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Pharmacokinetics of Rizatriptan Tablets During and Between Migraine Attacks

Authors

  • Neal R. Cutler MD,

    Corresponding author
    1. From California Clinical Trials, Beverly Hills (Drs. Cutler and Jhee) and
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  • Stanford S. Jhee PharmD,

    1. From California Clinical Trials, Beverly Hills (Drs. Cutler and Jhee) and
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  • Anup K. Majumdar PhD,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Debra McLaughlin,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Mary Jo Brucker,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Alexandra D. Carides PhD,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Mark S. Kramer MD, PhD,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Deborah Matzura-Wolfe,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Scott A. Reines MD, PhD,

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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  • Michael R. Goldberg MD, PhD

    1. Merck Research Laboratories, Blue Bell, Penn (Dr. Majumdar, Ms. McLaughlin, Ms. Brucker, Dr. Carides, Dr. Kramer, Ms. Matzura-Wolfe, Dr. Reines, and Dr. Goldberg).
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Address all correspondence to Dr. Neal R. Cutler, California Clinical Trials, 7th Floor, 8500 Wilshire Boulevard, Beverly Hills, CA 90211.

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-∞), Cmax, Tmax) of rizatriptan 5-mg tablets administered during and between migraine attacks were comparable. The median Tmax 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.

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