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DA agonists - Ergot derivaties: Dihydroergocryptine (DHEC)


Book ID
102505271
Publisher
John Wiley and Sons
Year
2002
Tongue
English
Weight
51 KB
Volume
17
Category
Article
ISSN
0885-3185

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โœฆ Synopsis


BASIC PHARMACOLOGY MECHANISM OF ACTION

DHEC is a dihydro-derivative of ergocryptine acting as a D2 agonist and a partial D1 agonist. Therefore, DHEC has a pharmacodynamic profile quite comparable to that of bromocriptine. Like all ergotamine derivatives, DHEC has effects on serotonergic and adrenergic receptors. 1,2 DHEC improves the symptoms of the MPTP-treated monkey model of Parkinson's disease (PD). In healthy volunteers, its effects on D2 receptors reduce prolactin plasma levels, and induce nausea and hypotension. Preclinical data suggest that DHEC may have neuroprotective properties. 3,4 PHARMACOKINETICS DHEC, like other ergot derivatives, has linear kinetics. Its oral bioavailability after first pass effect is low (below 5%). It has linear metabolism with generation of active metabolites, is eliminated through feces, and has no interference with L-dopa kinetics.

REVIEW OF CLINICAL STUDIES PREVENTION OF DISEASE PROGRESSION

No qualified studies were identified.


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