Lisuride, a Dopamine Receptor Agonist With 5-HT2B Receptor Antagonist Properties: Absence of Cardiac Valvulopathy Adverse Drug Reaction Reports Supports the Concept of a Crucial Role for 5-HT2B Receptor Agonism in Cardiac Valvular Fibrosis

@article{Hofmann2006LisurideAD,
  title={Lisuride, a Dopamine Receptor Agonist With 5-HT2B Receptor Antagonist Properties: Absence of Cardiac Valvulopathy Adverse Drug Reaction Reports Supports the Concept of a Crucial Role for 5-HT2B Receptor Agonism in Cardiac Valvular Fibrosis},
  author={Caroline Hofmann and U Penner and Rainer Dorow and Heinz H. Pertz and Sven J{\"a}hnichen and Reinhard Horowski and Klaus Peter Latt{\'e} and Dirk Palla and Bj{\"o}rn Schurad},
  journal={Clinical Neuropharmacology},
  year={2006},
  volume={29},
  pages={80-86}
}
Objectives: The high incidence of fibrotic cardiac valvulopathies reported in association with the 8&bgr;-ergoline dopamine (DA) agonist, pergolide, and also case reports for cabergoline and bromocriptine have made it necessary to review the theoretical basis and actual findings in the case of another DA agonist, the 8&agr;-ergoline lisuride (used since the 1970s for migraine prophylaxis as well as since the 1980s for its prolactin-lowering and anti-Parkinson activity). Methods: We have… Expand
Characterization of the Molecular Fragment That Is Responsible for Agonism of Pergolide at Serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A Receptors
TLDR
It is concluded that the N(6) propyl substituent of pergolide is crucial for 5-HT2B receptor agonism and thus a determinant of valvular regurgitation. Expand
The Bulky N(6) Substituent of Cabergoline Is Responsible for Agonism of This Drug at 5-Hydroxytryptamine (5-HT)2A and 5-HT2B Receptors and Thus Is a Determinant of Valvular Heart Disease
TLDR
It is concluded that the bulky N(6) substituent of cabergoline is responsible for 5- HT2AR and 5-HT2BR agonism and the increased ERK1/2 phosphorylation and production of extracellular matrix by Cabergoline are mediated by 5-ht2ARs. Expand
Transdermal delivery of dopamine receptor agonists.
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There is good evidence that once-daily patch usage provides patients with constant dopaminergic stimulation, and that patches are of equal potency to other oral non-ergot derivatives such as ropinirole and pramipexole. Expand
Serotonergic drugs and valvular heart disease
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A more likely cause of fenfluramines-induced valvulopathy is activation of 5-HT2B receptors on heart valves by the metabolite norfenfluramine, and future serotonergic medications should be designed to lack 5- HT2B agonist activity. Expand
Dopamine Agonists in Parkinson Disease : Special Focus on Pramipexole
S8 CONSULTANT SEPTEMBER 2008 (SUPPLEMENT) ABSTRACT: Dopamine receptor agonists have played an important role in antiparkinsonian therapy since the first ergoline derivative was introduced in 1974.Expand
Current and prospective pharmacological targets in relation to antimigraine action
TLDR
Pharmacological targets in migraine are discussed, with special emphasis on compounds acting on 5-HT (5-HT1–7), adrenergic (α1, α2, and β), cortisol, calcitonin gene-related peptide, adenosine, glutamate, NMDA, AMPA, kainate, and metabotropic receptors, dopamine, endothelin, and female hormone (estrogen and progesterone) receptors. Expand
Risk of heart failure following treatment with dopamine agonists in Parkinson's disease patients
TLDR
The pharmacodynamic and cardiovascular effects of DAs on PD patients are reviewed, and results showed higher heart failure risk following use of pramipexole or cabergoline. Expand
Structural determinants of 5-HT2B receptor activation and biased agonism
TLDR
Four crystal structures of a prototypical serotonin receptor 5-HT2BR in complex with chemically and pharmacologically diverse drugs elucidate the structural bases for receptor activation, agonist-mediated biased signaling and β-arrestin2 translocation. Expand
Dopamine agonists and valvular heart disease
TLDR
Dopamine agonist doses in prolactinoma therapy are 10-fold lower than those employed in Parkinson's disease, although occasionally dopamine agonist-resistant patients require higher doses, and the risk for valvulopathy appears low. Expand
Cardiovascular toxicity of novel psychoactive drugs: Lessons from the past
  • P. Dawson, J. Moffatt
  • Medicine, Psychology
  • Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2012
The long use of ephedrine, amphetamines, cocaine, LSD and more recently 3,4-methylenedioxy-N-methylamphetamine (MDMA; "Ecstasy") allows us to predict with some confidence what cardiovascular risksExpand
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It is suggested that alterations at both presynaptic and postsynaptic levels contributing to these motor complications tend to normalize with the more physiological stimulation afforded by continuous replacement strategies, especially when given chronically. Expand
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The results indicate, to a certain extent, that the relative risk for onset of dopamine agonist-related fibrotic syndromes is lower particularly for pramipexole and lisuride, which have been available for more years than pramipesxole. Expand
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