Hydergine

ヒデルギン

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/22 21:56:50」(JST)

wiki en

[Wiki en表示]

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 Y
ATC code	C04AE01
DrugBank	DB01049 Y
ChEBI	CHEBI:59756 N
N (what is this?)  (verify)

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), 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.

Ergoloids are also used by many people as a nootropic. It may be used in conjunction with other cerebral enhancers like piracetam, with which it may act synergistically.

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.

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. 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.

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.

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, bradycardia
• Dermatologic: skin rash, flushing
• Ocular: blurred vision
• Respiratory: nasal congestion
• Increased risk of fibrosis and ergotism.

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.

Chemistry

The four constituents differ only in which of four proteinogenic amino acids is used in biosynthesis:

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

Trade names

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

References

External links

• Ergoloid Mesylates (University of Maryland Medical Center)

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

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

English Journal

• Effect of electroacupuncture on brain-derived neurotrophic factor mRNA expression in mouse hippocampus following cerebral ischemia-reperfusion injury.

• Zhao J, Xu H, Tian Y, Hu M, Xiao H.SourceThe Third Hospital Affiliated to Beijing University of Traditional Chinese Medicine, Beijing 100029, China.
• Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan / sponsored by All-China Association of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine.J Tradit Chin Med.2013 Apr;33(2):253-7.
• OBJECTIVE: This work aims to observe the effects of electroacupuncture on brain-derived neurotrophic factor (BDNF) mRNA expression in mouse hippocampus following cerebral ischemia-reperfusion injury.METHODS: The models of mouse cerebral ischemia-reperfusion injury were established. A total of 96 hea
• PMID 23789227

• Effects of electroacupuncture on hippocampal and cortical apoptosis in a mouse model of cerebral ischemia-reperfusion injury.

• Zhao JX, Tian YX, Xiao HL, Hu MX, Chen WR.SourceThe Third Hospital Affiliated to Beijing University of Chinese Medicine, Beijing 100029, China.
• Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan / sponsored by All-China Association of Traditional Chinese Medicine, Academy of Traditional Chinese Medicine.J Tradit Chin Med.2011 Dec;31(4):349-55.
• OBJECTIVE: To observe the effects of electroacupuncture on hippocampal and cortical apoptosis in a mouse model of cerebral ischemia-reperfusion injury.METHODS: Mouse models established by repeated cerebral ischemia-reperfusion, followed by electroacupuncture at Shenshu, Geshu, and Baihui points. The
• PMID 22462244

• Alternative drug therapies for dementia.

• Howland RH.SourceUniversity of Pittsburg School of Medicine, Western Psychiatric Institute and Clinic, Pittsburg, Pennsylvania 15213, USA. HowlandRH@upmc.edu
• Journal of psychosocial nursing and mental health services.J Psychosoc Nurs Ment Health Serv.2011 May;49(5):17-20. doi: 10.3928/02793695-20110407-03. Epub 2011 Apr 27.
• Drugs currently approved by the U.S. Food and Drug Administration (FDA) for the treatment of Alzheimer's disease include acetylcholinesterase inhibitor (i.e., tacrine, donepezil, rivastigmine, and galantamine) and glutamate-modulating (i.e., memantine) drugs. Because these drugs have modest benefits
• PMID 21553703

Japanese Journal

• 強皮症におけるレイノー現象に対するヒデルギン錠の臨床的有用性の検討

• 西日本皮膚科 58(5), 840-842, 1996
• NAID 130004474237

• 耳鳴の薬物療法-テルネリン単独とヒデルギン併用

• 耳鼻咽喉科臨床 88(5), 645-656, 1995-05-01
• NAID 10005603900

• 耳鳴患者に対するメシル酸ジヒドロエルゴトキシンおよびフマル酸プロビンカミン併用療法による臨床治験

• 耳鼻咽喉科展望 34, 271-280, 1991
• NAID 130003974582

---

★リンクテーブル★

リンク元	「ジヒドロエルゴトキシン」「ergoloid mesylate」

「ジヒドロエルゴトキシン」

　　[★]

英

dihydroergotoxine

化

ジヒドロエルゴトキシンメシル酸塩 メシル酸ジヒドロエルゴトキシン dihydroergotoxine mesilate

商

エポス、バソラックス、ヒデルギン Hydergine

関

その他の循環器官用薬。メシル酸エルゴロイド

• 脳循環改善薬

「ergoloid mesylate」

　　[★]

メシル酸エルゴロイド

関

Hydergine