Ergoloid mesylates
Encyclopedia
Ergoloid mesylates or codergocrine mesilate (BAN
), trade name Hydergine, is a mixture of the methanesulfonate
salts of three dihydrogenated
ergot
alkaloid
s (dihydroergocristine
, dihydroergocornine
, and alpha- and beta-dihydroergocryptine
).
It was developed by Albert Hofmann
(the same discoverer of LSD
) for Sandoz
(now part of Novartis
).
and age-related cognitive impairment (such as in Alzheimer disease), as well as to aid in recovery after stroke
.
Ergoloids are also used by many people as a nootropic
.
is still not clear. It stimulates dopamine
rgic and serotonergic
receptors and blocks alpha-adrenoreceptors. Current studies imply that the major effect of hydergine may be the modulation of synaptic neurotransmission rather than solely increasing blood flow as was once thought. A prominent feature that accompanies aging is an increase in monoamine oxidase
(MAO) levels which results in decreased availability of catecholamines in the synaptic cleft. In one study, an interaction between age and hydergine treatment was observed in the hypothalamus
, hippocampus
and cerebellum
. The hydergine effect was more pronounced in the aged group in the hypothalamus and cerebellum, and more pronounced in the adult in the hippocampus
. These findings imply that increased brain MAO activity in aging can be modified by hydergine treatment in some brain regions.
Dihydroergotoxine Mesilate, Dihydroergotoxine Mesylate, Dihydroergotoxine Methanesulfonate, Dihydroergotoxine Methanesulphonate, Ergoloid Mesylates, Hydergine, Hydergine LC, Hydrogenated Ergot Alkaloids, Ischelium.
.
Specific drug interactions are unknown so administration should be done with care.
Cardiovascular: orthostatic hypotension
, bradycardia
Dermatologic: skin rash
, flushing
Ocular: blurred vision
Respiratory: nasal congestion
Alleviation of symptoms is usually gradual and effects may be seen in 3–4 weeks.
It may be used in conjunction with other cerebral enhancers like Piracetam
, with which it is synergistic.
Sizes: 4.5 mg p/T (x30) or 1.5 mg p/T
There is some evidence suggesting that potentially effective doses may be higher than those currently approved.
British Approved Name
A British Approved Name is the official non-proprietary or generic name given to a pharmaceutical substance, as defined in the British Pharmacopoeia...
), trade name Hydergine, is a mixture of the methanesulfonate
Mesylate
In chemistry, a mesylate is any salt or ester of methanesulfonic acid . In salts, the mesylate is present as the CH3SO3− anion. When modifying the International Nonproprietary Name of a pharmaceutical substance containing the group or anion, the correct spelling is mesilate .Mesylate esters are a...
salts of three dihydrogenated
Hydrogenation
Hydrogenation, to treat with hydrogen, also a form of chemical reduction, is a chemical reaction between molecular hydrogen and another compound or element, usually in the presence of a catalyst. The process is commonly employed to reduce or saturate organic compounds. Hydrogenation typically...
ergot
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...
alkaloid
Alkaloid
Alkaloids are a group of naturally occurring chemical compounds that contain mostly basic nitrogen atoms. This group also includes some related compounds with neutral and even weakly acidic properties. Also some synthetic compounds of similar structure are attributed to alkaloids...
s (dihydroergocristine
Dihydroergocristine
Dihydroergocristine is an ergot alkaloid. Alongside dihydroergocornine and dihydroergocryptine, it is one of the components of ergoloid....
, dihydroergocornine
Dihydroergocornine
Dihydroergocornine is an ergot alkaloid. Alongside dihydroergocristine and dihydroergocryptine, it is one of the three components of ergoloid....
, and alpha- and beta-dihydroergocryptine
Dihydroergocryptine
Dihydroergocryptine is a dopamine agonist of the ergoline chemical class used as an antiparkinson agent....
).
It was developed by Albert Hofmann
Albert Hofmann
Albert Hofmann was a Swiss scientist known best for being the first person to synthesize, ingest and learn of the psychedelic effects of lysergic acid diethylamide . He authored more than 100 scientific articles and a number of books, including LSD: My Problem Child...
(the same discoverer of LSD
LSD
Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an...
) for Sandoz
Sandoz
Founded in 2003, Sandoz presently is the generic drug subsidiary of Novartis, a multinational pharmaceutical company. The company develops, manufactures and markets generic drugs as well as pharmaceutical and biotechnological active ingredients....
(now part of Novartis
Novartis
Novartis International AG is a multinational pharmaceutical company based in Basel, Switzerland, ranking number three in sales among the world-wide industry...
).
Uses
It has been used to treat dementiaDementia
Dementia is a serious loss of cognitive ability in a previously unimpaired person, beyond what might be expected from normal aging...
and age-related cognitive impairment (such as in Alzheimer disease), as well as to aid in recovery after stroke
Stroke
A stroke, previously known medically as a cerebrovascular accident , is the rapidly developing loss of brain function due to disturbance in the blood supply to the brain. This can be due to ischemia caused by blockage , or a hemorrhage...
.
Ergoloids are also used by many people as a nootropic
Nootropic
Nootropics , also referred to as smart drugs, brain steroids, memory enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration...
.
Mechanism of action
Despite the fact that hydergine has been used in the treatment of dementia for many years, its mechanism of actionMechanism of action
In pharmacology, the term mechanism of action refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect...
is still not clear. It stimulates dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
rgic and serotonergic
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
receptors and blocks alpha-adrenoreceptors. Current studies imply that the major effect of hydergine may be the modulation of synaptic neurotransmission rather than solely increasing blood flow as was once thought. A prominent feature that accompanies aging is an increase in monoamine oxidase
Monoamine oxidase
L-Monoamine oxidases are a family of enzymes that catalyze the oxidation of monoamines. They are found bound to the outer membrane of mitochondria in most cell types in the body. The enzyme was originally discovered by Mary Bernheim in the liver and was named tyramine oxidase...
(MAO) levels which results in decreased availability of catecholamines in the synaptic cleft. In one study, an interaction between age and hydergine treatment was observed in the hypothalamus
Hypothalamus
The Hypothalamus is a portion of the brain that contains a number of small nuclei with a variety of functions...
, hippocampus
Hippocampus
The hippocampus is a major component of the brains of humans and other vertebrates. It belongs to the limbic system and plays important roles in the consolidation of information from short-term memory to long-term memory and spatial navigation. Humans and other mammals have two hippocampi, one in...
and cerebellum
Cerebellum
The cerebellum is a region of the brain that plays an important role in motor control. It may also be involved in some cognitive functions such as attention and language, and in regulating fear and pleasure responses, but its movement-related functions are the most solidly established...
. The hydergine effect was more pronounced in the aged group in the hypothalamus and cerebellum, and more pronounced in the adult in the hippocampus
Hippocampus
The hippocampus is a major component of the brains of humans and other vertebrates. It belongs to the limbic system and plays important roles in the consolidation of information from short-term memory to long-term memory and spatial navigation. Humans and other mammals have two hippocampi, one in...
. These findings imply that increased brain MAO activity in aging can be modified by hydergine treatment in some brain regions.
Chemical agent synonyms and analogues
Co-Dergocrine Mesylate, Deapril-ST, Dihydroergotoxin Mesilat, Dihydroergotoxin Mesylate, Dihydroergotoxin Methanesulfonate,Dihydroergotoxine Mesilate, Dihydroergotoxine Mesylate, Dihydroergotoxine Methanesulfonate, Dihydroergotoxine Methanesulphonate, Ergoloid Mesylates, Hydergine, Hydergine LC, Hydrogenated Ergot Alkaloids, Ischelium.
Contra-indications
Hydergine (ergoloid mesylates) preparations are contraindicated in individuals who have previously shown hypersensitivity to the drug. Hydergine (ergoloid mesylates) preparations are also contraindicated in patients who have psychosis, acute or chronic, regardless of etiologyEtiology
Etiology is the study of causation, or origination. The word is derived from the Greek , aitiologia, "giving a reason for" ....
.
Specific drug interactions are unknown so administration should be done with care.
Precautions
Pleural and peritoneal fibrosis have been reported with prolonged daily use. Cardiac valvular fibrosis has also been associated with ergot alkaloids.Adverse reactions
Adverse effects are minimal. The most common include transient, dose dependent nausea and gastrointestinal disturbances and sublingual irritation with SL tablets. Other common side effects include:Cardiovascular: orthostatic hypotension
Orthostatic hypotension
Orthostatic hypotension, also known as postural hypotension, orthostasis, and colloquially as head rush or dizzy spell, is a form of hypotension in which a person's blood pressure suddenly falls when the person stands up or stretches. The decrease is typically greater than 20/10 mm Hg, and may be...
, 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...
Dermatologic: skin rash
Rash
A rash is a change of the skin which affects its color, appearance or texture. A rash may be localized in one part of the body, or affect all the skin. Rashes may cause the skin to change color, itch, become warm, bumpy, chapped, dry, cracked or blistered, swell and may be painful. The causes, and...
, flushing
Flushing (physiology)
For a person to flush is to become markedly red in the face and often other areas of the skin, from various physiological conditions. Flushing is generally distinguished, despite a close physiological relation between them, from blushing, which is milder, generally restricted to the face, cheeks or...
Ocular: blurred vision
Respiratory: nasal congestion
Dosage
1 mg three times per day is the recommended dosage.Alleviation of symptoms is usually gradual and effects may be seen in 3–4 weeks.
It may be used in conjunction with other cerebral enhancers like Piracetam
Piracetam
Piracetam is a nootropic drug. Piracetam's chemical name is 2-oxo-1-pyrrolidine acetamide; it shares the same 2-oxo-pyrrolidone base structure with 2-oxo-pyrrolidine carboxylic acid . Piracetam is a cyclic derivative of GABA. It is one of the group of racetams...
, with which it is synergistic.
Sizes: 4.5 mg p/T (x30) or 1.5 mg p/T
There is some evidence suggesting that potentially effective doses may be higher than those currently approved.