Clinical Pharmacokinetics

, Volume 41, Issue 11, pp 801–811

Clinical Pharmacokinetics of Intranasal Sumatriptan

  • Eliane Fuseau
  • Olivier Petricoul
  • Katy H. P. Moore
  • Andrew Barrow
  • Tim Ibbotson
Review Articles Drug Disposition

DOI: 10.2165/00003088-200241110-00002

Cite this article as:
Fuseau, E., Petricoul, O., Moore, K.H.P. et al. Clin Pharmacokinet (2002) 41: 801. doi:10.2165/00003088-200241110-00002
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Abstract

A substantial proportion of migraine patients have gastric stasis and suffer severe nausea and/or vomiting during their migraine attack. This may lead to erratic absorption from the gastrointestinal tract and make oral treatment unsatisfactory. For such patients, an intranasal formulation may be advantageous. Sumatriptan is a potent serotonin 5HT1B/1D agonist widely used in the treatment of migraine; the effectiveness of the intranasal formulation (20mg) has been well established in several clinical studies. This article reviews the pharmacokinetics of intranasal sumatriptan and includes comparisons with oral and subcutaneous administration.

After intranasal administration, sumatriptan is directly and rapidly absorbed, with 60% of the maximum plasma concentration (Cmax) occurring at 30 minutes after administration of a single 20mg dose. Following intranasal administration, approximately 10% more sumatriptan is absorbed probably via the nasal mucosa when compared with oral administration. Mean Cmax after a 20mg intranasal dose is approximately 13.1 to 14.4 ng/mL, with median time to Cmax approximately 1 to 1.75 hours. When given as a single dose, intranasal sumatriptan displays dose proportionality in its extent of absorption and Cmax over the dose range 5 to 10mg, but not between 5 and 20mg for Cmax. The elimination phase half-life is approximately 2 hours, consistent with administration by other routes.

Sumatriptan is metabolised by monoamine oxidase (MAO; predominantly the A isozyme, MAO-A) to an inactive metabolite. Coadministration with a MAO-A inhibitor, moclobemide, leads to a significant increase in sumatriptan plasma concentrations and is contraindicated.

Single-dose pharmacokinetics in paediatric and adolescent patients following intranasal sumatriptan were studied to determine the effect of changes in nasal morphology during growth, and of body size, on pharmacokinetic parameters. The pharmacokinetic profile observed in adults was maintained in the adolescent population; generally, factors such as age, bodyweight or height did not significantly affect the pharmacokinetics. In children below 12 years, Cmax is comparable to that seen in adolescents and adults, but total exposure (area under the concentration-time curve from zero to infinity) was lower in children compared with older patients, especially in younger children treated with 5mg.

Clinical experience suggests that intranasal sumatriptan has some advantages over the tablet (more rapid onset of effect and use in patients with gastrointestinal complaints) or subcutaneous (noninvasive and fewer adverse events) formulations.

Copyright information

© Adis International Limited 2002

Authors and Affiliations

  • Eliane Fuseau
    • 1
  • Olivier Petricoul
    • 1
  • Katy H. P. Moore
    • 1
  • Andrew Barrow
    • 3
  • Tim Ibbotson
    • 4
  1. 1.EMF Consulting FranceAix en ProvenceFrance
  2. 2.GlaxoSmithKline Inc.Clinical Pharmacology, Research Triangle ParkResearch Triangle ParkUSA
  3. 3.GlaxoSmithKline R&DWare, HertfordshireUK
  4. 4.GlaxoSmithKline R&DGreenford, MiddlesexUK

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