Ergotamine and nicergoline - facts and myths.

Abstract

Ergotamine, being a representative of naturally occurring ergoline alkaloids, derived from d-lysergic acid, and nicergoline, a d-lumilysergic acid derivative belonging to semi-synthetic ergot-derived alkaloids, display diversified affinity for adrenergic, serotoninergic, and dopamine receptors. Although introduction of triptans marginalized use of ergotamine, nicergoline is used in cerebral metabolic-vascular disorders, and dementia. Additionally, nicergoline exhibits a safety profile comparable to that of placebo, and none of the reviewed studies reported any incidence of fibrosis or ergotism with nicergoline treatment. In line with the recent data, activation of 5-HT2B receptor by ergot derivatives i.e. ergotamine, methysergide, pergolide, and carbegoline is involved in pathogenesis of drug-induced valvulopathy. In contrary structurally related drugs - lisuride and terguride do not increase the risk of valvular heart disease. It seems, that more detailed mechanistic studies on nicergoline and ergotamine might be beneficial for determining structural requirements related to activation of G-protein as well as alternative signal transduction pathways e.g. β-arrestins or different kinases, and responsible for drug liabilities.

• Authors: Paweł Zajdel, Marek Bednarski, Jacek Sapa, Gabriel Nowak
• Journal: Pharmacological reports : PR (Pharmacol Rep) Vol. 67 Issue 2 Pg. 360-3 (Apr 2015) ISSN: 2299-5684 [Electronic] Switzerland
• PMID: 25712664 (Publication Type: Journal Article, Review)
• Copyright: Copyright © 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

Chemical References

• Nicergoline
• Ergotamine

Topics

• Ergotamine (adverse effects, pharmacology, therapeutic use)
• Heart Valve Diseases (chemically induced)
• Humans
• Nicergoline (adverse effects, pharmacology, therapeutic use)