Nicergoline
Encyclopedia
Nicergoline is an ergot
derivative used to treat senile dementia
and other disorders with vascular
origins. It has been found to increase mental agility and enhance clarity and perception. It 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.
It is used for vascular disorders such as cerebral thrombosis
and atherosclerosis
, arterial blockages in the limbs, Raynaud's disease, vascular migraine
s, and retinopathy
.
Nicergoline has been registered in over fifty countries and has been used for more than three decades for the treatment of cognitive, affective, and behavioral disorders of older people.
Dosages for known conditions are usually administered at 5–10 mg three times a day, however anti-aging preventative purposes may want to consider 5 mg once or twice a day more adequate.
(heart conditions), hypertension, bradycardia
or using alpha or beta receptor agonists should consult with their physician before use.
Although toxicology studies have not shown nicergoline to have any teratogenic effect, the use of this medicine during pregnancy should be limited to those cases where it is absolutely necessary.
Nicergoline is considered unsafe in porphyria
.
, increased appetite, agitation, diarrhea and perspiration have been known to occur. A single case of acute interstitial nephritis
has been reported.
, Gingko biloba, picamilon
, vinpocetine
or xantinol nicotinate
.
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.
Ergot
Ergot or ergot fungi refers to a group of fungi of the genus Claviceps. The most prominent member of this group is Claviceps purpurea. This fungus grows on rye and related plants, and produces alkaloids that can cause ergotism in humans and other mammals who consume grains contaminated with its...
derivative used to treat senile dementia
Dementia
Dementia is a serious loss of cognitive ability in a previously unimpaired person, beyond what might be expected from normal aging...
and other disorders with vascular
Blood vessel
The blood vessels are the part of the circulatory system that transports blood throughout the body. There are three major types of blood vessels: the arteries, which carry the blood away from the heart; the capillaries, which enable the actual exchange of water and chemicals between the blood and...
origins. It has been found to increase mental agility and enhance clarity and perception. It decreases vascular resistance
Vascular resistance
Vascular resistance is a term used to define the resistance to flow that must be overcome to push blood through the circulatory system. The resistance offered by the peripheral circulation is known as the systemic vascular resistance , while the resistance offered by the vasculature of the lungs...
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.
It is used for vascular disorders such as cerebral thrombosis
Thrombus
A thrombus , or blood clot, is the final product of the blood coagulation step in hemostasis. It is achieved via the aggregation of platelets that form a platelet plug, and the activation of the humoral coagulation system...
and atherosclerosis
Atherosclerosis
Atherosclerosis is a condition in which an artery wall thickens as a result of the accumulation of fatty materials such as cholesterol...
, arterial blockages in the limbs, Raynaud's disease, vascular migraine
Migraine
Migraine is a chronic neurological disorder characterized by moderate to severe headaches, and nausea...
s, and retinopathy
Retinopathy
Retinopathy is a general term that refers to some form of non-inflammatory damage to the retina of the eye. Frequently, retinopathy is an ocular manifestation of systemic disease.-Pathophysiology:Causes of retinopathy are varied:...
.
Nicergoline has been registered in over fifty countries and has been used for more than three decades for the treatment of cognitive, affective, and behavioral disorders of older people.
Clinical uses
Nicerogline is used in the following cases:- Acute and chronic cerebral metabolic-vascular disorders (cerebral arteriosclerosis, thrombosisThrombosisThrombosis is the formation of a blood clot inside a blood vessel, obstructing the flow of blood through the circulatory system. When a blood vessel is injured, the body uses platelets and fibrin to form a blood clot to prevent blood loss...
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 degenerationMacular degenerationAge-related macular degeneration is a medical condition which usually affects older adults and results in a loss of vision in the center of the visual field because of damage to the retina. It occurs in “dry” and “wet” forms. It is a major cause of blindness and visual impairment in older adults...
and retinal angiosclerosis - Oto-vestibular problems of a vascular nature: dizziness, auditory hallucinations, hypoacusis.
Dosages for known conditions are usually administered at 5–10 mg three times a day, however anti-aging preventative purposes may want to consider 5 mg once or twice a day more adequate.
Contraindications
Persons suffering from acute bleeding, myocardial infarctionMyocardial infarction
Myocardial infarction or acute myocardial infarction , commonly known as a heart attack, results from the interruption of blood supply to a part of the heart, causing heart cells to die...
(heart conditions), hypertension, bradycardia
Bradycardia
Bradycardia , in the context of adult medicine, is the resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min. It may cause cardiac arrest in some patients, because those with bradycardia may not be pumping enough oxygen to their heart...
or using alpha or beta receptor agonists should consult with their physician before use.
Although toxicology studies have not shown nicergoline to have any teratogenic effect, the use of this medicine during pregnancy should be limited to those cases where it is absolutely necessary.
Nicergoline is considered unsafe in porphyria
Porphyria
Porphyrias are a group of inherited or acquired disorders of certain enzymes in the heme bio-synthetic pathway . They are broadly classified as acute porphyrias and cutaneous porphyrias, based on the site of the overproduction and accumulation of the porphyrins...
.
Adverse effects
The side effects of nicergoline are usually limited to nausea, hot flushes, mild gastric upset, hypotension and dizziness. At high dosages bradycardiaBradycardia
Bradycardia , in the context of adult medicine, is the resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min. It may cause cardiac arrest in some patients, because those with bradycardia may not be pumping enough oxygen to their heart...
, increased appetite, agitation, diarrhea and perspiration have been known to occur. A single case of acute interstitial nephritis
Interstitial nephritis
Interstitial nephritis is a form of nephritis affecting the interstitium of the kidneys surrounding the tubules...
has been reported.
Interactions
Nicergoline is known to enhance the cardiac depressive effects of propranolol. At high dosages, it is advisable to seek one’s physician's guidance if combining with potent vasodilators such as bromocriptineBromocriptine
Bromocriptine , an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease , hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.- Indications :Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly...
, Gingko biloba, picamilon
Picamilon
Picamilon is a dietary supplement formed by combining niacin with GABA. It was developed in the Soviet Union in 1969 by the All-Union Vitamins Scientific Research Institute and further studied in both Russia and Japan as a prodrug of GABA.Picamilon is sold in the United States as a dietary...
, vinpocetine
Vinpocetine
Vinpocetine is a semisynthetic derivative alkaloid of vincamine , an extract from the periwinkle plant....
or xantinol nicotinate
Xantinol nicotinate
Xantinol nicotinate is a vasodilator. It is a combination of xanthinol and niacin ....
.
Mechanism of action
Nicergoline is an ergot alkaloid derivative that acts as a potent and selective alpha-1A adrenergic receptorAlpha-1A adrenergic receptor
The alpha-1A adrenergic receptor , also known as ADRA1A, formerly known as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it.-Agonists:...
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
Nerve growth factor
Nerve growth factor is a small secreted protein that is important for the growth, maintenance, and survival of certain target neurons . It also functions as a signaling molecule. It is perhaps the prototypical growth factor, in that it is one of the first to be described...
in the aged brain.
External links
- National Electronic Library for Medicines Nicergoline for dementia and other age associated forms of cognitive impairment.