Methylxanthines and pain

Research output: Chapter in Book/Report/Conference proceedingChapter

59 Citations (Scopus)

Abstract

Caffeine, an antagonist of adenosine A1, A2A and A2B receptors, is known as an adjuvant analgesic in combination with non-steroidal anti-inflammatory drugs (NSAIDs) and acetaminophen in humans. In preclinical studies, caffeine produces intrinsic antinociceptive effects in several rodent models, and augments the actions of NSAIDs and acetaminophen. Antagonism of adenosine A2A and A2B receptors, as well as inhibition of cyclooxygenase activity at some sites, may explain intrinsic antinociceptive and adjuvant actions. When combined with morphine, caffeine can augment, inhibit or have no effect depending on the dose, route of administration, nociceptive test and species; inhibition reflects spinal inhibition of adenosine A1 receptors, while augmentation may reflect the intrinsic effects noted above. Low doses of caffeine given systemically inhibit antinociception by several analgesics (acetaminophen, amitriptyline, oxcarbazepine, cizolirtine), probably reflecting block of a component of action involving adenosine A1 receptors. Clinical studies have demonstrated adjuvant analgesia, as well as some intrinsic analgesia, in the treatment of headache conditions, but not in the treatment of postoperative pain. Caffeine clearly exhibits complex effects on pain transmission; knowledge of such effects is important for understanding adjuvant analgesia as well as considering situations in which dietary caffeine intake may have an impact on analgesic regimens.

Original languageEnglish
Title of host publicationMethylxanthines
EditorsBertil Fredholm
Pages311-329
Number of pages19
DOIs
Publication statusPublished - 2011

Publication series

NameHandbook of Experimental Pharmacology
Volume200
ISSN (Print)0171-2004

ASJC Scopus Subject Areas

  • Biochemistry
  • Pharmacology, Toxicology and Pharmaceutics(all)

PubMed: MeSH publication types

  • Journal Article
  • Review

Fingerprint

Dive into the research topics of 'Methylxanthines and pain'. Together they form a unique fingerprint.

Cite this