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Expert Opin Drug Metab Toxicol. 2013 Jan;9(1):91-103. doi: 10.1517/17425255.2013.744394. Epub 2012 Dec 10.

Sumatriptan: a review of its pharmacokinetics, pharmacodynamics and efficacy in the acute treatment of migraine.

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  • 1University of Copenhagen, Glostrup Hospital, Danish Headache Center, Department of Neurology, Glostrup, Denmark.



Sumatriptan was developed more than 20 years ago as a 5-HT1B/1D receptor agonist, the first drug in a new class of specific anti-migraine drugs, the triptans. A large amount of information and experience has been gained from the clinical trials undertaken as well the various formulations of sumatriptan used over this period of time.


This evaluation specifically reviews the pharmacokinetics, pharmacodynamics, clinical efficacy, and safety of different formulations and dosages of sumatriptan used for the acute treatment of migraines. Special clinical trials of the timing of dosage and sumatriptan in combination with other triptans as well as non-triptan drugs are also included.


Oral sumatriptan is effective, but not in a convincing majority (60%) of patients in clinical trials. Sumatriptan has failed to show superiority over more standard and cheaper treatment such as aspirin or aspirin plus metoclopramide. In addition, migraine patients want to quickly become pain free, and to remain pain free, but oral sumatriptan at 100 mg managed to keep patients pain free for 24 h is only 20% of cases. Even though sumatriptan has been a major step forward in providing a new specific therapy for the treatment of migraines, there are still are limitations in its use. There is still an unmet need to develop new non-triptan, anti-migraine drugs which act as effective treatment for those who suffer with migraines.

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