic potential)
- Hypersensitivity to ergotamine, caffeine, or other ergot alkaloids
- Use within 24 hours of a triptan or other ergot-type medication
Drug Interactions
- Potent CYP3A4 inhibitors — contraindicated; markedly increase ergotamine levels and risk of vasospasm, ischemia, and limb amputation
- Beta-blockers may potentiate peripheral vasoconstriction
- Sympathomimetics/other vasoconstrictors — risk of marked, additive hypertension
- Other 5-HT1 agonists or ergot derivatives within 24 hours — additive vasospastic risk
Adverse Effects
- Nausea and vomiting are common
- Vasospasm/ischemia: cold extremities, paresthesias, muscle pain, cyanosis, and (rarely) gangrene
- Retroperitoneal and pleuropulmonary fibrosis with prolonged use
- Ergotamine dependence and psychological dependence with overuse, with rebound (medication-overuse) headache on discontinuation
- Hypertension or hypotension
Monitoring Parameters
- Monitor frequency of use closely — overuse drives dependence, rebound headache, and ergotism
- Assess for signs/symptoms of peripheral ischemia and for chest, abdominal, or extremity pain
- Cardiovascular risk assessment given vasoconstrictive effects
Pregnancy & Lactation
- Contraindicated in pregnancy — oxytocic/uterotonic and vasoconstrictive effects pose risk of fetal harm and teratogenicity
- Ergotamine is excreted in breast milk; breastfeeding not recommended due to risk of vomiting, diarrhea, and hemodynamic instability in the infant