Class
- Ergot, migraine preventative
Methysergide
Commonly Prescribed for
(FDA approved in bold)
- Migraine prophylaxis
- Cluster headache prophylaxis
- Diarrhea associated with carcinoid syndrome
Methysergide
How the Drug Works
- 5-HT2 and 5-HT1A/B/C receptor antagonist and partial agonist of 5-HT1B/D. It is unclear which action accounts for drug effectiveness
- Migraine/cluster: Proposed mechanisms include vasoconstrictive actions or inhibition of the release of inflammatory neuropeptides, such as calcitonin gene-related peptide. Prevention of cortical spreading depression may be the mechanism of action for all migraine preventatives
Methysergide
How Long Until It Works
- Migraines – within 2 weeks, but can take up to 2 months on a stable dose to see full effect
Methysergide
If It Works
- In migraine, the goal is a 50% or greater decrease in migraine frequency or severity. Consider tapering or stopping if headaches remit for more than 6 months or if considering pregnancy
Methysergide
If It Doesn’t Work
- Increase to highest tolerated dose
- Migraine/cluster: address other issues such as medication-overuse, other coexisting medical disorders, such as anxiety, and consider changing to another drug or adding a second drug
Methysergide
Best Augmenting Combos for Partial Response or Treatment-Resistance
- Migraine/cluster: Usually used in refractory cases of migraine and cluster headache, usually as an adjunctive agent. May use in combination with AEDs, antidepressants, natural products, and non-pharmacologic treatments, such as biofeedback, to improve headache control
Methysergide
Tests
- Monitor blood pressure. In patients on long-term continuous therapy, consider screening for fibrotic disorders
Adverse Effects (AEs)
Methysergide
How Drug Causes AEs
- Actions on serotonin receptors including vasoconstriction. Fibrotic complications are related to 5-HT2B actions
Methysergide
Notable AEs
- Muscle aching, claudication, nausea, vomiting, weight gain
- Dizziness, giddiness, drowsiness, paresthesias, insomnia
- Hypertension, postural hypertension, tachycardia
- Rarely hallucinations, seizures, blood dyscrasias, such as neutropenia, eosinophilia, or thrombocytopenia
Methysergide
Life-Threatening or Dangerous AEs
- Severe hypertension
- Ergots and related drugs are associated with the development of retroperitoneal, pulmonary, or endocardial fibrosis. Long-term continuous use appears to be the biggest risk factor
Methysergide
Weight Gain
- Not Unusual
Methysergide
Sedation
- Unusual