Nicergoline Has Been Shown to Enhance Mental Clarity, Perception and Concentration

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Nicergoline is an ergot derivative smart drug known as a ergot alkaloid, and is commonly used to treat senile dementia and other disorders with vascular origins.  Nicergoline was developed in the 1970’s, and was originally used for disorders affecting blood supply to the brain and to exert an effect on blood vessels.  It is marketed under the trade name Sermion. 

Over the years, researchers discovered that Nigeroline had additional benefits beyond its vasoactive qualities.

NicergolineMolecule

Nicergoline molecule

Benefits and Mechanism of Action of Nicergoline

Over the years of use and application, Nicergoline has been shown to enhance:

  • Mental agility
  • Mental clarity
  • Perception
  • Concentration
  • Vigilance

Nicergoline has a broad spectrum of action.  It has been found to:  1

  • Activate the brain’s metabolism
  • Increase arterial flow
  • Lower vascular resistance
  • Improve the utilization of glucose and oxygen in the brain  2
  • Act as an alpha(1)-adrenoceptor antagonist, it induces vasodilation and increases arterial blood flow  3
  • Enhances cholinergic and catecholaminergic neurotransmitter function
  • Have antithrombotic activity via inhibition of platelet phospholipase, thus interfering with platelet aggregation  4  5
  • Have neurotrophic and antioxidant properties  6

Clinical Uses of Nicergoline

In a clinical setting, Nicerogline is approved to be used in the following cases:   7

  • Acute and chronic cerebral metabolic-vascular disorders (cerebral arteriosclerosis, thrombosis and cerebral embolism, transitory cerebral ischaemia). Acute and chronic peripheral metabolic-vascular disorders (organic and functional arteriopathies of the limbs), Raynaud’s disease and other syndromes caused by altered peripheral irrigation
  • Migraines of vascular origin
  • Coadjutant therapy in clinical situations accompanied by platelet hyper-aggregability, arterial tension
  • Corio-retinal vascular disorders: diabetic retinopathy, macular degeneration and retinal angiosclerosis
  • Oto-vestibular problems of a vascular nature: dizziness, auditory hallucinations, hypoacusis
  • Improves the apathy and affective disorders caused by cerebral infarction (such as reduced mental alertness, inattention, impairment of recent memory, hypobulia, and depression)
  • Treating acute and chronic peripheral circulation disorders (such as obliterative vascular disease of the limbs, Raynaud’s syndrome, and other peripheral circulation dysfunction symptoms)
  • Treating vascular dementia, especially for the improvement in cognitive dysfunction and memory and to reduce the severity of this disease
  • Acute and chronic cerebral metabolic-vascular disorders, such as the hardening of the walls of the blood vessels in the brain, thrombosis (blood clot in a cerebral blood vessel), obstructions of a blood vessel in the brain and occasional blood supply problems to the brain
  • Diseases of the arteries affecting the limbs, Raynaud’s Disease and other conditions caused by altered peripheral blood flow
  • Problems of a vascular nature, such as dizziness, auditory hallucinations and hearing impairments caused by a deficiency in the conductive hearing organs
  • Corio-retinal vascular disorders – damage to the retina of the eye caused by blood supply problems, macular degeneration and a hardening of the walls of the blood vessels in the retina
  • Decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs
  • Vascular disorders such as cerebral thrombosis and atherosclerosis, arterial blockages in the limbs

The Table below lists a number of study abstracts of Nicergoline’s use in the conditions of stroke and various neurological conditions:

Nicergoline
ConditionAbstract of StudiesReference
Stoke
The present study suggests a possible effect of nicergoline to increase substance P level in ischaemic stroke patients with partial damage to basal ganglia, who have a decreased swallowing response and consequent risk of aspiration pneumonia. Further trials of nicergoline treatment in patients at risk for aspiration pneumonia are warranted.1
25 patients with neurological and neuropsychological deficits after a mild ischaemic stroke were treated with nicergoline (Adavin 60 mg/d) versus placebo in a double blind cross-over trial (3 and 3 months). The patients were examined repeatedly by a neurologist and a neuropsychologist using a battery of tests (PPL, AVLT, Benton and Bourdon tests, number-repetition test). On completion of the trial the improvement of neurological signs (mainly cerebellar deficits) and neuropsychological impairments (in particular of attention and manual manipulation difficulties) was found to be more marked after the period of nicergoline treatment than after placebo. 2
Beta Amyloid toxicity
Nicergoline increased the basal levels of Bcl-2 and reduced the increase in Bax levels induced by beta-amyloid, indicating that the drug inhibits the execution of an apoptotic program in cortical neurons. In mixed cultures of rat cortical cells containing both neurons and astrocytes, nicergoline and MDL were more efficacious than in pure neuronal cultures in reducing beta-amyloid neurotoxicity.3
Acetylcholine levels
Nicergoline treatment did not change ACh levels in young rats, but substantially restored the reduced ACh levels in aged rats. These results indicate that nicergoline is an effective cognitive enhancer in a learning model of age-related deficits and that these results may be related to changes in the cholinergic system.4
Brain-derived neurotrophic factor (BDNF)In microglia stimulated with LPS and IFN-gamma, nicergoline suppressed the production of superoxide anions, interleukin (IL)-1beta, IL-6, and tumor necrosis factor (TNF)-alpha in a dose-dependent manner. In astrocytes, nicergoline also suppressed the production of proinflammatory cytokines and enhanced brain-derived neurotrophic factor (BDNF). Thus, nicergoline-mediated neuroprotection resulted primarily from the inhibition of inflammatory mediators and the upregulation of neurotrophic factors by glial cells.5
Nerve growth factor (NGF)In young Fischer rats, repeated intraperitoneal injections of nicergoline (0.3 and 1.0 mg/kg body weight) did not show any effects on frontal NGF contents determined by a highly sensitive enzyme immunoassay. In aged rats, 22-month-old, however, repeated injections of nicergoline (1.0 mg/kg body weight) induced a significant increase in the NGF level in the frontal region.6

Safety Concerns and Warnings on the Use of Nicergoline

There have been some concerns regarding the safety of Nicergoline. 

The European medicines agency’s (EMEA’s) Committee for Medicinal Products for Human Use (CHMP) in its recommendations in June 2013, suggested that ergot containing medicines, including nicergoline, should no longer be used to treat conditions due to vascular aetiology (such as peripheral artery disease, Raynaud’s syndrome, and retinopathies of vascular origin), in the prevention of migraine headaches or in the symptomatic treatment of venolymphatic insufficiency. This recommendation has been supported by the EMEA as ergot derivatives have a high likelihood of causing serious adverse events (SAEs) such as fibrosis and ergotism.  8

Despite the safety warning by the EMEA, most of the available literature and data suggest that the adverse events with Nicergoline are mild and transient.  9

Nicergoline has been used as a strong inhibitor of platelet aggregation and decreases blood viscosity. There are current admonitions to patients concurrently taking anticoagulants or antiplatelet agents to be closely monitored throughout the duration of therapy with Nicergoline.  10 

If Nicergoline is combined with other potent vasodilators, such as:

  • Bromocriptine
  • Picamilon
  • Vinpocetine
  • Ginko Biloba
  • Xantinol nicotinate

it is advisable to seek one’s physician’s guidance, especially if taking Nicergoline in higher doses. 

Nicergoline (Sermion) is a drug and requires advise and a prescription from a licensed physician for its use. 


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