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
- DOI
- 10.1002/mds.5564
No coin nor oath required. For personal study only.
โฆ 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.
๐ SIMILAR VOLUMES
Lisuride is an alpha-amino-ergoline with D2 receptor agonist properties and has no apparent D1 receptor effects. Similar to most ergotamine derivatives, lisuride also has 5-HT2 activity. In animal models of Parkinson's disease (PD), lisuride antagonizes reserpine-induced akinesia and induces rotatio
In de novo patients with early parkinsonism, acute subcutaneous challenges with apomorphine monotherapy have been proposed to test the dopaminergic responsiveness of the motor symptoms in order to help clinicians in differential diagnosis between "idiopathic" Parkinson's disease and other parkinsoni
Piribedil is a non-ergot derivative D2/D-3 agonist 1 with alpha-2 antagonistic effects 2 . Piribedil is effective in reversing parkinsonian symptoms in the MPTP-treated primate 3 . The clinical effects of piribedil cause lower prolactin plasma levels and blood pressure, and induces nausea. There is