General Information

Dihydroergotamine Impurities and Dihydroergotamine

Daicel Pharma synthesizes high-quality impurities for Dihydroergotamine, an active pharmaceutical ingredient. These impurities, including Dihydroergotamine impurity D and Dihydrolysergamide, help in assessing Dihydroergotamine purity, reliability, and safety. Daicel Pharma also offers a customized synthesis of Dihydroergotamine impurities to cater to client requirements, with worldwide delivery options available.

Dihydroergotamine [CAS: 511-12-6] is a derivative of ergotamine that treats migraine headaches. It is a vasoconstrictor for the management of migraine disorders. It acts as a serotonergic agonist, a non-narcotic analgesic, a vasoconstrictor agent, a dopamine agonist, and a sympatholytic agent.

Dihydroergotamine: Use and Commercial Availability  

Dihydroergotamine (DHE) treats migraine, even during the prevalence of triptans. It interacts with 5-HT1A and 5-HT2 receptors and alpha-1 and -2 receptors, indicating its potential to provide therapeutic benefits through multiple receptor mechanisms. Dihydroergotamine is available in nasal spray and injectable forms (IV, IM, or SC). Clinical trials of orally inhaled DHE have demonstrated its effectiveness in relieving headaches and associated symptoms like nausea, photophobia, and phonophobia. D.H.E. 45, Dihydroergotamine Mesylate, Embolex, Migranal, and Trudhesa are some of the brand names under which the drug is available.

Dihydroergotamine Structure and Mechanism of Action

The chemical name of Dihydroergotamine is (5′α,10α)-9,10-Dihydro-12′-hydroxy-2′-methyl-5′-(phenylmethyl)ergotaman-3′,6′,18-trione. Its chemical formula is C₃₃H₃₇N₅O_5, and its molecular weight is approximately 583.7 g/mol.

Dihydroergotamine binds with 5-HT_1Dα and 5-HT_1Dβ receptors. It acts as a selective agonist for the 5-HT1B/D receptors, leading to cranial vasoconstriction and inhibition of calcitonin gene-related peptide (CGRP) release from trigeminal afferents during migraine episodes. It possesses oxytocic properties.

Dihydroergotamine Impurities and Synthesis

Dihydroergotamine impurities can originate from various sources, including the synthetic process¹, degradation over time, or impure starting materials. They affect the drug quality, efficacy, and safety. The analysis and control of these impurities are crucial to ensure the purity and reliability of the final product. They can impact the drug’s stability, pharmacokinetics, and potential adverse effects. Therefore, comprehensive analysis and control of Dihydroergotamine impurities are necessary to comply with regulatory guidelines and ensure patient safety. It involves thorough characterization, quantification, and implementing measures to minimize impurity formation during manufacturing and storage.

Daicel Pharma offers a comprehensive Certificate of Analysis (CoA) for Dihydroergotamine impurity standards, including Dihydroergotamine impurity D and Dihydrolysergamide. They generate from an analytical facility that complies with cGMP standards. The CoA provides a detailed characterization report with data obtained through techniques such as 1H NMR, 13C NMR, IR, MASS, and HPLC purity analysis². We give additional data like 13C-DEPT upon request. Daicel Pharma synthesizes unknown Dihydroergotamine impurities or degradation products, and labeled compounds, to evaluate the efficacy of generic Dihydroergotamine. Also, Dihydroergotamine D3, a deuterium-labeled Dihydroergotamine standard, is available for bio-analytical research, including BA/BE studies. Every delivery accompanies a complete characterization report.