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See Latest ArticlesRapid oral transmucosal absorption of sumatriptan, and pharmacodynamics in acute migraine
Headache: The Journal of Head and Face Pain, 06/25/09
Dilone E et al. – The initial pharmacokinetics of lingual spray (LS) approximate to those of subcutaneous injection, despite some fraction of swallowed dose. These pharmacokinetics correspond with earlier effectiveness of LS compared with a 50-mg sumatriptan tablet, and at lower dose, in an enriched, relevant pt population.
Methods- Study of whether sumatriptan is absorbed across oral mucosa
- Description of pharmacokinetics
- Evaluation of potential pharmacodynamic correlates of such pharmacokinetics in pts with migraine attacks
- Clinical trial 1: comparison of pharmacokinetic performance of sumatriptan LS formulation (2 dose sizes, 1 in both fed/fasted state) vs orthodox 50-mg sumatriptan tablet in normal volunteers
- Clinical trial 2: multiple-attack, crossover, fixed dose-order, open-label comparison of sumatriptan LS (up to 3 different dose sizes) vs 100-mg sumatriptan tablet for pt population enriched by documenting suboptimal response to initial 50-mg sumatriptan tablet
- LS formulations resulted in double-peaked time-plasma concentration curves consistent with absorption of sumatriptan across oral mucosa
- First Tmax usually ~10-15 min
- In enriched pt population, first Tmax corresponded with evidence of earlier efficacy for LS vs 50-mg tablet
- Lower dose size for former consistent with oral mucosal drug absorption and evasion of first-pass metabolism
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