ERGOLOIDS

US Previously Marketed

First approved in 1953

Description
Sources: https://www.drugs.com/pro/ergoloid.html
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB01049 | http://www.solutionspharmacyrx.com/drug-detail/3432 | https://www.ncbi.nlm.nih.gov/pubmed/32430 | https://www.ncbi.nlm.nih.gov/pubmed/4894

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). Ergoloid mesylates act centrally, decreasing vascular tone and slowing the heart rate, and acts peripherally to block alpha-receptors. One other possible mechanism is the effect of ergoloid mesylates on neuronal cell metabolism, resulting in improved oxygen uptake and cerebral metabolism, thereby normalizing depressed neurotransmitter levels. Ergoloid Mesylate may increase cerebral metabolism and blood flow. The role of this medication in the therapy of dementia is controversial. A recent controlled study in patients with Alzheimer's disease found that there was no advantage to the use of ergoloid mesylates compared to placebo, suggesting that ergoloid mesylates may lower scores on some cognitive and behavioral rating scales. Further study is needed to determine the risk-benefit profile of ergoloid mesylates in the treatment of dementia.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adrenergic receptor alpha 65 Target ID: CHEMBL2095203 Sources: https://www.ncbi.nlm.nih.gov/pubmed/4894	Blocker 555

Conditions

Condition	Modality	Highest Phase	Product
Primary progressive dementia 2 Sources: http://www.solutionspharmacyrx.com/drug-detail/3432	Primary	Approved 8583	HYDERGINE Approved Use Indications and Usage. Treatment of age-related decline in mental capacity, primary progressive dementia, Alzheimer dementia, multi-infarct dementia and senile onset. Launch Date 1977
Alzheimer's dementia 6 Sources: http://www.solutionspharmacyrx.com/drug-detail/3432	Primary	Approved 8583	HYDERGINE Approved Use Indications and Usage. Treatment of age-related decline in mental capacity, primary progressive dementia, Alzheimer dementia, multi-infarct dementia and senile onset. Launch Date 1977
Multi-infarct dementia 2 Sources: http://www.solutionspharmacyrx.com/drug-detail/3432	Primary	Approved 8583	HYDERGINE Approved Use Indications and Usage. Treatment of age-related decline in mental capacity, primary progressive dementia, Alzheimer dementia, multi-infarct dementia and senile onset. Launch Date 1977

C_max

Value	Dose	Analyte	Population
239 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
384 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
490 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
426 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
317 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, sublingual dose: 6 mg route of administration: Sublingual experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
343 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
308 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
385 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	9 mg single, oral dose: 9 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
288 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	9 mg single, oral dose: 9 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

AUC

Value	Dose	Analyte	Population
1051 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2054 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2813 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2080 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2322 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, sublingual dose: 6 mg route of administration: Sublingual experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2089 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2028 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2134 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	9 mg single, oral dose: 9 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2085 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	9 mg single, oral dose: 9 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

T_1/2

Value	Dose	Analyte	Population
2.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	3 mg single, oral dose: 3 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, sublingual dose: 6 mg route of administration: Sublingual experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	9 mg single, oral dose: 9 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3207855/	9 mg single, oral dose: 9 mg route of administration: Oral experiment type: SINGLE co-administered:	ERGOLOIDS plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED

Doses

Dose	Population	Adverse events
9 mg single, oral Highest studied dose Dose: 9 mg Route: oral Route: single Dose: 9 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11215321/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/11215321/	Sources: https://pubmed.ncbi.nlm.nih.gov/11215321/
2.5 mg 2 times / day multiple, oral Studied dose Dose: 2.5 mg, 2 times / day Route: oral Route: multiple Dose: 2.5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30177490/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/30177490/	Sources: https://pubmed.ncbi.nlm.nih.gov/30177490/
2 mg 3 times / day multiple, sublingual Dose: 2 mg, 3 times / day Route: sublingual Route: multiple Dose: 2 mg, 3 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/762369/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/762369/	Sources: https://pubmed.ncbi.nlm.nih.gov/762369/

PubMed

Title	Date	PubMed
Beta-ergokryptine, a new alkaloid of the ergotoxine group.	1967-12-15	4965668

Patents

Sample Use Guides

In Vivo Use Guide

PO/sublingual 1 to 2 mg 3 times daily (up to 12 mg/day has been used).

Route of Administration: Oral

In Vitro Use Guide

Mouse C1300 neuroblastoma cells were culturcd in medium having a pH of 7.3-7.4 (regular medium) and in medium having a pH of 6.6-6.8 (low pH medium). Cells were treated with Hydergine (Ergoloid mesylates) in various concentrations (0.1-10mkg/ml) for 8 days, and at the end of this time cell viability, cell number, neurites formation and lipofusein pigment formation were assessed. Hydergine, betwen 0.1 and 3 mkg/ml, caused aconcentration-related decrease in pigment content. Hydergine also stimulated neurite formation in cells in regular pH medium and was slightly toxic to cells in low pH medium.

Substance Class	Mixture Created by `admin` on `Mon Mar 31 18:06:40 GMT 2025` Edited by `admin` on `Mon Mar 31 18:06:40 GMT 2025`
Record UNII	34HPE9Z8IP
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

DIHYDROERGOTOXINE

Preferred Name

English

ERGOLOIDS

Common Name

English

CODERGOCRINE

Common Name

English

DIHYDROERGOTOXINE [VANDF]

Common Name

English

Dihydroergotoxine [WHO-DD]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175766