TheraRadar
Data updated: May 26, 2026

DIHYDROERGOTAMINE MESYLATE

CNS Approved 2003-04-28

Dihydroergotamine Mesylate Injection is a pharmaceutical agent indicated for the acute treatment of migraine headaches, including cases with or without aura. It is also approved for the acute treatment of cluster headache episodes. The medication is intended for the immediate management of these conditions rather than for preventative use.

Source: FDA Label • AMNEAL

How DIHYDROERGOTAMINE MESYLATE Works

Dihydroergotamine acts as an agonist at the 5-HT1B, 5-HT1D, and 5-HT1F receptors. Its efficacy in treating migraine is attributed to two primary mechanisms: 1) activation of 5-HT1B receptors located on intracranial blood vessels, leading to vasoconstriction, and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system, which inhibits the release of pro-inflammatory neuropeptides (such as calcitonin gene-related peptide, or CGRP). It also interacts with alpha-adrenergic and dopaminergic receptors, which contributes to its complex pharmacological profile and potential side effects.

Source: FDA Label
13
Indications
--
Phase 3 Trials
23
Years on Market

Details

Status
Discontinued
First Approved
2003-04-28
Routes
NASAL, INJECTION
Dosage Forms
SPRAY, METERED, INJECTABLE

DIHYDROERGOTAMINE MESYLATE Approval History

2004
2005
2006
2007
2008
2009
2010
2011
2012
2013
2014
2015
2016
2017
2018
2019
2020
2021
2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
21 FDA actions from 2003 to 2025
Feb 2025 ORIGINAL
Update
Jan 2025 ORIGINAL
Update
Dec 2024 SUPPL
Label · Labeling

What DIHYDROERGOTAMINE MESYLATE Treats

2 indications

DIHYDROERGOTAMINE MESYLATE is approved for 2 conditions since its original approval in 2003. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Migraine
  • Cluster Headache
Source: FDA Label

DIHYDROERGOTAMINE MESYLATE Boxed Warning

PERIPHERAL ISCHEMIA FOLLOWING COADMINISTRATION WITH POTENT CYP3A4 INHIBITORS Serious and/or life-threatening peripheral ischemia has been associated with the co-administration of dihydroergotamine with potent CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because CYP3A4 inhibition elevates the serum levels of dihydroergotamine, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Hence, concomitant use of these medicatio...

DIHYDROERGOTAMINE MESYLATE Competitive Set

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Key Completed Trials

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Trial Timeline

Full development history with FDA approval milestones

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Understanding FDA Approval Types
Count Type What it means
- ORIG Original approval - drug first enters market
- SUPPL - Efficacy New indication (new disease/condition approved)
- SUPPL - Labeling Label text changes (warnings, dosing updates)
- SUPPL - Manufacturing Production changes (new facility)
- SUPPL - Chemistry Formulation changes (new dosage strength)

Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.

DIHYDROERGOTAMINE MESYLATE FDA Label Details

Indications & Usage

DIHYDROERGOTAMINE MESYLATE is indicated for the treatment of Migraine; Cluster Headache.

⚠️ BOXED WARNING

WARNING: PERIPHERAL ISCHEMIA FOLLOWING COADMINISTRATION WITH POTENT CYP3A4 INHIBITORS Serious and/or life-threatening peripheral ischemia has been associated with the co-administration of dihydroergotamine with potent CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because...

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BREKIYA (AUTOINJECTOR)

Full clinical data, patents, trials, and competitive landscape for dihydroergotamine mesylate.

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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.