Dosing & Uses
Dosage Forms & Strengths
ergotamine/caffeine
oral tablet (Cafergot)
- 1mg/100mg
rectal suppository (Migergot)
- 2mg/100mg
Vascular Headache
Indicated as therapy to abort or prevent vascular headache (eg, migraine, migraine variants, “histaminic cephalalgia”)
Not for chronic daily use
Oral
- 2 tablets (ergotamine 2 mg/caffeine 200 mg) PO at first sign of attack; may take 1 tablet (ergotamine 1 mg/caffeine 100 mg) q30min prn
- Not to exceed 6 tablets/attack
- Not to exceed 10 tablets/week
Rectal
- Insert 1 suppository rectally at first sign of attack; may repeat once after 1 hr
- Not to exceed 2 suppositories/attack
- Not to exceed 5 suppositories/week
Short-term prevention
- In carefully selected patients, with due consideration of maximum dosage recommendations, administration of the drug at bedtime may be an appropriate short-term preventive measure
Dosage Modifications
Renal or hepatic impairment
- Contraindicated
Dosing Considerations
Not effective for other types of headaches; lacks analgesic properties
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
Frequency Not Defined
Gastrointestinal: Nausea and vomiting; rectal or anal ulcer (from overuse of suppositories)
Neurological: Paresthesia, numbness, weakness, and vertigo
Allergic: Localized edema and itching
Cardiovascular
- Serious vasoconstrictive complications may occur including ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, EKG changes, and muscle pains
- Most commonly occurs with long-term therapy at relatively high doses; also reported with short-term or normal doses
- Other cardiovascular adverse effects include transient tachycardia or bradycardia and hypertension
Warnings
Black Box Warnings
Serious and/or life-threatening peripheral ischemia associated with coadministration of ergotamine and caffeine with potent CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics
Because CYP3A4 inhibition elevates ergotamine and caffeine serum levels, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased
Concomitant use of these medications is contraindicated
Contraindications
Potent CYP3A4 inhibitors owing to risk of acute ergot toxicity
Pregnancy
Peripheral vascular disease, coronary heart disease, hypertension, impaired hepatic or renal function, sepsis
Hypersensitivity to any of the ingredients
Cautions
Ergotism
- Although ergotism rarely develop even after long-term intermittent use of orally administered ergotamine, do not exceed dosage recommendations
- Ergotism manifested by intense arterial vasoconstriction, producing signs and symptoms of peripheral vascular ischemia
- Headache, intermittent claudication, muscle pains, numbness, or coldness and pallor of the digits may occur with chronic intoxication; if the condition is allowed to progress untreated, gangrene can result
- While most cases result from frank overdosage, some cases involve hypersensitivity
- There are few reports among patients taking doses within recommended limits or for brief periods
- Withdrawal symptoms (eg, rebound headache) upon discontinuation are rare; typically reported with long, indiscriminate use
Fibrotic complications
- Retroperitoneal and/or pleuropulmonary fibrosis reported
- Rare reports of fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves with long-term, continuous use of ergotamine tartrate and caffeine
- Do not use for chronic daily administration
Drug interaction overview
- Ergotamine is a CYP3A substrate and inhibitor
-
CYP3A inhibitors
- Potent inhibitors: Contraindicated owing to risk for acute ergot toxicity (ergotism) characterized by vasospasm and ischemia of the extremities
- Less potent inhibitors: Although not contraindicated, avoid if possible owing to risk for vasospasm
Pregnancy & Lactation
Pregnancy
Contraindicated; ergotamine elicits oxytocic effects
There are no studies on placental transfer or teratogenicity of the combination of ergotamine and caffeine
Labor and delivery
- Contraindicated in labor and delivery owing to ergotamine’s oxytocic effect, which is maximal in the third trimester
Animal studies
- Caffeine is known to cross the placenta and has been shown to be teratogenic in animals
- Ergotamine crosses the placenta in small amounts, although it does not appear to be embryotoxic in this quantity; however, prolonged vasoconstriction of uterine vessels and/or increased myometrial tone leading to reduced myometrial and placental blood flow may have contributed to fetal growth retardation observed in animals
Lactation
Ergot drugs are known to inhibit prolactin, but there are no reports of decreased lactation with ergotamine/caffeine
Ergotamine is excreted in breast milk and may cause symptoms of vomiting, diarrhea, weak pulse, and unstable blood pressure in nursing infants
Owing to the potential serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, considering the importance of the drug to the mother
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Ergotamine: Alpha-adrenergic blocking agent with direct stimulating effect on smooth muscle of peripheral and cranial blood vessels; also elicits serotonin antagonism
Caffeine: Cranial vasoconstrictor; added to further enhance vasoconstrictive effect without increasing ergotamine dosage
Absorption
Bioavailability: <5%
Peak plasma time: 2 hr (PO)
Distribution
Vd: 1.85 L/kg
Metabolism
Extensively metabolized in liver hepatic metabolism
Elimination
Half-life: 2-2.5 hr
Excretion: Feces (90%, mostly as metabolites)
Administration
Oral Administration
May take with or without food
Rectal Administration
Remove suppository from foil wrap
Lay on side and insert pointed end of suppository into rectum; remain on side to allow suppository to dissolve and absorb
Avoid handling unwrapped suppository for too long
If needed, may cut suppository lengthwise
Storage
Tablets
- Store at 20-25ºC (68-77ºF)
- Dispense in tight, light-resistant container
Suppositories
- Refrigerate at 2-8ºC (36-46ºF) in sealed foil
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