Differential medication overuse risk of novel anti-migraine therapeutics

Brain. 2020 Sep 1;143(9):2681-2688. doi: 10.1093/brain/awaa211.

Abstract

Medication overuse headache is estimated to affect 2% of the population, and is ranked in the top 20 most disabling disorders due to its high level of disability. Several therapies used in the treatment of acute migraine are thought to be associated with medication overuse headache, including opioids and triptans. With limited treatment options, it is critical to determine the risk profile of novel therapies prior to their widespread use. The current study explores the potential medication overuse risk of two novel therapeutic drug classes, namely the ditans: 5-HT1F receptor agonists, and the gepants: calcitonin gene-related peptide receptor antagonists, in a preclinical model of medication overuse. Persistent exposure of mice to the 5-HT1F agonist LY344864, but not olcegepant produced a significant reduction in hind paw and orofacial mechanical withdrawal thresholds as a surrogate readout of allodynia. In agreement, only LY344864 induced neuroplastic changes in trigeminal sensory afferents, increasing calcitonin gene-related peptide expression and basal trigeminal nociception. Our data highlight a differential medication overuse headache risk profile for the ditan and gepant classes of drugs that has important implications for their clinical use and patient education to help reduce the burden of medication overuse headache.

Keywords: headache: drug treatment; headache: experimental models; migraine; secondary headache; trigeminal ganglion.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcitonin Gene-Related Peptide Receptor Antagonists / pharmacology
  • Calcitonin Gene-Related Peptide Receptor Antagonists / therapeutic use
  • Carbazoles / pharmacology
  • Carbazoles / therapeutic use
  • Fluorobenzenes / pharmacology
  • Fluorobenzenes / therapeutic use
  • Headache Disorders, Secondary / drug therapy
  • Headache Disorders, Secondary / metabolism*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Migraine Disorders / drug therapy
  • Migraine Disorders / metabolism*
  • Pain Measurement / drug effects*
  • Pain Measurement / methods
  • Piperazines / pharmacology
  • Piperazines / therapeutic use
  • Quinazolines / pharmacology
  • Quinazolines / therapeutic use
  • Receptor, Serotonin, 5-HT1F
  • Receptors, Calcitonin Gene-Related Peptide / metabolism*
  • Receptors, Serotonin / metabolism*
  • Risk Factors

Substances

  • Calcitonin Gene-Related Peptide Receptor Antagonists
  • Carbazoles
  • Fluorobenzenes
  • LY 344864
  • Piperazines
  • Quinazolines
  • Receptors, Calcitonin Gene-Related Peptide
  • Receptors, Serotonin
  • olcegepant