Ergoloid

Overview

Ergoloid mesylates (USAN), co-dergocrine mesilate (BAN) or dihydroergotoxine mesylate, trade name Hydergine, is a mixture of the methanesulfonate salts of three dihydrogenated ergot alkaloids (dihydroergocristine, dihydroergocornine, and alpha- and beta-dihydroergocryptine). WP

It was developed by Albert Hofmann (the discoverer of LSD) for Sandoz (now part of Novartis). WP

Uses, dosage and effects

Medical uses

It has been used to treat dementia and age-related cognitive impairment (such as in Alzheimer's disease), as well as to aid in recovery after stroke.[1] WP

A systematic review published in 1994 found little evidence to support the use of ergoloid mesylates, concluding only that potentially effective doses may be higher than those currently approved in dementia treatment.[2] WP

Ergoloid Mesylate Tablets USP for sublingual use contain 1 mg of Ergoloid Mesylates USP, a mixture of the methanesulfonate salt of the following hydrogenated alkaloids: Dihydroergocornine mesylate 0.333 mg, Dihydroergocristine mesylate 0.333 mg, Dihydroergocryptine mesylate 0.333 mg.[3] WP

It has been used to treat hyperprolactinemia (high prolactin levels).[4] WP

The use of ergoloid alkaloids for dementia has been surrounded with uncertainties. In 2000, a systematic Cochrane review concluded that hydergine was well tolerated and showed significant treatment effects when assessed by either global ratings or comprehensive rating scales. The small number of available trials for analysis, however, limited the ability to demonstrate statistically significant moderating effects in certain subgroups (e.g. younger age, higher dosage, Alzheimer disease).[5] WP

Risks and side effects

Contraindications

Ergoloid is contraindicated in individuals who have previously shown hypersensitivity to the drug. They are also contraindicated in patients who have psychosis, acute or chronic, regardless of etiology. Specific drug interactions are unknown but it has been claimed that there are multiple potential interactions.[6] WP

Side effects

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:[6][7][8] WP

• Cardiovascular: orthostatic hypotension, bradycardia[6][7][8] WP
• Dermatologic: skin rash, flushing[6][7][8] WP
• Ocular: blurred vision[6][7][8] WP
• Respiratory: nasal congestion[6][7][8] WP
• Possible risk of fibrosis and ergotism[9][10] WP⚠ Wikipedia itself has flagged this text: failed verification.

As a result of the last-mentioned effects, the use of ergoline derivatives for the treatment of blood circulation disorders, memory problems, sensation problems and the treatment of migraine is no longer permitted in some EU countries because the risks are believed to outweigh any benefits. However, this concern may be unnecessarily suppressing the use of ergoline medications.[9][11] WP

Pharmacology

Mechanism of action

Despite the fact that this drug 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. 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. This 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.[7][12][13][14] WP

Legal status

Brand names

Brand names include Hydergine, Hydergina, Gerimal, Niloric, Redizork, Alkergot, Cicanol, Redergin, and Hydrine. WP

Chemistry

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Flynn BL, Ranno AE. Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. The Annals of Pharmacotherapy. February 1999. doi:10.1345/aph.17172 · PMID 10084415
2. Journal / agency Schneider LS, Olin JT. Overview of clinical trials of hydergine in dementia. Archives of Neurology. August 1994. doi:10.1001/archneur.1994.00540200063018 · PMID 8042927
3. Other Ergoloid
4. Journal / agency Bankowski BJ, Zacur HA. Dopamine agonist therapy for hyperprolactinemia. Clinical Obstetrics and Gynecology. June 2003. doi:10.1097/00003081-200306000-00013 · PMID 12808385
5. Journal / agency Olin J, Schneider L, Novit A, Luczak S. Hydergine for dementia. The Cochrane Database of Systematic Reviews. 2001. doi:10.1002/14651858.CD000359 · PMID 11405961 · PMC6769017
6. Journal / agency Drugs to Treat Alzheimer's Disease. Journal of Psychosocial Nursing & Mental Health Services. April 2014
7. Journal / agency Schiff PL. Ergot and its alkaloids. American Journal of Pharmaceutical Education. October 2006. doi:10.5688/aj700598 · PMID 17149427 · PMC1637017
8. Journal / agency Majumdar A, Mangal NS. Hyperprolactinemia. Journal of Human Reproductive Sciences. July 2013. doi:10.4103/0974-1208.121400 · PMID 24347930 · PMC3853872
9. Journal / agency Ergot derivatives: restricted use. WHO Drug Information. 2013
10. Journal / agency Helsen V, Decoutere L, Spriet I, Fagard K, Boonen S, Tournoy J. Ergotamine-induced pleural and pericardial effusion successfully treated with colchicine. Acta Clinica Belgica. 2013. doi:10.2143/ACB.3138 · PMID 23967719
11. Journal / agency Zajdel P, Bednarski M, Sapa J, Nowak G. Ergotamine and nicergoline - facts and myths. Pharmacological Reports. April 2015. doi:10.1016/j.pharep.2014.10.010 · PMID 25712664
12. Journal / agency Markstein R. Hydergine: interaction with the neurotransmitter systems in the central nervous system. Journal de Pharmacologie. 1985. PMID 2869188
13. Journal / agency Rowell PP, Larson BT. Ergocryptine and other ergot alkaloids stimulate the release of [3H]dopamine from rat striatal synaptosomes. Journal of Animal Science. July 1999. doi:10.2527/1999.7771800x · PMID 10438027
14. Journal / agency Kennedy GJ, Tanenbaum S. Suicide and aging: international perspectives. The Psychiatric Quarterly. Dec 2000. doi:10.1023/a:1004636307592 · PMID 11025912

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0). Each value links to the exact revision it came from.