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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).

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

Uses

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

There is some evidence suggesting that potentially effective doses may be higher than those currently approved in dementia treatment.^[2]

Ergoloids are also used by many people as a nootropic.^{[citation needed]} It may be used in conjunction with other cerebral enhancers like piracetam, with which it may act synergistically.^[3]^{[unreliable source?]}

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.^[4]

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.^[5] It stimulates dopaminergic and serotonergic receptors and blocks alpha-adrenoreceptors.^[6] 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.^[7] A prominent feature that accompanies aging is an increase in monoamine oxidase (MAO) levels.^[8] 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.

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.^[9] Specific drug interactions are unknown but it has been claimed that there are multiple potential interactions.^[9]

Adverse reactions

Adverse effects are minimal. The most common include transient, dose dependent nausea and gastrointestinal disturbances,^[5] and sublingual irritation with SL tablets. Other common side effects include:^[9]^[10]

Cardiovascular: orthostatic hypotension, bradycardia
Dermatologic: skin rash, flushing
Ocular: blurred vision
Respiratory: nasal congestion
Increased risk of fibrosis and ergotism.^[11]^[12]

As a result of the last-mentioned effects, the use of ergot 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.^[11]

Chemistry

The four constituents differ only in which of four proteinogenic amino acids is used in biosynthesis:^[13]

Compound	Amino acid
Dihydroergocristine	Phenylalanine
Dihydroergocornine	Valine
alpha-Dihydroergocryptine	Leucine
beta-Dihydroergocryptine	Isoleucine

Trade names

Hydergine, Hydergina, Gerimal, Niloric, Redizork, Alkergot, Cicanol, Redergin.

References

^ Flynn, B. L.; Ranno, A. E. (February 1999). "Pharmacologic Management of Alzheimer Disease, Part II: Antioxidants, Antihypertensives, and Ergoloid Derivatives". Annals of Pharmacotherapy 33 (2): 188–197. doi:10.1345/aph.17172. PMID 10084415.
^ Schneider, L. S.; Olin, J. T. (August 1994). "Overview of Clinical Trials of Hydergine in Dementia". Archives of Neurology 51 (8): 787–798. doi:10.1001/archneur.1994.00540200063018. PMID 8042927.
^ Pearson, D.; Shaw, S. (1982). "Part III Chapter 2 : Revitalizing Your Brain Power". Life Extension - A Practical Scientific Approach. Warner Books. ISBN 0-446-51229-X.
^ Ergoloid (Drugs.com http://www.drugs.com/pro/ergoloid.html). Retrieved 08-02-2013.
^ ^a ^b Schiff, Paul L, Jr (2006) "Ergot and Its Alkaloids", American Journal of Pharmaceutical Education 70.5 p.98.
^ Markstein, R. (1985). "Hydergine: Interaction with the Neurotransmitter Systems in the Central Nervous System". Journal of Pharmacology 16 (Suppl 3): 1–17. PMID 2869188.
^ Rowell et al. (Jul 1999) "Ergocryptine and other ergot alkaloids stimulate the release of [3H] dopamine from rat striatal synaptosomes", Journal of Animal Science 77.7 pp.1800-6
^ Kennedy et al. (Dec 2000) "Suicide and Aging: International Perspectives", Psychiatric Quarterly 71.4 pp.345-62
^ ^a ^b ^c "Drugs to Treat Alzheimer's Disease" (Apr 2014) Journal of Psychosocial Nursing & Mental Health Services 52.4 pp. 21-2
^ Majumdar et al (Jul-Sep 2013) "Hyperprolactinemia", Journal of Human Reproductive Sciences 6.3 pp.168-175
^ ^a ^b "Ergot derivatives: restricted use" (2013) WHO Drug Information 27.3 p.225
^ Helsen et al. (2013) "Ergotamine-Induced Pleural and Pericardial Effusion Successfully Treated with Colchicine", Acta Clinica Belgica 68.2 pp.113-5
^ Steinhilber, D.; Schubert-Zsilavecz, M.; Roth, H. J. (2005). Medizinische Chemie (in German). Stuttgart, Germany: Deutscher Apotheker Verlag. p. 142. ISBN 3-7692-3483-9.

External links

Ergoloid Mesylates (University of Maryland Medical Center)

UpToDate Contents

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1. 脳血管性認知症の治療および予防 treatment and prevention of vascular dementia

English Journal

Influence of dihydroergotoxine, bromocriptine, and ergotamine on penile erection in Wistar rats.

Radosavljevic M, Pajovic B, Radunovic M, Radojevic N, Bjelogrlic B.SourceDepartment of Forensic Medicine, Clinical Centre of Montenegro, 2000 Podgorica, Ljubljanska 1, Montenegro.
Journal of andrology.J Androl.2012 Sep-Oct;33(5):866-71. Epub 2012 Mar 22.
The pilot study presented was conducted to determine as to whether ergot alkaloids (alpha-adrenergic blockers) have a potential effect on penile erectile function. The influence of dihydroergotoxine, bromocriptine, and ergotamine was studied on the erection ability in intact, two-grade outbred m
PMID 22441761

[The use of vasobral in patients with chronic cerebrovascular disorders].

Kamchatnov PR.
Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova / Ministerstvo zdravookhraneniia i meditsinskoĭ promyshlennosti Rossiĭskoĭ Federatsii, Vserossiĭskoe obshchestvo nevrologov [i] Vserossiĭskoe obshchestvo psikhiatrov.Zh Nevrol Psikhiatr Im S S Korsakova.2011;111(10 Pt 1):70-2.
PMID 22500318

[Use of vasobral in therapy of central nervous system pathology in children of early age].

Zaĭtseva IN.
Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova / Ministerstvo zdravookhraneniia i meditsinskoĭ promyshlennosti Rossiĭskoĭ Federatsii, Vserossiĭskoe obshchestvo nevrologov [i] Vserossiĭskoe obshchestvo psikhiatrov.Zh Nevrol Psikhiatr Im S S Korsakova.2010;110(1):92-4.
PMID 20614656

Japanese Journal

耳鳴の薬物療法-テルネリン単独とヒデルギン併用

北奥恵之,松永喬,北村溥之,安里亮,金子賢一,太田和博,上田和孝,柏木令子,横田雅子,衛藤幸男,秋岡勝哉,山中泰輝,岡亮,畠史子,岡坂利章,岡本英之,鶴田至宏,金田宏和
耳鼻咽喉科臨床 88(5), 645-656, 1995-05-01
… Patients with tinnitus were treated with Ternelin® (tizanidine hydrochloride) alone or in combination with Hydergine® (dihydroergotoxine mesylate). …
NAID 10005603900

Dopaminergic Regulation of Aldosterone Secretion in Primary Aldosteronism: A Clinical Study.

Rossi Gian Paolo,Zanin Lucia,Toni Renzo de,Venturini Roberta,Albertin Giovanna,Pavan Edoardo,Pessina Achille C
Hypertension Research 17(2), 105-115, 1994
… The DA2-antagonist metoclopramide (10mg i.v.) and the DA2-agonist dihydroergotoxine (6μg/Kg b.w. … Dihydroergotoxine significantly decreased plasma prolactin and aldosterone levels and adrenal vein aldosterone in patients with PH. In contrast, despite a similar decrease in prolactin, in PA a significant (p<0.05) increase in aldosterone was seen, both peripherally and in adrenal vein blood. …
NAID 130003456169

筋弛緩剤と代謝改善剤の併用による耳鳴治療

山際幹和,坂倉康夫,森下篤人,坂倉健二,稲垣政志,中本節夫,浜口富美,伊藤由紀子,田矢理子,久保将彦,村井須美子,矢野原邦生,荘司邦夫,前田太郎
耳鼻咽喉科臨床 86(11), 1661-1668, 1993
… used tizanidine hydrochloride, a muscle relaxant, and dihydroergotoxine mesilate, an activator of central nervous system function, as basic drugs in the treatment of 48 patients with tinnitus (25 males and 23 females, aged 25 to 82 years).Usual amounts of the two drugs were administered daily alone or in combination with other drugs for 2 to 31 weeks, and the clinical effect was evaluated by analyzing subjective tinnitus and accompanying symptoms before and after treatment.Loudness, continuousness and distress of tinnitus, and headache and shoulder …
NAID 130001812550

Related Pictures

★リンクテーブル★

リンク元	「脳保護薬」「ジヒドロエルゴトキシン」
拡張検索	「dihydroergotoxine mesilate」

「脳保護薬」

Ergoloid
Combination of
Dihydroergocristine	Ergot alkaloid
Dihydroergocornine	Ergot alkaloid
alpha-Dihydroergocryptine	Ergot alkaloid
beta-Dihydroergocryptine	Ergot alkaloid
Clinical data
Pregnancy; category	Contraindicated;
Legal status	℞ (Prescription only);
Routes of; administration	Oral, parenteral
Identifiers
CAS Registry Number	8067-24-1
ATC code	C04AE01
DrugBank	DB01049
ChEBI	CHEBI:59756
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