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Cafergot

Novartis AG

Drug Names(s): Ergotamine tartrate and caffeine

Description: Cafergot is an alpha adrenergic blocking agent with a direct stimulating effect on the smoothmuscle of peripheral and cranial blood vessels which produces depression of central vasomotorcenters. The compound also has the properties of serotonin antagonism. Caffeine, also a cranial vasoconstrictor, is added to further enhance the vasoconstrictive effect without the necessity of increasing ergotamine dosage.

Ergotamine acts on migraine by one of two proposed mechanisms: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.


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