The pharmacology of headache

Prog Neurobiol. 2000 Dec;62(5):509-25. doi: 10.1016/s0301-0082(00)00010-1.


Headache is a common problem which besets most of us at some time or the other. The pharmacology of headache is complex in an overall sense but can be understood in terms of the anatomy and physiology of the pain-producing structures. Migraine can be used as a template to understand the activation of nociceptive systems in the head and thus their neurotransmitter mediation and modulation. In recent years, the role of serotonin (5-HT) in headache pharmacology has been unravelled in the context of both understanding its role in the nociceptive systems related to headache and by exploiting its 5-HT1 receptor subtypes in headache therapeutics. The pharmacology of the head pain systems, as they are known and as they might evolve, are explored in the context of both, the anatomy and physiology of trigeminovascular nociception and in the context of clinical questions, such as those of efficacy, headache recurrence and adverse events.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Brain Chemistry / drug effects
  • Headache / drug therapy*
  • Humans
  • Serotonin Agents / therapeutic use*


  • Serotonin Agents