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Therapeutic Use of Nicergoline

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Abstract

The ergot alkaloid derivative nicergoline became clinically available about 35 years ago in the 1970s. Nicergoline has a broad spectrum of action: (i) as an α1-adrenoceptor antagonist, it induces vasodilation and increases arterial blood flow; (ii) it enhances cholinergic and catecholaminergic neurotransmitter function; (iii) it inhibits platelet aggregation; (iv) it promotes metabolic activity, resulting in increased utilization of oxygen and glucose; and (v) it has neurotrophic and antioxidant properties. Acting on several basic pathophysiological mechanisms, nicergoline has therapeutic potential in a number of disorders. This article provides an overview of the published clinical evidence relating to the efficacy and safety of nicergoline (30 mg twice daily) in the treatment of dementia (including Alzheimer’s disease and vascular dementia) and vascular and balance disorders.

For dementia of different aetiologies, the therapeutic benefit of nicergoline has been established, with up to 89% of patients showing improvements in cognition and behaviour. After as little as 2 months of treatment, symptom improvement is apparent compared with placebo, and most patients are still improved or stable after 12 months. Concomitant neurophysiological changes in the brain indicate (after only 4–8 weeks’ treatment) improved vigilance and information processing. In patients with balance disorders, mean improvements of 44–78% in symptom severity and quality of life have been observed with nicergoline. Although clinical experience with nicergoline in vascular disorders is limited to relatively short-term, small-scale studies, it has been successfully used in rehabilitation therapy of patients with chronic ischaemic stroke. Open-label evaluations suggest that nicergoline may also be valuable in glaucoma, depression and peripheral arteriopathy.

Adverse events of nicergoline, if any, are related to the central nervous system, the metabolic system and the overall body. Most are considered typical symptoms of ergot derivatives. Because of their generally mild and transient nature, treatment discontinuations occur relatively infrequently.

The efficacy of nicergoline combined with a favourable safety and tolerability profile at commonly applied doses (60 mg/day) make this agent a valuable therapy in patients with mild to moderate dementia, vascular diseases and balance disorders.

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Notes

  1. The use of trade names is for product identification purposes only and does not imply endorsement.

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Acknowledgements

Prof. M. Fioravanti has been involved in clinical studies with nicergoline in Parkinson’s disease. The other authors have no conflicts of interest that are directly relevant to the content of this review. The authors are grateful to Ismar Healthcare NV for their assistance in writing the manuscript. The writing was funded by Pfizer Central and Eastern Europe.

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Authors and Affiliations

  1. Karolinska Institute - Alzheimer Disease Research Center, Hälsovägen 7 (Novum 5th Floor), 14186, Stockholm, Sweden

    Bengt Winblad

  2. Department of Psychiatric Science and Psychological Medicine, University of Rome La Sapienza, Rome, Italy

    Mario Fioravanti

  3. Department of Pharmacology, Third Faculty of Medicine, Charles University, Prague, Czech Republic

    Tomas Dolezal

  4. Department of Neurology, Riga Stradin’s University, Riga, Latvia

    Inara Logina

  5. St Naum University Hospital, Sofia, Bulgaria

    Ivan Gospodinov Milanov

  6. Clinical Recovery Hospital, Iasi, Romania

    Dinu Cristian Popescu

  7. Institute of Clinical Medicine, Neurology Unit, Kuopio University, Kuopio, Finland

    Alina Solomon

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Correspondence to Bengt Winblad.

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Winblad, B., Fioravanti, M., Dolezal, T. et al. Therapeutic Use of Nicergoline. Clin. Drug Investig. 28, 533–552 (2008). https://doi.org/10.2165/00044011-200828090-00001

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