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Uses and side effects of Nicergoline

May 6，2022

Nicergoline is an ergot derivative that may protect againstdegeneration of cholinergic neurones.Nicergoline has a broad spectrum of action:(1) as a1-adrenoceptor antagonist it induces vasodilata-tion and increases arterial blood flow;(2) it enhances cholin-ergic and catecholaminergic neurotransmission; (3) it inhibitsplatelet aggregation; (4) it promotes metabolic activity, result-ing in increased oxygen and glucose utilization; and (5) it hasneurotrophic and antioxidant properties.

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Uses

Nicergoline has been used for the treatment of various dementias, including AD andVaD. The therapeutic effects ofnicergoline were evident by 2 months of treatment and were maintained for 6-12 months. Cognitive assessment (MMSE)was performed in 261 patients. The difference between treat-ment and control groups on the MMSE favoured nicergoline;at 12 months, the effect size was 2.86.

Interactions

Nicergoline is known to enhance the cardiac depressive effects of propranolol.[6] At high dosages, it is advisable to seek one’s physician's guidance if combining with potent vasodilators such as bromocriptine, Ginkgo biloba, picamilon, vinpocetine or xantinol nicotinate.

Pharmacology

Nicergoline is an ergot alkaloid derivative that acts as a potent and selective α1A-adrenergic receptor antagonist.The IC50 of nicergoline in vitro has been reported to be 0.2 nM.The primary action of nicergoline is to increase arterial blood flow by vasodilation.

Furthermore, it is known that nicergoline inhibits platelet aggregation. Studies have shown that nicergoline also increases nerve growth factor in the aged brain.In addition to the α1A-adrenergic receptor, nicergoline is an antagonist of the serotonin 5-HT1A receptor (IC50 = 6 nM) and shows moderate affinity for serotonin 5-HT2 and α2-adrenergic receptors and low affinity for the dopamine D1 and D2 and muscarinic acetylcholine M1 and M2 receptors.The major metabolites of nicergoline, MMDL and MDL, show low or no affinity for adrenergic, serotonin, dopamine, or acetylcholine receptors.

Side effects

The side effects of nicergoline are usually limited to nausea, hot flushes, mild gastric upset, hypotension and dizziness.At high drug dosages, bradycardia, increased appetite, agitation, diarrhea and perspiration were reported. Most of the available literature suggests that the side effects of nicergoline are mild and transient.

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