Dihydroergotamine

Updated: 2026-09-18

Overview

Dihydroergotamine (DHE) is a semi-synthetic derivative of ergotamine, an alkaloid produced by the fungus Claviceps purpurea. It is classified as an ergopeptide and shares structural similarities with other ergot derivatives. DHE is primarily used in medicine due to its potent vasoconstrictive and serotonin receptor-modulating effects. Developed in the mid-20th century, DHE was designed to retain the therapeutic benefits of ergotamine while reducing adverse effects. It is commonly administered via injection or nasal spray for acute migraine relief and is sometimes used off-label for other vascular conditions. Its mechanism involves constricting dilated cranial blood vessels and inhibiting neurogenic inflammation.

Physical and Chemical Properties

Dihydroergotamine is a white to off-white crystalline powder with a molecular weight of 583.68 g/mol. It decomposes when heated to temperatures above 230°C and exhibits limited solubility in water but dissolves well in organic solvents like ethanol and methanol. The compound is sensitive to light and moisture, requiring controlled storage conditions. Its stability is pH-dependent, with optimal preservation in slightly acidic environments. Analytical techniques such as HPLC and UV spectrometry are typically used for purity assessment due to its complex ergot alkaloid structure.

Main Applications

Dihydroergotamine is predominantly used in the treatment of acute migraines and cluster headaches, where it provides rapid relief by constricting blood vessels and blocking pain pathways. It is often reserved for cases unresponsive to first-line treatments like triptans. In clinical settings, DHE is also employed for managing orthostatic hypotension and certain vascular headaches. Its vasoactive properties make it useful in research related to cerebrovascular and peripheral circulatory disorders. Off-label applications include adjunct therapy for septic shock, though evidence remains limited.

Safety and Storage

Dihydroergotamine must be handled with caution due to its potent pharmacological effects. Direct contact with skin or inhalation of dust should be avoided. It is contraindicated in patients with coronary artery disease, hypertension, or peripheral vascular disorders due to vasoconstriction risks. Proper storage involves sealing the compound in airtight containers under refrigeration (2-8°C) and protecting it from light. Stability studies indicate a shelf life of 2-3 years when stored correctly. Disposal should comply with local regulations for pharmaceutical waste to prevent environmental contamination.

B2B Procurement Guide

When procuring dihydroergotamine, buyers should prioritize suppliers certified for pharmaceutical-grade production (e.g., USP, EP, or GMP compliance). Key documentation includes a Certificate of Analysis (COA) detailing purity (>98%), residual solvents, and heavy metal content. Bulk pricing varies by quantity and purity, with negotiation common for orders exceeding 100 grams. Lead times typically range from 4-8 weeks for custom synthesis. Importers must ensure compliance with regional regulations (e.g., FDA or EMA approvals) and verify cold-chain logistics for transport to maintain stability.