It has been used to treatdementia and age-related cognitive impairment (such as inAlzheimer disease),[1] as well as to aid in recovery afterstroke.
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]
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]
The use of ergoloid alkaloids for dementia has been surrounded with uncertainties. In 2000, a systematicCochrane 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]
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 ofetiology.[6] Specific drug interactions are unknown but it has been claimed that there are multiple potential interactions.[6]
Adverse effects are minimal. The most common include transient, dose dependent nausea and gastrointestinal disturbances,[7] and sublingual irritation with SL tablets. Other common side effects include:[6][8]
As a result of the last-mentioned effects, the use ofergoline 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.[9] However, this concern may be unnecessarily suppressing the use of ergoline medications.[11]
Despite the fact that this drug has been used in the treatment of dementia for many years, itsmechanism of action is still not clear.[7] It stimulatesdopaminergic andserotonergic receptors and blocks alpha-adrenoreceptors.[12] 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.[13] A prominent feature that accompanies aging is an increase inmonoamine oxidase (MAO) levels.[14] This results in decreased availability ofcatecholamines in the synaptic cleft. In one study, an interaction between age and hydergine treatment was observed in thehypothalamus,hippocampus andcerebellum. The hydergine effect was more pronounced in the aged group in the hypothalamus and cerebellum, and more pronounced in the adult in thehippocampus. These findings imply that increased brain MAO activity in aging can be modified by hydergine treatment in some brain regions.
^Markstein R (1985). "Hydergine: interaction with the neurotransmitter systems in the central nervous system".Journal de Pharmacologie.16 (Suppl 3):1–17.PMID2869188.
^Rowell PP, Larson BT (July 1999). "Ergocryptine and other ergot alkaloids stimulate the release of [3H]dopamine from rat striatal synaptosomes".Journal of Animal Science.77 (7):1800–1806.doi:10.2527/1999.7771800x.PMID10438027.
^Steinhilber D, Schubert-Zsilavecz M, Roth HJ (2005).Medizinische Chemie (in German). Stuttgart, Germany: Deutscher Apotheker Verlag. p. 142.ISBN3-7692-3483-9.
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