Abstract

Nicergoline is a semisynthetic ergot derivative and has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions, both in the brain and in the periphery. It is in clinical use for over three decades in over fifty countries for conditions such as cerebral infarction, acute and chronic peripheral circulation disorders, vascular dementia, and Alzheimer's disease and has been found to be beneficial in a variety of other conditions. However, concerns about its safety have been raised, especially after the European medicines agency's (EMEA's) restriction in the use of all ergot derivatives including nicergoline. But, most of the available literature and data suggest that the adverse events with nicergoline are mild and transient. Further, none of the available treatment options for cognitive disorders afford definitive resolution of symptoms. In this backdrop, we discuss the pharmacology of nicergoline with special emphasis on the safety of this compound, especially when used in patients suffering from cognitive function disorders.

Highlights

  • Cognitive function disorders (CFDs) are a group of disorders characterized by disruption in one or more of the cognitive domains

  • The European medicines agency’s (EMEA’s) Committee for Medicinal Products for Human Use (CHMP) in its recommendations suggested that ergot containing medicines, including nicergoline, should no longer be used to treat conditions due to vascular aetiology, in the prevention of migraine headaches or in the symptomatic treatment of venolymphatic insufficiency

  • In this paper we have reviewed the pharmacology of nicergoline with a special emphasis on the various adverse events (AEs) reported when being used as an agent to treat CFDs of various origins

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Summary

Introduction

Cognitive function disorders (CFDs) are a group of disorders characterized by disruption in one or more of the cognitive domains. Diagnostic Statistical Manual of Mental Disorders, 5th edition (DSM-5), addresses CFDs as major neurocognitive disorder, which includes three groups of disorders, namely, delirium, dementia, and amnestic disorders [1] All these three are characterized by an impairment in cognition (as in memory, language, or attention) [2]. It has been predicted that there might be a considerable worldwide increase in the prevalence of dementia from 25 million in the year 2000 to 63 million in 2030 [3] It is a clinical condition characterized by global impairment in cognitive function and is usually progressive impairment of cognitive functions. Memantine is a useful psychotropic drug for AD, especially for moderate-to-severe disease but with little proven benefit in mild disease [7, 8] Each of these drugs has only modest efficacy for AD. The controversy surrounding the usefulness of these antidementia medications is quite profound, especially as these agents slow the progression of cognitive decline but do not reverse the effects of the disease in AD [9]

H MMDL N-demethylation
Pharmacology
Rationale for Using Nicergoline in CFD
Pharmacokinetics of Nicergoline
Uses of Nicergoline
Concerns regarding Safety of Nicergoline
Risk of Fibrosis and Ergotism
Drug Interactions
Findings
Conclusions
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