Pharmacokinetics of rizatriptan tablets during and between migraine attacks

Headache. 1999 Apr;39(4):264-9. doi: 10.1046/j.1526-4610.1999.3904264.x.

Abstract

Gastric stasis during migraine attacks results in delayed absorption of several orally administered antimigraine agents. This study, as part of a larger trial, was conducted to examine the pharmacokinetics of rizatriptan tablets during and between migraine attacks. Participating patients met IHS criteria for migraine with or without aura, and suffered between one and eight migraines per month for the previous 6 months. In part 1 of the study, 21 patients were randomized to receive a single 5-mg tablet of rizatriptan or placebo in the migraine-free state. In part 2, the same patients were treated during migraine with rizatriptan 5-mg tablets (n=18) or placebo (n=3). Blood samples were obtained before dosing and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours after dosing. The plasma concentration profile (ie, AUC((0-infinity)), C(max), T(max)) of rizatriptan 5-mg tablets administered during and between migraine attacks were comparable. The median T(max) for rizatriptan between and during attacks was 1 hour, indicating rapid absorption even during a migraine attack. Rizatriptan 5 mg was well tolerated and 67% of the patients experienced headache relief 2 hours postdose.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Male
  • Middle Aged
  • Migraine Disorders / drug therapy*
  • Serotonin Receptor Agonists / blood
  • Serotonin Receptor Agonists / pharmacokinetics*
  • Serotonin Receptor Agonists / therapeutic use
  • Time Factors
  • Triazoles / blood
  • Triazoles / pharmacokinetics*
  • Triazoles / therapeutic use
  • Tryptamines / blood
  • Tryptamines / pharmacokinetics*
  • Tryptamines / therapeutic use

Substances

  • Serotonin Receptor Agonists
  • Triazoles
  • Tryptamines
  • rizatriptan