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Pronunciation:

(er GOT a meen & KAF een)

U.S. Brand Names:

Cafergot®; Wigraine®

Synonyms:

Caffeine and Ergotamine; Ergotamine Tartrate and Caffeine

Generic Available:

Canadian Brand Names:

Cafergor®

Use:

Abort or prevent vascular headaches, such as migraine, migraine variants, or so-called "histaminic cephalalgia"

Pregnancy Risk Factor:

Pregnancy Implications:

May cause prolonged constriction of the uterine vessels and/or increased myometrial tone leading to reduced placental blood flow. This has contributed to fetal growth retardation in animals.

Lactation:

Enters breast milk/not recommended

Contraindications:

Hypersensitivity to ergotamine, caffeine, or any component of the formulation; peripheral vascular disease; hepatic or renal disease; coronary artery disease; hypertension; sepsis; ergot alkaloids are contraindicated with strong inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics); pregnancy

Warnings/Precautions:

Avoid prolonged administration or excessive dosage because of the danger of ergotism (intense vasoconstriction), gangrene, cardiac valvular fibrosis, retroperitoneal and/or pleuropulmonary fibrosis. Patients who take ergotamine for extended periods of time may experience withdrawal symptoms and rebound headache when ergotamine is discontinued. May be harmful due to reduction in cerebral blood flow; may precipitate angina, myocardial infarction, or aggravate intermittent claudication; therefore, not considered a drug of choice in the elderly.

Concomitant use with medications considered to be "strong" CYP3A4 inhibitors has been associated with acute ergot toxicity; use caution with inhibitors of CYP3A4 enzymes.

Adverse Reactions:

Frequency not defined.

Cardiovascular: Absence of pulse, bradycardia, cardiac valvular fibrosis, cyanosis, edema, ECG changes, gangrene, hypertension, ischemia, precordial distress and pain, tachycardia, vasospasm

Central nervous system: Vertigo

Dermatologic: Itching

Gastrointestinal: Anal or rectal ulcer (with overuse of suppository), nausea, vomiting

Genitourinary: Retroperitoneal fibrosis

Neuromuscular & skeletal: Muscle pain, numbness, paresthesia, weakness

Respiratory: Pleuropulmonary fibrosis

Miscellaneous: Cold extremities

Overdosage/Toxicology:

Symptoms of overdose include vasospastic effects, nausea, vomiting, lassitude, impaired mental function, hypotension, hypertension, unconsciousness, seizures, shock, and death. Treatment includes general supportive therapy. Activated charcoal is effective at binding ergot alkaloids. Vasodilators should be used with caution to avoid exaggerating any pre-existing hypotension.

Drug Interactions:

Ergotamine: Substrate of CYP3A4 (major); Inhibits CYP3A4 (weak)

Caffeine: Substrate of CYP1A2 (major), 2C8/9 (minor), 2D6 (minor), 2E1 (minor), 3A4 (minor); Inhibits CYP1A2 (weak), 3A4 (moderate)

See Ergotamine monograph for related interactions.

CYP1A2 inhibitors: May increase the levels/effects of caffeine. Example inhibitors include amiodarone, fluvoxamine, ketoconazole, and rofecoxib.

CYP3A4 substrates: Caffeine may increase the levels/effects of CYP3A4 substrates. Example substrates include benzodiazepines, calcium channel blockers, cyclosporine, mirtazapine, nateglinide, nefazodone, sildenafil (and other PDE-5 inhibitors), tacrolimus, and venlafaxine. Selected benzodiazepines (midazolam and triazolam), cisapride, ergot alkaloids, selected HMG-CoA reductase inhibitors (lovastatin and simvastatin), and pimozide are generally contraindicated with strong CYP3A4 inhibitors.

Quinolone antibiotics (specifically ciprofloxacin, norfloxacin, ofloxacin): Caffeine levels may be increased by quinolone antibiotics.

Ethanol/Nutrition/Herb Interactions:

Food: Avoid tea, cola, and coffee (caffeine may increase GI absorption of ergotamine). Grapefruit juice may cause increased blood levels of ergotamine, leading to increased toxicity.

Stability:

Suppositories: Store below 25°C (77°F) in sealed foil; protect from moisture.

Tablet: Store at room temperature 15°C to 30°C (59°F to 86°F).

Mechanism of Action:

Has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha-adrenergic receptors depending upon their site; is a highly active uterine stimulant; it causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers

Pharmacodynamics/Kinetics:

Absorption: Ergotamine: Oral, rectal: Erratic; enhanced by caffeine coadministration

Metabolism: Extensively hepatic

Time to peak, serum: Ergotamine: 0.5-3 hours

Half-life elimination: 2 hours

Excretion: Feces (90% as metabolites)

Dosage:

Adults:

Oral: Two tablets at onset of attack; then 1 tablet every 30 minutes as needed; maximum: 6 tablets per attack; do not exceed 10 tablets/week.

Rectal: One suppository rectally at first sign of an attack; follow with second dose after 1 hour, if needed; maximum: 2 per attack; do not exceed 5/week.

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy without consulting prescriber. Take this drug as directed; do not increase dose or use more often than prescribed. If relief is not obtained, contact your prescriber. Avoid products that contain caffeine (eg, tea, coffee, colas, cocoa); caffeine increases GI absorption of ergotamines. May cause drowsiness (avoid activities requiring alertness until effects of medication are known); mild nausea or vomiting (consult prescriber for approved antiemetic); or mild weakness or numbness of extremities (avoid activities that may have a potential for injury). Inspect your extremities for coldness, numbness, or injury. Report immediately any extreme numbness, pain, tingling or weakness in extremities (toes, fingers); severe unresolved nausea or vomiting; or respiratory difficulty or irregular heartbeat. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant 1 month before, during, or for 1 month following therapy. Consult prescriber for instruction on appropriate contraceptive measures. This drug may cause severe fetal defects. Do not donate blood during or for 1 month following therapy (same reason). Breast-feeding is not recommended.

Cardiovascular Considerations:

This drug should be used extremely carefully because of its potent vasoconstrictor action. Administration may elicit marked increases in blood pressure and intracranial hemorrhage. Use should be avoided in patients with cardiovascular disease, including hypertension, coronary artery disease and peripheral vascular disease.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

Drowsiness and dizziness are common

Mental Health: Effects on Psychiatric Treatment:

Use caution with propranolol; vasoconstriction has been reported; coadministration with strong CYP3A4 inhibitors has been associated with serious adverse events (some weaker inhibitors include nefazodone, fluoxetine and fluvoxamine)

Dosage Forms:

Suppository, rectal (Cafergot®): Ergotamine tartrate 2 mg and caffeine 100 mg (12s)

Tablet (Cafergot®, Wigraine®): Ergotamine tartrate 1 mg and caffeine 100 mg

International Brand Names:

Cafergor® (CA)

References

Carlton MC, Kunkel DB, and Curry SC, "Ergotism Treated With Cyproheptadine,"Clin Toxicol, 1995, 33(5):552.

Carlton MC, "Great Balls of Fire: St Anthony and Ergotism,"Clin Toxicol, 1995, 33(5):560.

Edwards WM, "Accidental Poisoning of Newborn Infants With Ergonovine Maleate. A Lesson Application To All Delivery Rooms,"Clin Pediatr (Phila), 1971, 10(5):257-60.

Husum B, Metz P, and Rasmussen JP, "Nitroglycerin Infusion for Ergotism,"Lancet, 1979, 2(8146):794-5.

McGuigan MA, "Ergot Alkaloids,"Clin Toxicol Rev, 1984, 6:1-2.

Orton DA and Richardson RJ, "Ergotamine Absorption and Toxicity,"Postgrad Med J, 1982, 58(675):6-11.

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