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 alpha(1)-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 arterio-pathy. 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.