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ergotamine

Brand: Ergomar, Cafergot (with caffeine)

⚠ BBW Beers Criteria Prototype Drug
Drug Class: ergot alkaloid / vasoconstrictor
Drug Family: antimigraine
Subclass: ergot alkaloid migraine agent
Organ Systems: cnscardiovascular

Mechanism of Action

Partial agonist/antagonist at serotonin, adrenergic, and dopaminergic receptors; produces cranial vasoconstriction via serotonergic and adrenergic mechanisms. Less receptor selective than triptans; the broader receptor activity explains more adverse effects and potential for ergotism.

5-HT1B receptor5-HT1D receptoralpha-adrenergic receptordopamine receptor

Indications

  • acute migraine (historical; now largely replaced by triptans due to superior tolerability)
  • cluster headache (second-line)

Contraindications

  • coronary artery disease
  • peripheral vascular disease
  • severe hypertension
  • renal/hepatic impairment
  • pregnancy (strong oxytocic — causes uterine contraction)
  • concurrent CYP3A4 inhibitors
  • concurrent triptans within 24 hours

Adverse Effects

Common

  • nausea
  • vomiting
  • peripheral paresthesias
  • weakness
  • vasoconstriction
  • muscle cramps

Serious

  • ergotism (gangrene of extremities from severe, prolonged vasoconstriction)
  • ergotamine overuse headache/rebound
  • cardiac ischemia
  • peripheral ischemia

Pharmacokinetics (ADME)

Absorption oral bioavailability ~1-3% (very poor); sublingual: ~2%; inhalation: better
Distribution protein binding ~98%; Vd very large
Metabolism primarily CYP3A4; active metabolites with prolonged vasoconstrictive activity
Excretion fecal (90%)
Half-life 2 hours (but ergotism can persist for days due to prolonged tissue binding)
Onset sublingual: 20-30 minutes
Peak 1-2 hours
Duration hours to days with prolonged binding
Protein Binding 98%
Vd very large

Drug Interactions

Drug / Agent Mechanism Severity
strong CYP3A4 inhibitors (macrolides, protease inhibitors, azole antifungals) markedly increase ergotamine levels; severe peripheral ischemia and gangrene (BBW) contraindicated
triptans additive vasospasm; 24-hour separation required contraindicated
beta-blockers potentiate peripheral vasoconstriction major

Nursing Considerations

  1. Ergotamine is contraindicated in pregnancy as a strong uterotonic; verify pregnancy status before dispensing.
  2. CYP3A4 inhibitor BBW is critical: clarithromycin, erythromycin, ritonavir, and azole antifungals are absolutely contraindicated — verify complete medication list.
  3. Assess extremities for signs of ischemia (cold, pale, pulseless): ergotism is a medical emergency requiring immediate discontinuation and vasodilator therapy.
  4. Ergotamine overuse headache develops with use >10 days/month; assess frequency of use at every visit.

Clinical Pearls

  • Ergotamine was the primary migraine treatment for decades before triptans; it is now considered second-line due to its narrow therapeutic index and the superior tolerability of triptans.
  • The interaction with CYP3A4 inhibitors is one of the most clinically dangerous in all of pharmacology: macrolide antibiotics (a common drug class) can cause life-threatening ergotism in ergotamine-treated patients within days of concurrent use.

Safety Profile

Pregnancy contraindicated
Lactation contraindicated
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.

Acute Migraine (historical; Now Largely Replaced By Triptans Due To Superior Tolerability) Cluster Headache (second-line) Ergot Alkaloid / Vasoconstrictor
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