ERGOLOID MESYLATES

Description

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 64	Blocker 537

Conditions

Condition	Modality	Highest Phase	Product
Primary progressive dementia 2	Primary	Approved 8,429	HYDERGINE
Alzheimer's dementia 6	Primary	Approved 8,429	HYDERGINE
Multi-infarct dementia 2	Primary	Approved 8,429	HYDERGINE

C_max

Value	Dose	Analyte	Population
239 pg/mL	3 mg single, oral	ERGOLOIDS plasma	Homo sapiens
384 pg/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
490 pg/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
426 pg/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
317 pg/mL	6 mg single, sublingual	ERGOLOIDS plasma	Homo sapiens
343 pg/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
308 pg/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
385 pg/mL	9 mg single, oral	ERGOLOIDS plasma	Homo sapiens
288 pg/mL	9 mg single, oral	ERGOLOIDS plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
1051 pg × h/mL	3 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2054 pg × h/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2813 pg × h/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2080 pg × h/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2322 pg × h/mL	6 mg single, sublingual	ERGOLOIDS plasma	Homo sapiens
2089 pg × h/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2028 pg × h/mL	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2134 pg × h/mL	9 mg single, oral	ERGOLOIDS plasma	Homo sapiens
2085 pg × h/mL	9 mg single, oral	ERGOLOIDS plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
2.2 h	3 mg single, oral	ERGOLOIDS plasma	Homo sapiens
3.2 h	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
3.6 h	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
3.7 h	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
4.9 h	6 mg single, sublingual	ERGOLOIDS plasma	Homo sapiens
3.9 h	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
4.3 h	6 mg single, oral	ERGOLOIDS plasma	Homo sapiens
3.4 h	9 mg single, oral	ERGOLOIDS plasma	Homo sapiens
4 h	9 mg single, oral	ERGOLOIDS plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
9 mg single, oral Highest studied dose	healthy, ADULT
2.5 mg 2 times / day multiple, oral Studied dose	unhealthy, ADULT
2 mg 3 times / day multiple, sublingual	unhealthy, ADULT

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PubMed

Title	Date	PubMed
No data available in table

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.