Version May 2024
Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of ergotamine with potent CYP 3A4 inhibitors, including protease inhibitors and macrolide antibiotics. Because CYP3A4 inhibition elevates the serum levels of ergotamine, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Therefore, concomitant use of these medications is contraindicated.
Migraine, moderate to severe, acute treatment (alternative agent):
Note: Contraindicated in patients with coronary artery disease, hypertension, peripheral vascular disease, or renal or hepatic disease, or patients who are pregnant or of childbearing potential. May be associated with significant side effects and may worsen nausea and vomiting associated with migraine. Other migraine-specific agents are preferred; ergotamine may be considered in patients with migraine attacks >48 hours or those with frequent headache recurrence (EHF/WHO [Steiner 2019]; Tfelt-Hansen 2000; manufacturer's labeling).
Sublingual: 2 mg as a single dose; if symptoms persist, may repeat dose after ≥30 minutes. Maximum: 6 mg per 24 hours; 10 mg/week.
Use is contraindicated in patients with impaired renal function.
Use is contraindicated in patients with impaired hepatic function.
Not recommended for use in older patients.
(For additional information see "Ergotamine: Pediatric drug information")
Vascular headache: Very limited data available; efficacy results variable; not routinely used: Adolescents: Sublingual: 2 mg (1 tablet) under tongue at first sign of migraine, then 2 mg (1 tablet) every 30 minutes as tolerated; maximum dose: 6 mg per 24 hours, or 10 mg/week has been reported in clinical experience (Géraud 2004; Welborn 1997) Note: Not a preferred agent, use of ergotamine has largely been replaced by newer agents with improved efficacy and adverse effect profile.
Use is contraindicated in patients with impaired renal function.
Use is contraindicated in patients with impaired hepatic function.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.
Cardiovascular: Bradycardia, cold extremities, ECG changes, edema, hypertension, ischemia, tachycardia, valvular sclerosis, vasospasm
Central nervous system: Numbness, paresthesia, precordial pain, vertigo
Dermatologic: Gangrene of skin or other tissue, pruritus
Gastrointestinal: Nausea, vomiting
Genitourinary: Retroperitoneal fibrosis
Neuromuscular & skeletal: Myalgia, weakness
Respiratory: Cyanosis, pleuropulmonary fibrosis
Hypersensitivity to ergotamine or any component of the formulation; pregnancy or childbearing potential; peripheral vascular disease; hepatic or renal impairment; coronary artery disease; hypertension; sepsis; ergot alkaloids are contraindicated with strong inhibitors of CYP3A4 (includes protease inhibitors, azole antifungals, and some macrolide antibiotics).
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
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 in any patient at risk or predisposed to vascular effects of ergot alkaloids. In a scientific statement from the American Heart Association, ergotamine has been determined to be an agent that may cause direct myocardial toxicity (magnitude: major) (AHA [Page 2016]).
• 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.
Special populations:
• Older adult: Avoid use in the elderly due to the vasoconstrictive properties and cardiovascular adverse effects associated with ergot alkaloids.
Other warnings/precautions:
• Appropriate use: Acute migraine agents (eg, 5-HT1 agonists, opioids, ergotamine, or a combination of the agents) used for 10 or more days per month may lead to worsening of headaches (medication overuse headache); withdrawal treatment may be necessary in the setting of overuse (Thorlund 2016)
• Withdrawal: Discontinuation even after limited use may result in withdrawal symptoms (ie, rebound headache, nausea, vomiting).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet Sublingual, Sublingual, as tartrate:
Ergomar: 2 mg [contains fd&c blue #1 (brill blue) aluminum lake, quinoline (d&c yellow #10) aluminum lake, saccharin sodium]
No
Sublingual (Ergomar Sublingual)
2 mg (per each): $85.39
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Do not crush sublingual tablets.
Sublingual: Place tablet under the tongue; do not crush; may administer without regard to meals.
Migraine, moderate to severe, acute treatment: Treatment of migraine.
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs that have a heightened risk of causing significant patient harm when used in error.
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha-/Beta-Agonists: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination
Alpha1-Agonists: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may enhance the vasoconstricting effect of Alpha1-Agonists. Risk X: Avoid combination
Aprepitant: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
Beta-Blockers: May enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
Bromocriptine: Ergot Derivatives may enhance the adverse/toxic effect of Bromocriptine. Risk X: Avoid combination
Chloroprocaine (Systemic): May enhance the hypertensive effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Delavirdine: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Dihydroergotamine: Ergot Derivatives may enhance the vasoconstricting effect of Dihydroergotamine. Risk X: Avoid combination
Erythromycin (Systemic): May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fosamprenavir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Lenacapavir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Letermovir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Lisuride: May enhance the adverse/toxic effect of Ergot Derivatives. Risk X: Avoid combination
Lorcaserin (Withdrawn From US Market): May enhance the adverse/toxic effect of Ergot Derivatives. Specifically, use of these drugs together may increase the risk of developing valvular heart disease. Lorcaserin (Withdrawn From US Market) may enhance the serotonergic effect of Ergot Derivatives. This could result in serotonin syndrome. Risk X: Avoid combination
Methysergide: Ergot Derivatives may enhance the vasoconstricting effect of Methysergide. Risk X: Avoid combination
Nefazodone: May enhance the serotonergic effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). This could result in serotonin syndrome. Nefazodone may increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Nitroglycerin: Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates) may diminish the vasodilatory effect of Nitroglycerin. Nitroglycerin may increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Management: Avoid the use of ergot derivatives in patients receiving nitroglycerin for angina (or in any angina patient) if possible. If combined, monitor for decreased effects of nitroglycerin and increased adverse effects of the ergot derivative (eg, ergotism). Risk D: Consider therapy modification
Pergolide: May enhance the adverse/toxic effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
Reboxetine: May enhance the hypertensive effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
Roxithromycin: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Serotonergic Agents (High Risk): Ergot Derivatives may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Tipranavir: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Grapefruit juice may cause increased blood levels of ergotamine, leading to increased toxicity. Management: Monitor for increased effects/toxicity with concomitant use.
Ergotamine crosses the placenta.
Ergotamine 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. Limited human data support the potential for ergotamine to contribute to major congenital malformations and other adverse pregnancy outcomes (Acs 2006; Bánhidy 2007; Medveczky 2004; Raymond 1995; Smets 2004).
The risk of preeclampsia may be increased in patients with migraine (ACOG 2022). Treatment for migraine headaches in pregnant patients should be individualized (AHS [Ailani 2021]). When treatment for acute migraine in pregnancy is needed, other agents are recommended. Use of ergotamine is contraindicated for the treatment of migraine during pregnancy (ACOG 2022; CHS [Worthington 2013]).
Ergotamine is present in breast milk.
Milk production may be reduced by ergot alkaloids. In addition, toxicity may occur in the mother and infant (Anderson 2019). Exposure to ergotamine via breast milk may cause vomiting, diarrhea, weak pulse, and unstable BP in the breastfed infant.
Treatment for migraine headaches in lactating patients should be individualized (AHS [Ailani 2021]). Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends a decision be made to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother. Use of ergot alkaloids is not recommended for the treatment of migraine in lactating patients (ACOG 2022; Anderson 2019; WHO 2002). Infants exposed to ergotamine via breast milk should be monitored for side effects (WHO 2002).
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 (Perrin 1985)
Distribution: Vd: Adults: 1.85 L/kg
Metabolism: Extensively hepatic, including high first-pass metabolism (Perrin 1985)
Bioavailability: Oral, rectal: ≤5% (Perrin 1985)
Half-life elimination: 2-2.5 hours (Perrin 1985)
Time to peak, serum: Oral: 2 hours (Perrin 1985)
Excretion: Feces (90%, primarily as metabolites) (Perrin 1985)
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