methylergonovine

Class




  • Ergot, migraine preventive




Methylergonovine


Commonly Prescribed for


(FDA approved in bold)



  • Uterine contractions/bleeding after delivery
  • Migraine prophylaxis
  • Cluster headache



Methylergonovine


How the Drug Works



  • 5-HT2A/B/C receptor antagonist and 5-HT1B/D agonist
  • Used to prevent or control excessive bleeding following childbirth and spontaneous or elective abortion. Causes uterine contractions to aid in expulsion of retained products of conception after miscarriage and to help deliver the placenta after childbirth
  • 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. An active metabolite of methysergide



Methylergonovine


How Long Until It Works



  • Obstetrical: hours, or minutes as an injection
  • Migraines – within 2 weeks, but can take up to 2 months on a stable dose to see full effect



Methylergonovine


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



Methylergonovine


If It Doesn’t Work



  • Increase to highest tolerated dose
  • Migraine: 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



Methylergonovine


Best Augmenting Combos for Partial Response or Treatment-Resistance



  • Migraine: 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



Methylergonovine


Tests



  • Monitor blood pressure. In patients on long-term continuous therapy, consider screening for fibrotic disorders



Adverse Effects (AEs)




Methylergonovine


How Drug Causes AEs



  • Actions on serotonin receptors, including vasoconstriction. Fibrotic complications are related to 5H-T2B actions



Methylergonovine


Notable AEs



  • Muscle aching, claudication, nausea, vomiting, weight gain
  • Dizziness, giddiness, drowsiness, paresthesias
  • Hypertension
  • Rarely hallucinations



Methylergonovine


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



Methylergonovine


Weight Gain



  • Not unusual



Methylergonovine


Sedation



  • Unusual

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

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