Dihydroergotamine
生产企业：Valeant pharmaceuticals international, Bedford laboratories，另有 1 家
Dihydroergotamine is an ergot alkaloid used in the acute treatment of migraine headache and cluster headache.
Dihydroergotamine is an ergot alkaloid used in the acute treatment of migraine headache and cluster headache.
DHE has several proposed mechanisms which may contribute to its therapeutic efficacy as an abortive therapy in migraines. Firstly, DHE's s agonist action on 5-hydroxytryptamine (5HT) 1b receptors in the smooth muscle of the cranial vasculature may provide relief via vasoconstriction of the blood vessels which typically become dilated due to the release of CGRP during migraine attacks. DHE's off-target action at alpha-adrenergic receptors may further contribute via this mechanism. The remaining mechanisms are thought to provide relief through the effects on the neurogenic causes of migraine symptoms. Agonist action by DHE on 5-HT and 5-HT receptors inhibits nociceptive signalling through the ventroposteromedial thalamus to the trigeminal sensory neurons. Further action on 5-HT and 5-HT receptors with the addition of agonist activity on 5-HT in the trigeminal nucleus caudalis decreases afferent signalling to trigeminal sensory neurons which contributes to central sensitization. The success of experimental compounds selectively targetting the 5-HT receptor lends support to this mechanism. Lastly, action at 5-HT receptors on trigeminal nerve terminals inhibits the release of vasoactive neuropeptides thought to contribute to pain and inflammation during a migraine attack. DHE is known to have 10-fold less potency at the 5-HT receptor than its predecessor ergotamine which reduces the incidence of vascular side effects. Notably, DHE slowly diffuses from receptors resulting in unreliable prediction of effects from plasma concentration.
Dihydroergotamine (DHE) in all formulations is indicated for the acute treatment of migraine with or without aura in adults. As an injection, DHE is also indicated for the acute treatment of cluster headache episodes. DHE is not indicated for migraine prevention or the management of hemiplegic or basilar migraine.
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