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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)
U.S. Brand Names
Index Terms
Generic Available
No
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.
• Pediatrics: Safety and efficacy have not been established in children.
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); Inhibits CYP3A4 (weak)
Drug Interactions
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
Macrolide Antibiotics: May enhance the adverse/toxic effect of Ergot Derivatives. Specifically leading the development of ergotism. Exceptions: Azithromycin; Dirithromycin [Off Market]; Spiramycin. Risk D: Consider therapy modification
Posaconazole: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
Protease Inhibitors: May decrease the metabolism 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
Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination
Sibutramine: May enhance the serotonergic effect of Ergot Derivatives. This may cause serotonin syndrome. Risk X: Avoid combination
Voriconazole: May increase the serum concentration of Ergot Derivatives. Risk X: Avoid combination
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.
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
Time to peak, serum: 0.5-3 hours
Half-life elimination: 2 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
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. Breast-feeding is not recommended.
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
Assess potential for interactions with other prescriptions, OTC medications, or herbal products patient may be taking. Assess therapeutic effectiveness and adverse response on a regular basis during therapy. Teach patient proper use, possible side effects/appropriate interventions, and adverse symptoms to report. Abrupt discontinuation after long-term use may result in withdrawal symptoms (eg, rebound headache). Pregnancy risk factor X: Determine that patient is not pregnant before beginning treatment. Do not give to women of childbearing unless woman is capable of complying with contraceptive measures 1 month prior to therapy, during therapy, and for 1 month following therapy. Instruct patient on appropriate contraceptive measures. Breast-feeding is not recommended.
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 August 2009
Content last modified August 2009
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