Yes

Ergot Derivative

Abort or prevent vascular headaches, such as migraine or cluster

X

Hypersensitivity to ergotamine, caffeine, or any component; peripheral vascular disease, hepatic or renal disease, hypertension, peptic ulcer disease, sepsis; avoid during pregnancy; concurrent use with ritonavir, nelfinavir, and amprenavir

Avoid prolonged administration or excessive dosage because of the danger of ergotism and gangrene; patients who take ergotamine for extended periods of time may become dependent on it. 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.

>10%:

Cardiovascular: Tachycardia, bradycardia, arterial spasm, claudication and vasoconstriction; rebound headache may occur with sudden withdrawal of the drug in patients on prolonged therapy; localized edema, peripheral vascular effects (numbness and tingling of fingers and toes)

Central nervous system: Drowsiness, dizziness

Gastrointestinal: Nausea, vomiting, diarrhea, xerostomia

1% to 10%:

Cardiovascular: Transient tachycardia or bradycardia, precordial distress and pain

Neuromuscular & skeletal: Weakness in the legs, abdominal or muscle pain, muscle pains in the extremities, paresthesia

Symptoms include vasospastic effects, nausea, vomiting, lassitude, impaired mental function, hypotension, hypertension, unconsciousness, seizures, shock, and death

Treatment includes general supportive therapy, gastric lavage, or induction of emesis, activated charcoal, saline cathartic; keep extremities warm. Activated charcoal is effective at binding certain chemicals, and this is especially true for ergot alkaloids; treatment is symptomatic with heparin, vasodilators (nitroprusside); vasodilators should be used with caution to avoid exaggerating any pre-existing hypotension.

Increased toxicity:

Erythromycin, troleandomycin and other macrolide antibiotics: Monitor for signs of ergot toxicity

Ritonavir, amprenavir and nelfinavir increase blood levels of ergot alkaloids. Avoid concurrent use.

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

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

Metabolism: Extensively in the liver

Bioavailability: Poor overall (<5%)

Time to peak serum concentration: Within 0.5-3 hours following coadministration with caffeine

Elimination: In bile as metabolites (90%)

Oral:

Cafergot®: 2 tablets at onset of attack; then 1 tablet every 30 minutes as needed; maximum: 6 tablets per attack; do not exceed 10 tablets/week.

Ergostat®: 1 tablet under tongue at first sign, then 1 tablet every 30 minutes, 3 tablets/24 hours, 5 tablets/week

Rectal (Cafergot® suppositories, Wigraine® suppositories, Cafatine® suppositories): 1 at first sign of an attack; follow with second dose after 1 hour, if needed; maximum: 2 per attack; do not exceed 5/week.

Nasal inhalation (Migranal®):One spray (0.5 mg) in each nostril, repeat with an additional spray in each nostril after 15 minute (total dose: 4 sprays or 2.0 mg)

Avoid tea, cola, and coffee, caffeine may increase GI absorption of ergotamine

Drowsiness and dizziness are common

Use caution with propranolol; vasoconstriction has been reported

No information available to require special precautions

>10% of patients experience dry mouth

Take this drug as directed; do not increase dose or use more often than prescribed. If relief is not obtained, contact your prescriber. Avoid caffeine-containing products (eg, tea, coffee, colas, cocoa); caffeine increases GI absorption of ergotamines. May cause drowsiness (avoid activities requiring alertness until effects of medication are known). You may experience mild nausea/vomiting (you may have an antiemetic prescribed), mild weakness or numbness of extremities (avoid injury). Inspect your extremities for coldness, numbness, or injury. Report immediately extreme numbness, pain, tingling or weakness in extremities (toes, fingers), severe unresolved nausea or vomiting, difficulty breathing 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). Do not breast-feed.

Do not crush sublingual drug product

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

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

Tablet, sublingual (Ergomar®): Ergotamine tartrate 2 mg

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.