Pharmacokinetics and safety of a new aspirin formulation for the acute treatment of primary headaches

Expert Opin Drug Metab Toxicol. 2014 Oct;10(10):1381-95. doi: 10.1517/17425255.2014.952631.

Abstract

Introduction: For more than a century, aspirin has been used for the acute treatment of primary headaches. However, the many formulations available are characterized by differences in the pharmacokinetic profile that could affect therapy effectiveness.

Areas covered: The formulations of aspirin affect the speed of absorption of the drug. This feature, in turn, moduates the peak plasmatic concentration (the faster the absorption, the higher the peak plasmatic concentration of aspirin). Recently, a new formulation, consisting in a micronized tablet with an effervescent nucleus, has been shown to be comparable to the formulations associated to the faster absorption. The efficacy of aspirin in migraine is well characterized: the drug is able to rapidly reduce pain and restore functionality, acting also on associated symptoms, in a manner comparable to that of oral sumatriptan. In tension-type headache, aspirin acts in a dose-dependent fashion. The safety profile of the drug is favorable: gastrointestinal complaints are generally mild in intensity and with an incidence comparable to that of ibuprofen and paracetamol.

Expert opinion: According to international guidelines, aspirin should be considered as first-line therapy in primary headaches. Formulations that allow fast absorption, like the new micronized tablets, and portability, are to be preferred.

Keywords: aspirin; headache treatment; micronized aspirin; migraine; pharmacokinetics; safety; speed of action; tension-type headache.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
  • Aspirin / administration & dosage
  • Aspirin / pharmacokinetics
  • Aspirin / therapeutic use*
  • Dose-Response Relationship, Drug
  • Headache / drug therapy*
  • Humans
  • Migraine Disorders / drug therapy
  • Practice Guidelines as Topic
  • Sumatriptan / administration & dosage
  • Sumatriptan / therapeutic use
  • Tablets

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Tablets
  • Sumatriptan
  • Aspirin