What is Nicergoline?
Nicergoline ([(8b)-10-methoxy-1,6-dimethylergolin-8-yl]methyl 5-bromopyridine-3-carboxylate, also known by the trade names Sermion, Nicerbium, and Cholergol) is a chemical derivative of ergot and is similar to hydergine. It has been used as a prescription drug for over four decades to treat cognitive, behavioral, and affective disorders that are the result of vascular dementia, cerebral thrombosis, and atherosclerosis. These primarily occur in older individuals. Some also use nicergoline as a brain supplement, although because it is a prescription drug it is not as easy to obtain as others.
How does it work?
The compound has at least five different actions. Nicergoline is an alpha(1)-adrenoceptor antagonist, which means that it blocks the effects of adrenaline (noradrenaline) that causes vasodilation and increases blood flow. It increases cholinergic and catecholaminergic neurotransmission; it inhibit platelet aggregation; it enhances metabolic activity (oxygen and glucose consumption); it can act as a neurotrophin (nerve growth factor); and it seems to have antioxidant properties.
Regarding blood flow, nicergoline lowers vascular resistance, which increases arterial flow and the delivery of oxygen and glucose to the brain.
In terms of antioxidant properties, although nicergoline does not reduce existing free radicals, it seems to prevent neutrophils (a type of immune cell that causes inflammation) from generating additional free radicals. It does inhibit lipid peroxidation – a pathological process that damages cell membranes.
Nicergoline Benefits
The primary indications of nicergoline are for Alzheimer’s disease, vascular dementia, and cerebrovascular insufficiency. It is also used to treat retinal blood vessel disorders (e.g., diabetic retinopathy and macular degeneration) and peripheral vascular disorders (e.g., peripheral artery disease or Raynaud’s disease). Clinical studies have shown that Alzheimer’s patients treated with nicergoline for eight weeks demonstrated increased vigilance and information processing as assessed by electroencephalogram recordings. Some reports found that up to 89% of patients had improved cognition and behavior.
Beneficial effects are not limited to dementia patients. Healthy people also take it to enhance mental processing speed by increasing oxygen availability and consumption. They report that it improves perception and clarity. There is some evidence that nicergoline is helpful for treating migraines with a vascular origin (due to blood vessel constriction).
Nicergoline Side Effects
Side effects commonly reported for nicergoline include nausea, hypotension, dizziness, and hot flashes. People taking high doses may experience increased appetite, restlessness, diarrhea, excessive perspiration, and bradycardia (rapid heart beat). Most of these adverse effects are related to central nervous system stimulation and are common to other ergot derivatives. They can often be reduced or eliminating by cutting back the number of doses per day or the dosage size. Another way to prevent bothersome side effects is to take brief breaks from a nicergoline regimen, e.g., taking it 5 days a week instead of 7.
Nicergoline Dosage
The bioavailability of nicergoline is fairly poor. It undergoes extensive first pass metabolism and less than 5% actually reaches systemic circulation. Its half-life is 13-20 hours. Most of the published clinical evidence for nicergoline uses a 30 mg dose taken twice daily. This is most commonly prescribed for the treatment of dementia (including Alzheimer’s and vascular types) and balance disorders, and is the maximum recommended dose. Individuals without dementia typically start out taking 5-mg doses one to three times a day. Capsules are usually 5 or 10 mg. It is also available in a drop formulation, 1 mL contains 5 mg. Each dose should be taken between meals to maximize absorption. It may take 4-8 weeks of regular use to notice improvements.
A doctor should be consulted before combining nicergoline with vasodilators, including vinpocetine and picamilon. It should not be taken with propranolol because both depress heart rate. Because it inhibits platelet aggregation, it is not advisable for people with clotting disorders or acute bleeding to take nicergoline.
Bibliography
Fabbrini, G. “Nicergoline in the Treatment of Dementia: Effects on Cerebral Blood Flow Measured by SPECT.” Electroencephalography and Clinical Neurophysiology98.5 (1996): P79. Print.
Fioravanti, M., and L. Flicker. “Efficacy of Nicergoline in Dementia and Other Age Associated Forms of Cognitive Impairment.” Cochrane Database Syst Rev 4.CD003159 (2001). Print.
Iliff, L. D., G. H. D. Boulay, J. Marshall, R. W. R. Russell, and L. Symon. “Effect of Nicergoline on Cerebral Blood Flow.” Journal of Neurology, Neurosurgery & Psychiatry 40.8 (1977): 746-47. Print.
Saletu, B., E. Paulus, L. Linzmayer, P. Anderer, H. V. Semlitsch, J. Grünberger, L. Wicke, A. Neuhold, and I. Podreka. “Nicergoline in Senile Dementia of Alzheimer Type and Multi-infarct Dementia: A Double-blind, Placebo-controlled, Clinical and EEG/ERP Mapping Study.” Psychopharmacology 117.4 (1995): 385-95. Print.
Winblad, Bengt, Mario Fioravanti, Tomas Dolezal, Inara Logina, Ivan Gospodinov Milanov, Dinu Cristian Popescu, and Alina Solomon. “Therapeutic Use of Nicergoline.” Clinical Drug Investigation 28.9 (2008): 533-52. Print.
Zhou, Y.-B., J. Tian, L.-L. Ran, Y. Zuo, G.-Y. Hu, and J.-S. Ding. Chinese Pharmaceutical Journal 43.22 (2008): 1740-743. Print.
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