methysergide

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

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Feb 16, 2017 | Posted by in PHARMACY | Comments Off on methysergide

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