Dihydroergotamine (DHE) – Is there a place for its use?

Abstract

Nowadays, dihydroergotamine (DHE) is sporadically used as a vasoconstrictor in the treatment of acute migraine. The importance of this drug in medicine has significantly decreased in the recent years. Limitations on the use of dihydroergotamine are due to the high toxicity and increased the risk of severe adverse events after prolonged theraphy. The Committee for Medicinal Products for Human Use of the European Medicines Agency recommends limiting the use of drugs that contain ergotamine derivatives due to the potential risk of ischemic vascular events, fibrosis and ergotism. However, ergot alcaloids preparations are not recommended for use in the prophylaxis of migraine pain, although it is still a good alternative for people with status migrainosus, migraine recurrence or chronic daily headache that do not respond to the classical theraphy. In clinical practice, DHE can be used as a rescue medication to treat migraine attacks involving aura or without aura, as well as for the acute treatment of cluster headache episodes. The effectiveness of DHE in alleviating migraine headache was assessed in multiple clinical studies. This review describes the pharmacodynamic and pharmacokinetic properties of DHE in an expanded view and its role in modern therapy based on available clinical trials. Most clinical data confirm that the drug is still an important element of contemporary migraine therapy, especially in cases when conventional medicine fails.

Potentially Remediable Shortcomings in the Contemporary Drug Treatment of Migraine

“…While no good data regarding ergotamine s elimination half-life and its other pharmacokinetic parameters appear to be generally available, clinical experience of the apparent duration of action of a single oral dose of the drug suggests that, whether in the form of the parent substance or its metabolites, it could be effective for around 12 h or longer after intake. The elimination half-life of dihydroergotamine is around 12 h [47].…”

Could Inhaled Drug Formulations Be the Future of Acute Migraine treatment?

“…Administration of dihydroergotamine via inhalation was demonstrated to be superior to a placebo in relieving migraine symptoms, with or without aura in adults, and sustaining relief in patients who experience nausea or vomiting, photophobia and phonophobia. Pharmacokinetic studies demonstrated that inhaled dihydroerhotamine demonstrated rapid absorption (t max of 10 min), high bioavailability (77%) and long t 1/2 (15 h), thus succeeding low oral bioavailability and absorption, in addition to avoiding patient suffering from being repeatedly injected intravenously [6].…”

Dihydroergotamine affects spatial behavior and neurotransmission in the central nervous system of Wistar rats

“…Current indications for DHE cover mainly acute migraine management. Although some new drugs, such as triptanes, were introduced to therapy, dihydroergotamine still occurs in recommendations [8][9][10]. There are also data supporting the use of DHE in menstrual migraine, migraine with central sensitization and cutaneous allodynia, medication-overuse headache, migraine recurrence, and migrainous state [11].…”