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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Pronunciation
(er GOT a meen)
Generic Available (U.S.)
No
Index Terms
Brand Names: U.S.
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Abort or prevent vascular headaches, such as migraine, migraine variants, or so-called “histaminic cephalalgia”
Pregnancy Risk Factor
X
Pregnancy Considerations
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
Breast-Feeding Considerations
Ergotamine is excreted in breast milk and may cause vomiting, diarrhea, weak pulse, and unstable blood pressure in the nursing infant. Consider discontinuing the drug or discontinuing nursing.
Contraindications
Hypersensitivity to ergotamine 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
Boxed warnings:
• CYP3A4 inhibitors: See “Concurrent drug therapy issues” below.
Concerns related to adverse effects:
• Cardiac valvular fibrosis: Ergot alkaloids have been associated with fibrotic valve thickening (eg, aortic, mitral, tricuspid); usually associated with long-term, chronic use.
• Cardiovascular effects: Vasospasm or vasoconstriction can occur, possibly resulting in decreased cerebral blood flow, ECG changes, and hypertension; sustained vasoconstriction may also lead to ischemic colitis, intermittent claudication, aggravation of angina, or precipitation of MI. Do not use is any patient at risk or predisposed to vascular effects of ergot alkaloids.
• Ergotism: Ergot alkaloid use may result in ergotism (intense vasoconstriction) resulting in peripheral vascular ischemia and possible gangrene. Ergotism is usually associated with overdosage or prolonged chronic use; do not exceed dosing guidelines and avoid prolonged administration.
• Pleural/retroperitoneal fibrosis: Rare cases of pleural and/or retroperitoneal fibrosis have been reported with prolonged daily use.
Concurrent drug therapy issues:
• CYP3A4 inhibitors: [U.S. Boxed Warning]: Ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics); concomitant use associated with acute ergot toxicity (ergotism).
Special populations:
• Elderly: Use with extreme caution or avoid use in the elderly; due to vasoconstrictive properties and cardiovascular adverse effects associated with ergot alkaloids.
Other warnings/precautions:
• Withdrawal: Discontinuation after extended use may result in withdrawal symptoms (eg, rebound headache).
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: Nausea, vomiting
Genitourinary: Retroperitoneal fibrosis
Neuromuscular & skeletal: Muscle pain, numbness, paresthesia, weakness
Respiratory: Pleuropulmonary fibrosis
Miscellaneous: Cold extremities
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP3A4 (weak)
Drug Interactions
Alpha-/Beta-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha-/Beta-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Alpha1-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Risk X: Avoid combination
Antipsychotics: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy
Boceprevir: May increase the serum concentration of Ergotamine. Risk X: Avoid combination
Clarithromycin: May increase the serum concentration of Ergotamine. Risk X: Avoid combination
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
Crizotinib: May increase the serum concentration of Ergotamine. Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Efavirenz: May enhance the adverse/toxic effect of Ergot Derivatives. Specifically, the risk for peripheral vasospasm and ischemia may be increased. Risk X: Avoid combination
Itraconazole: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Macrolide Antibiotics: May enhance the adverse/toxic effect of Ergot Derivatives. Specifically leading the development of ergotism. Exceptions: Azithromycin; Azithromycin (Systemic); Fidaxomicin; Spiramycin. Risk D: Consider therapy modification
Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Risk C: Monitor therapy
Nitroglycerin: Ergot Derivatives may diminish the vasodilatory effect of Nitroglycerin. This is of particular concern in patients being treated for angina. Nitroglycerin may increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Posaconazole: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Protease Inhibitors: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Serotonin 5-HT1D Receptor Agonists: Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Risk X: Avoid combination
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification
Telaprevir: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Voriconazole: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Ethanol/Nutrition/Herb Interactions
Food: Caffeine may increase GI absorption of ergotamine. Grapefruit juice may cause increased blood levels of ergotamine, leading to increased toxicity. Management: Avoid caffeinated tea, cola, coffee, or other significant sources of caffeine.
Storage
Store sublingual tablet at room temperature; protect from heat. Protect from light.
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: Oral: Erratic; enhanced by caffeine coadministration
Metabolism: Extensively hepatic
Half-life elimination: 2 hours
Time to peak, serum: 0.5-3 hours
Excretion: Feces (90% as metabolites)
Dosage
Sublingual: One tablet under tongue at first sign, then 1 tablet every 30 minutes if needed; maximum dose: 3 tablets/24 hours, 5 tablets/week
Administration: Oral
Do not crush sublingual tablets.
Patient Education
If relief is not obtained, contact your prescriber. Avoid products that contain caffeine; caffeine increases GI absorption of ergotamine. May cause drowsiness, mild nausea or vomiting, or mild weakness or numbness of extremities. 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.
Geriatric Considerations
Not recommended for use in the elderly. May be harmful due to reduction in cerebral blood flow. May precipitate angina, myocardial infarction, or aggravate intermittent claudication.
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)
Nursing: Physical Assessment/Monitoring
Cardiovascular status should be evaluated prior to initiating medication and periodically thereafter. Abrupt discontinuation after long-term use may result in withdrawal symptoms (eg, rebound headache).
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, sublingual, as tartrate:
Ergomar®: 2 mg [peppermint flavor]
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.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
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