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Ergoloid
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| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | |
| ATC code | C04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C33H45N5O5 |
| Mol. mass | 591.741 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 25% |
| Protein binding | 98-99% |
| Metabolism | 50% |
| Half life | 3.5 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | Oral, Parenteral |
Ergoloid mesylates (USAN) or co-dergocrine mesylate (BAN) is a mixture of the methanesulfonate salts of three dihydrogenated ergot alkaloids (dihydroergocristine, dihydroergocornine, and alpha- and beta-dihydroergocryptine). It is used to treat dementia and age-related cognitive impairment, as well as to aid in recovery after stroke. Ergoloids are also used by many people as a nootropic. It was developed by Albert Hofmann for Sandoz (now part of Novartis).
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Mechanism of action
Despite the fact that hydergine has been used in the treatment of dementia for many years, its mechanism of action is still not clear. It stimulates dopaminergic and serotonergic receptors and blocks alpha-adrenoreceptors. It is a nootropic. 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.
Names
Brand names
Hydergine, Hydergina, Gerimal, Niloric, Redizork, Alkergot, Cicanol, Redergin.
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 etiology. Specific drug interactions are unknown so administration should be done with care and proper research.
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 nausea, gastrointestinal disturbances and sublingual irritation with SL tablets. Other common side effects include:
Cardiovascular: orthostatic hypotension, bradycardia
Dermatologic: skin rash, flushing
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, with which it is synergesic.
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.[1]
External links
- ^ Schneider; Olin (Aug 1994). "Overview of clinical trials of hydergine in dementia". Archives of Neurology 51 (8). PMID 8042927.
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Wikipedia content modification information:
- This page was last modified on 16 September 2008, at 02:42.
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