Nicergoline Review: Nootropic Benefits, Dosage, & Side Effects

Nicergoline is an ergot derivative and has gained attention due to its potential benefits in managing cognitive dysfunction, especially in conditions like dementia and cerebrovascular disorders. This article delves into the efficacy of nicergoline, its safety, doses, and the use of nicergoline as a therapeutic agent. 

Through examining clinical studies on nicergoline, we explore how nicergoline may support improvement in cognitive abilities in patients with mild to moderate cognitive and behavioural impairment. We will also explore its mechanism of action and the risk of adverse effects associated with nicergoline treatment.

Nicergoline, known for its role in enhancing cerebral and cerebrovascular blood flow, has been successfully used in the treatment of various cognitive impairments. It holds particular promise in the management of age-associated forms of cognitive decline or disease in elderly patients, such as senile dementia.

This article reviews observed data from clinical trials and studies to evaluate the related therapeutic effects of nicergoline administration in these medical conditions. Additionally, we discuss the role of nicergoline therapy in improving symptoms like dizziness and balance disorders linked to cerebral insufficiency.

What is Nicergoline?

Nicergoline, an ergot derivative, is widely recognized for its protective effects that have the potential to manage cognitive and vascular disorders, particularly in the treatment of senile dementia, and ameliorate cognitive deficits in cerebrovascular diseases.

Nicergoline functions primarily as a neuroprotective agent that enhances blood circulation, particularly in cerebral areas, thereby potentially treating mild cognitive impairment and alleviating symptoms experienced by Alzheimer’s disease patients, including mild to moderate dementia.

However, the limited information on the safety of nicergoline is a significant aspect to consider. While it has shown promise in cognitive improvement, understanding its adverse effects is crucial as the drug has not been evaluated and approved by the FDA (Food and Drug Administration).

In clinical settings, nicergoline has been reported to successfully treat conditions like acute and chronic cerebrovascular disorders, peripheral vascular diseases, and balance disorders. Its administration can be oral or through injections, and the dosage is determined based on the severity and type of cognitive or vascular impairment.

Overall, nicergoline stands out as a potent drug used for age-dependent cognitive impairment and has shown promising results in improving cognitive and behavioral disorders in patients with mild to moderate cognitive deficits.

Its role in the progression of cognitive decline, particularly in dementia of vascular origin, has been well-documented, making it a critical agent in the field of cognitive health and dementia treatment.

Pros

• Beneficial effects on cognitive function, particularly in patients with dementia, including Alzheimer’s disease and senile dementia
• Aids in increasing cerebral blood flow, which can be beneficial in cerebrovascular disorders
• Potential neuroprotective properties
• Efficacy in treating dizziness, balance disorders, and peripheral vascular diseases

Cons

• There could be potential drug interactions when used in combination with other medications
• Long-term safety data, especially in studies evaluated using elderly patients, is still limited

Mechanism of Action

Nicergoline exhibits a multifaceted mechanism of action that contributes to its effectiveness in the symptomatic treatment of the decline of cognition, particularly in dementia and other age associated forms of cognitive impairment, and cerebrovascular disorders. 

Its mechanism involves several key actions in the body and brain:

1. Alpha-Receptor Blockade: One of the primary mechanisms of nicergoline is the blockade of alpha-adrenergic receptors. This action leads to vasodilation, particularly in cerebral and arterial vessels, enhancing blood flow to the brain. This improvement in cerebral circulation is crucial to the management of cognitive function disorders.⁽¹⁾
2. Inhibition of Platelet Aggregation: Nicergoline inhibits platelet aggregation, which is a critical factor in preventing thrombotic events. This property is particularly beneficial and allows for the potential of nicergoline in the treatment of older adults and patients with Alzheimer’s disease who are at increased risk of vascular incidents that can lead to cognitive decline.
3. Increase in Serum Substance P: Studies have shown that nicergoline increases serum Substance P, a neuropeptide involved in neurogenic inflammation and pain perception. The increase in Substance P can play a role in neuroprotection and enhancing cognitive functions.⁽²⁾
4. Vascular Response Stimulation: Nicergoline as an agent that provides vascular responses elicited by stimulation of the vascular system is a potential use. This stimulation aids in improving blood circulation throughout the body and particularly to the brain, which is vital for maintaining cognitive function. The blockade by nicergoline of vascular responses elicited
5. Growth Factor Modulation: Nicergoline may influence the activity of various growth factors in the brain. Growth factors are essential for the development, maintenance, and regeneration of neuronal cells. This action can contribute to its neuroprotective effects.
6. Receptor Interaction: Beyond its alpha-blocking activity, nicergoline may interact with other receptor types in the brain, contributing to its overall therapeutic effects in cognitive disorders.
7. Effect on Subtype Receptors in Rats: Research conducted on receptor subtypes in rats has indicated that nicergoline interacts with specific receptor subtypes in the rat to increase glutamate, which might contribute to its therapeutic effects.⁽³⁾
8. Metabolism in Humans: The metabolism of nicergoline in humans has been studied to understand how the drug is processed in the body. CYP2C19, an enzyme belonging to the cytochrome P450 family, plays a critical role in the metabolism of various drugs, including nicergoline.

In conclusion, the mechanism of action of nicergoline is complex and involves multiple pathways. Its ability to improve cerebral blood flow, inhibit platelet aggregation, and potentially modulate growth factors and neurochemicals like Substance P, makes it a valuable therapeutic agent in the management of age-associated cognitive decline and cerebrovascular disorders.

However, the exact molecular mechanisms and the long-term implications of these actions continue to be areas of active research.

Nootropic Benefits of Nicergoline

Nicergoline, a drug noted for its cognitive-enhancing properties, is particularly used in the treatment of various forms of dementia and cognitive impairments.

Here’s an overview of its key nootropic benefits!

1. Improvement in Cognitive Functions

Nicergoline may improve cognitive functions such as memory, attention, and reasoning, especially in individuals with cognitive impairment due to aging or dementia. Nicergoline also is potent as a treatment to prevent cognitive decline.

According to Cochrane Database reviews, nicergoline has been studied for its effectiveness in improving symptoms of cognitive decline, with a focus on its safety and efficacy.⁽⁴⁾

2. Treatment of Behavioral Impairments

The efficacy of nicergoline in dementia treatment has been confirmed after following tests with control groups. It is effective in the treatment of behavioural impairment of various clinical origins, including those associated with dementia, offering a more comprehensive approach to cognitive health.⁽⁵⁾

3. Efficacy in Chronic Cerebrovascular Disorders

Nicergoline is beneficial in including chronic cerebrovascular disorders, improving blood flow to the brain and thereby enhancing cognitive functions.⁽⁶⁾

The blockade by nicergoline of vascular responses elicited by certain stimuli, such as vasoconstrictive agents, is significant in its therapeutic use. This effect makes it beneficial in treating disorders characterized by abnormal or reduced blood flow, such as peripheral vascular diseases and cerebrovascular insufficiency.

By inhibiting these vascular responses, nicergoline helps enhance blood circulation and oxygen supply to various tissues, potentially alleviating symptoms associated with these cognitive conditions.

4. Enhancement of Mood and Behavior

The drug has properties that can positively influence mood and behavior, which is crucial in patients with dementia, where mood swings and behavioral changes are common.⁽⁷⁾

5. Alleviation of Dementia Symptoms

Nicergoline is used to treat different forms of dementia, where it can help in slowing down the progression of cognitive decline. Patients treated with nicergoline experience an alleviation of severe symptoms.⁽¹⁾

6. Mitigation of Propranolol’s Cognitive Effects

In cases where patients are on propranolol, a beta-blocker that can affect cognition, nicergoline can help mitigate some of the cognitive side effects of propranolol.

7. Promotes Cerebrovascular Health

Given its properties, nicergoline is beneficial in conditions involving impaired cerebrovascular health, leading to enhanced cognitive abilities due to better cerebral blood flow.⁽¹⁾

Uses of Nicergoline

Nicergoline, commonly known by its brand name Sermion, is a medicine used for various medical conditions, particularly those related to cognitive and vascular health.

Here are some of its notable uses:

1. Agent for Management of Cognitive Disorders: Nicergoline is a potent nootropic and has been explored as an agent for the management of cognitive disorders, especially in older adults. It is believed to improve symptoms related to cerebral insufficiency and dementia, helping prevent a loss of important neurons.⁽⁸⁾
2. Treatment of Cognitive Impairment: Studies have shown that nicergoline can be effective in the treatment of cognitive impairment. Over a period of months, patients treated with nicergoline showed improvements compared to those who received a placebo.
3. Blockade of Vascular Responses: Nicergoline has the ability to block vascular responses, particularly those elicited by certain stimuli. This property is beneficial in managing conditions like Raynaud’s phenomenon or other circulatory disorders. 
4. Potential Benefits Suggested by Research: Various studies have suggested that nicergoline may offer benefits in treating conditions such as senile dementia, Alzheimer’s disease, and vascular dementia, though more research is needed to confirm these effects.
5. Nicergoline in Vascular Treatments: Nicergoline for the treatment of vascular issues is notable, particularly in improving blood flow and reducing symptoms of claudication. Nicergoline for this form of treatment is still undergoing research to confirm its long-term efficacy.

It’s important to note that although nicergoline shows promise in these areas, the efficacy and safety profile of the properties of nicergoline should be evaluated in the context of individual patient needs and medical history.

Where to Buy Nicergoline

Our top pick on where to buy Niceogoline (sold under the brand name Sermion) is the site called CosmicNootropic.com. 

This reputable retailer has a number of high-quality nootropic products (old and new) that are third-party tested for quality, with worldwide shipping. They have been around for a couple of years too, and over time have created a library of impressive, and usually hard-to-find research chemicals. 

Nicergoline Dosage

Nicergoline dosage can vary depending on the specific condition being treated, the severity of symptoms, and individual patient factors like age, weight, and overall health. It’s crucial to follow a healthcare provider’s prescription for nicergoline, as they will determine the appropriate dosage based on these factors.

Here is a general overview of typical dosages:

• For Cognitive Impairment and Dementia-Related Conditions: The usual dose can range from 5 to 30 mg, taken three times a day. Higher doses may be prescribed for more severe cases.
• Peripheral Vascular Disorders: Dosage typically ranges from 10 to 20 mg, taken three times a day.
• For Other Conditions: The dosage may vary based on the specific condition being treated and the patient’s response to the medication.
• Adjustments for Special Populations: Dosage may be adjusted for elderly patients or those with kidney or liver impairment. Caution is advised when prescribing to these groups, and lower starting doses may be considered to avoid an increased risk of adverse effects.
• Administration: Nicergoline is primarily administered orally in tablet form. Although injections of nicergoline are available, these should not be considered without the supervision of a medical professional. Capsules should be taken consistently, at the same times each day, to maintain an even level of the medication in the blood.

Nicergoline Side Effects and Safety

Nicergoline is generally well-tolerated, but like all medications, it can have side effects. The safety profile of nicergoline is based on its pharmacological action and patient-specific factors.⁽⁹⁾ Here are some common and rare side effects associated with its use:

• Gastrointestinal disturbances such as nausea, vomiting, and diarrhea.
• Headache and dizziness, especially at the start of treatment.
• Low blood pressure (hypotension), which may cause lightheadedness or fainting.
• Flushing and skin rash.

Safety Note: Nicergoline should be used with caution in patients with a history of heart disease, bleeding disorders, or severe hypotension. Additionally, Nicergoline may interact with other medications, so it’s important to inform the healthcare provider about all current medications, including over-the-counter drugs and supplements.

Summary

In conclusion, nicergoline has emerged as a significant agent in the management of cognitive function disorders, particularly in conditions like mild to moderate dementia and cerebrovascular disorders. 

The safety profile of nicergoline has been a critical aspect of its clinical use. While it is generally well-tolerated, the increased risk of adverse effects, particularly in elderly patients and those with certain medical conditions, necessitates careful administration and monitoring.

The understanding of its mechanism of action, especially the blockade by nicergoline of vascular responses and its neuroprotective effects, has been instrumental in its therapeutic application.

Moreover, nicergoline’s role as an ergot derivative with properties that influence cerebral and peripheral vascular systems, along with its potential to inhibit platelet aggregation, adds to its versatility as a medication. However, it is vital to consider the drug interactions, particularly with its metabolism involving enzymes like CYP2C19, to ensure the efficacy and safety of nicergoline.

In summary, nicergoline stands out as a potent and versatile drug used for age-dependent cognitive impairment and associated vascular disorders. Its efficacy and safety, particularly in the treatment of cognitive and dementia-related conditions, make it a valuable option in therapeutic interventions.

However, as with any medication, the administration of nicergoline must be carefully managed to avoid adverse effects and maximize its therapeutic benefits.

As always, remember to consult a healthcare professional before using Nicergoline to boost your cognitive performance.

FAQs

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2. Nishiyama, Yasuhiro et al. “Nicergoline increases serum substance P levels in patients with an ischaemic stroke.” Cerebrovascular diseases (Basel, Switzerland) vol. 29,2 (2010): 194-8. doi:10.1159/000267279 ↩
3. Eom, Sanung et al. “Differential Regulation of Human Serotonin Receptor Type 3A by Chanoclavine and Ergonovine.” Molecules (Basel, Switzerland) vol. 26,5 1211. 24 Feb. 2021, doi:10.3390/molecules26051211 ↩
4. Fioravanti, M, and L Flicker. “Efficacy of nicergoline in dementia and other age associated forms of cognitive impairment.” The Cochrane database of systematic reviews vol. 2001,4 (2001): CD003159. doi:10.1002/14651858.CD003159 ↩
5. Nappi, G et al. “Long-Term Nicergoline Treatment of Mild to Moderate Senile Dementia : Results of a Multicentre, Double-Blind, Placebo-Controlled Study.” Clinical drug investigation vol. 13,6 (1997): 308-16. doi:10.2165/00044011-199713060-00003 ↩
6. Im, Jooyeon J et al. “Changes in Regional Cerebral Perfusion after Nicergoline Treatment in Early Alzheimer’s Disease: A Pilot Study.” Dementia and neurocognitive disorders vol. 16,4 (2017): 104-109. doi:10.12779/dnd.2017.16.4.104 ↩
7. Winblad, Bengt et al. “Therapeutic use of nicergoline.” Clinical drug investigation vol. 28,9 (2008): 533-52. doi:10.2165/00044011-200828090-00001 ↩
8. Mizuno, Tetsuya et al. “Protective effects of nicergoline against neuronal cell death induced by activated microglia and astrocytes.” Brain research vol. 1066,1-2 (2005): 78-85. doi:10.1016/j.brainres.2005.10.050 ↩
9. Fioravanti, Mario et al. “A systematic review and meta-analysis assessing adverse event profile and tolerability of nicergoline.” BMJ open vol. 4,7 e005090. 30 Jul. 2014, doi:10.1136/bmjopen-2014-005090 ↩