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. 2009 Dec 10;11(1):5–12. doi: 10.1007/s10194-009-0170-y

Does sumatriptan cross the blood–brain barrier in animals and man?

Peer Carsten Tfelt-Hansen 1,✉
PMCID: PMC3452191  PMID: 20012125

Abstract

Sumatriptan, a relatively hydrophilic triptan, based on several animal studies has been regarded to be unable to cross the blood–brain barrier (BBB). In more recent animal studies there are strong indications that sumatriptan to some extent can cross the BBB. The CNS adverse events of sumatriptan in migraine patients and normal volunteers also indicate a more general effect of sumatriptan on CNS indicating that the drug can cross the BBB in man. It has been discussed whether a defect in the BBB during migraine attacks could be responsible for a possible central effect of sumatriptan in migraine. This review suggests that there is no need for a breakdown in the BBB to occur in order to explain a possible central CNS effect of sumatriptan.

Keywords: Blood–brain barrier, Sumatriptan, Migraine, CNS, Animal studies, Human studies

Full Text

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Acknowledgments

The study was supported by the Lundbeck Foundation via the Lundbeck Foundation Center for Neurovascular Signaling (LUCENS).

Conflict of interest

None.

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