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Ergotamine: Drug information

Ergotamine: Drug information
2024© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Ergotamine: Patient drug information" and "Ergotamine: Pediatric drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Concurrent drug therapy:

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.

Brand Names: US
  • Ergomar
Pharmacologic Category
  • Antimigraine Agent;
  • Ergot Derivative
Dosing: Adult
Migraine, moderate to severe, acute treatment

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 (Ref).

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.

Dosing: Kidney Impairment: Adult

Use is contraindicated in patients with impaired renal function.

Dosing: Hepatic Impairment: Adult

Use is contraindicated in patients with impaired hepatic function.

Dosing: Older Adult

Not recommended for use in older patients.

Dosing: Pediatric

(For additional information see "Ergotamine: Pediatric drug information")

Vascular headache

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 (Ref). Note: Not a preferred agent, use of ergotamine has largely been replaced by newer agents with improved efficacy and adverse effect profile.

Dosing: Kidney Impairment: Pediatric

Use is contraindicated in patients with impaired renal function.

Dosing: Hepatic Impairment: Pediatric

Use is contraindicated in patients with impaired hepatic function.

Adverse Reactions

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

Contraindications

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.

Warnings/Precautions

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).

Dosage Forms: US

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]

Generic Equivalent Available: US

No

Pricing: US

Sublingual (Ergomar Sublingual)

2 mg (per each): $85.39

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Do not crush sublingual tablets.

Administration: Pediatric

Sublingual: Place tablet under the tongue; do not crush; may administer without regard to meals.

Use: Labeled Indications

Migraine, moderate to severe, acute treatment: Treatment of migraine.

Medication Safety Issues
High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drugs (contraindicated in pregnancy) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Community/Ambulatory Care Settings).

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

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 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). Management: Consider avoiding this combination if possible. If required, monitor patients closely for increased adverse effects of the CYP3A4 substrate. Risk D: Consider therapy modification

Itraconazole: May increase the serum concentration of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). 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

Food Interactions

Grapefruit juice may cause increased blood levels of ergotamine, leading to increased toxicity. Management: Monitor for increased effects/toxicity with concomitant use.

Pregnancy Considerations

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]).

Breastfeeding Considerations

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).

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

Pharmacokinetics (Adult Data Unless Noted)

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)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (DE) Germany: Ergo-Kranit Migraene;
  • (FI) Finland: Exmigrex;
  • (GB) United Kingdom: Lingraine;
  • (IE) Ireland: Lingraine;
  • (JP) Japan: Ergotamine tartrate nichiiko;
  • (LT) Lithuania: Ergo-Kranit Migraene;
  • (LV) Latvia: Ergotam;
  • (PH) Philippines: Avamigran;
  • (PR) Puerto Rico: Ergomar;
  • (TH) Thailand: Ergomine | Ergosia | Ergotamine | Erraga;
  • (TW) Taiwan: Ergonagen
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