Ergotamin, Ergomar®

Brand name

  • Ergomar®

Drug Class

  • Migraine headaches

Preparations

  • Tablets: 2 mg

Indications

  • Treatment of migraine headache
  • Is a partial agonist and/or antagonist of tryptaminergic, dopaminergic and alpha-adrenergic receptors

Pharmacology

  • Metabolism: Extensively hepatic
  • Half-life: 2 hours
  • Time to peak: 0.5-3 hours

Metabolism

Dosing

  • Migraine:
    • One tablet under tongue at first sign, then 1 tablet every 30 minutes if needed
    • Maximum dose: 3 tablets/24 hours, 5 tablets/week

Drug Interactions

Drugs that may increase the serum concentration of Ergotamine or may enhance the adverse/toxic effect of ergot derivatives

  • Boceprevir
  • Clarithromycin
  • Crizotinib
  • Dasatinib
  • Efavirenz
  • Itraconazole
  • Macrolide Antibiotics
  • Posaconazole
  • Protease Inhibitors
  • Telaprevir
  • Tocilizumab

Adverse Effects

  • Cardiovascular:
    • Absence of pulse
    • bradycardia or tachycardia
    • cardiac valvular fibrosis
    • ECG changes
    • gangrene
    • hypertension
    • ischemia
  • Central nervous system: Vertigo, drowsiness and dizziness
  • Gastrointestinal: Nausea, vomiting, ischemic colitis
  • Genitourinary: Retroperitoneal fibrosis
  • Neuromuscular & skeletal: Muscle pain, numbness, paresthesia, weakness
  • Respiratory: Pleuropulmonary fibrosis
  • Others: Cold extremities

Contraindications

Pregnancy and Breastfeeding

  • 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
  • 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

Precautions

  • Ergotamine is a CYP3A4 inhibitors so it could increase the serum level of medications that are metabolized with this enzyme.
  • Cardivascular effects:
    • Cardiac valvular fibrosis: long term use of ergotamine compounds have been associated with fibrotic valve thickening
    • ECG changes
    • Hypertension;
    • Intermittent claudication, aggravation of angina
    • MI
    • Peripheral vascular ischemia and  gangrene
  • Ischemic colitis because of sustained vasoconstriction
  • Pleural/retroperitoneal fibrosis: Rare cases of pleural and/or retroperitoneal fibrosis have been reported with prolonged daily use

Warning

References:

  • 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
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