Factors associated with motor fluctuations and dyskinesia in Parkinson disease: Potential role of a new melevodopa plus Carbidopa formulation (Sirio)

Fabrizio Stocchi, Stefano Marconi

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Parkinson disease is a progressive movement disorder caused by loss of dopaminergic neurons in the substantia nigra. Of unknown etiology, Parkinson disease is characterized by 4 cardinal symptoms: tremor at rest, bradykinesia, postural instability, and rigidity. The current criterion-standard drug used in the management of parkinsonian symptoms is levodopa (l-dopa). However, long-term l-dopa therapy is associated with the development of motor complications; approximately 50% to 80% of patients will develop motor complications within 5 to 10 years of l-dopa treatment initiation. Motor complications can be divided into motor fluctuations, caused largely through pulsatile dopamine stimulation and low l-dopa concentrations, and dyskinesia, associated more often with peak l-dopa concentrations. Ultimately, the main goal was to provide steady l-dopa concentrations, without peaks and troughs. Empirical investigations using parenteral infusions of l-dopa and highly soluble l-dopa prodrugs have shown that there is benefit in ameliorating the peaks and troughs associated with traditional oral l-dopa formulations. Recently, the development of highly soluble oral l-dopa prodrugs has facilitated rapid, regular, and reliable l-dopa availability. This review evaluates some of the pharmacologic strategies in the management of motor complications in Parkinson disease and therapy optimization, with a focus on the use of CHF 1512 (Sirio), a combination of melevodopa (l-dopa methylester, a highly soluble prodrug of l-dopa) plus carbidopa in an effervescent tablet formulation.

Original languageEnglish
Pages (from-to)198-203
Number of pages6
JournalClinical Neuropharmacology
Volume33
Issue number4
DOIs
Publication statusPublished - Jul 2010

Fingerprint

Carbidopa
Dyskinesias
Levodopa
Parkinson Disease
Prodrugs
levodopa methyl ester
sirio
Parenteral Infusions
Hypokinesia
Dopaminergic Neurons
Movement Disorders
Tremor
Substantia Nigra
Tablets
Dopamine

Keywords

  • dyskinesia
  • latency to B "on"
  • melevodopa
  • motor complication

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology
  • Clinical Neurology

Cite this

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