Dihydroergotamine is a semi-synthetic ergot alkaloid derivative and pharmaceutical active ingredient primarily used for the acute treatment of migraine attacks, with or without aura. It acts on several serotonin, adrenergic and dopaminergic receptors and produces vasoconstrictive effects.
Dihydroergotamine is identified by CAS No. 511-12-6. Its molecular formula is C33H37N5O5 and its molecular weight is approximately 583.68 g/mol.
Dihydroergotamine is a hydrogenated derivative of ergot alkaloids. It is available in pharmaceutical formulations such as nasal sprays and injectable preparations, depending on the approved product and market.
Dihydroergotamine interacts with multiple vascular and neuronal receptors, particularly serotonergic receptors, contributing to its effect on migraine-associated cranial vascular and neuronal pathways.
Its pharmacological activity includes agonist or partial agonist activity at selected serotonin and adrenergic receptors, together with activity at dopaminergic receptors.
Dihydroergotamine produces its antimigraine effect through interaction with serotonin receptors, particularly 5-HT1B and 5-HT1D receptors, as well as other receptor systems.
Activation of these pathways contributes to constriction of certain cranial blood vessels and modulation of trigeminal neurovascular signaling associated with migraine.
Dihydroergotamine is primarily used for:
It is intended for acute treatment rather than routine preventive treatment of migraine.
Dihydroergotamine is relevant to pharmaceutical manufacturers and formulation-development organizations working on antimigraine and neurological pharmaceutical products.
It may be incorporated into approved pharmaceutical dosage forms according to the intended route, formulation and regulatory requirements.
Dihydroergotamine API quality evaluation may include:
Testing should be performed using validated analytical methods appropriate for the API and intended formulation.
Dihydroergotamine intended for pharmaceutical manufacturing should comply with applicable GMP, quality-control and regulatory requirements.
Because ergot alkaloids are pharmacologically potent compounds, appropriate controls for handling, contamination prevention and analytical testing are important.
A batch-specific Certificate of Analysis (CoA) should provide relevant analytical results and acceptance criteria.
Dihydroergotamine API should be stored in tightly closed, appropriately labelled containers under the manufacturer's recommended conditions. Protection from excessive heat, moisture and unsuitable environmental exposure should be maintained.
Dihydroergotamine is relevant to pharmaceutical companies developing and manufacturing acute migraine and antimigraine formulations.
For commercial pharmaceutical applications, customers should verify the API grade, identity, assay, purity, impurity profile, specification, regulatory documentation and batch-specific CoA before use.
Consistent Dihydroergotamine API quality is important for reliable formulation development and pharmaceutical manufacturing. Control of identity, assay, purity and related ergot alkaloid impurities supports reproducible product quality.
Appropriate documentation may include a Certificate of Analysis, specification sheet, safety documentation and applicable regulatory information.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | ≤ 0.5% |
| Water Content | NMT 0.5% |
| Melting Point | 150°C – 154°C |