Safinamide: an add-on treatment for managing Parkinson's disease.
Thomas Müller
- Vol. 10, pp 31-41
TLDR
Savinamide is discussed as an add-on therapeutic agent in orally levodopa-treated patients with “OFF” phenomena and a promising, future option will be combination of safinamide and opicapone in one formulation.Abstract:
Heterogeneous expression of neurotransmitter deficits results from onset and progression of Parkinson's disease. Intervals, characterized by reappearance of motor and associated certain nonmotor symptoms, determine the end of good tolerability and efficacy of oral levodopa therapy. These "OFF" states result from levodopa pharmacokinetics and disease progression-related deterioration of the central buffering capacity for fluctuations of dopamine levels. This review discusses safinamide as an add-on therapeutic agent in orally levodopa-treated patients with "OFF" phenomena. Safinamide provided beneficial effects on "OFF" symptoms in pivotal trials with doses of 50 or 100 mg once daily. Safinamide reversibly inhibits mono-amine oxidase B and declines abnormal glutamate release by modulation of potassium- and sodium ion channels. An ideal candidate for combination with safinamide is opicapone. This inhibitor of peripheral catechol-O-methyltransferase supports continuous brain delivery of levodopa and, thus, the continuous dopaminergic stimulation concept. Both compounds with their once-daily application and good tolerability may complement each other by reduction of necessary oral levodopa intakes and "OFF" times. Thus, a promising, future option will be combination of safinamide and opicapone in one formulation. It will reduce adherence issues and may complement levodopa treatment. It will probably cause less nausea and edema than a dopamine agonist/levodopa regimen.read more
Citations
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Journal ArticleDOI
Levodopa Equivalent Dose Conversion Factors: An Updated Proposal Including Opicapone and Safinamide.
TL;DR: The proposed LED conversion factors for opicapone and safinamide fit reasonably well into the previous scheme of conversion factors and still sufficiently reflect the potential of both drugs, but they follow the same limitations as the previous proposals.
Journal ArticleDOI
Long-Term Efficacy of Safinamide on Symptoms Severity and Quality of Life in Fluctuating Parkinson's Disease Patients
TL;DR: Savinamide, administered as add-on to standard therapy in fluctuating PD patients, significantly improved motor symptoms and clinical fluctuations in the overall population and in some subgroups of patients, and safinamide improved quality of life and activities of daily living.
Journal ArticleDOI
Pharmacokinetics and pharmacodynamics of levodopa/carbidopa cotherapies for Parkinson's disease
TL;DR: Long-term levodopa/dopa decarboxylase inhibitor application with concomitant inhibition of both, catechol-O-methyltransferase and monoamine oxidase-B supports a more continuous dopamine substitution, which ameliorates fluctuations of motor behavior.
Journal ArticleDOI
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
TL;DR: Propargylamine-derived multi-target directed ligands, such as ladostigil, M30, ASS234 and contilisant, involve different pathways and show improvement of cognitive impairment, antioxidant activities, enhancement of iron-chelating activities, protect against tau hyperphosphorylation, block metal-associated oxidative stress, regulate APP and Aβ expression processing by the non-amyloidogenic α-secretase pathway, suppress mitochondrial permeability transition pore opening, and coordinate protein kinase C signaling and Bcl-2 family proteins as mentioned in this paper.
Journal ArticleDOI
Safinamide Improves Non-Motor Symptoms Burden in Parkinson's Disease: An Open-Label Prospective Study.
Diego Santos García,Carmen Labandeira Guerra,Rosa Yáñez Baña,Maria Icíar Cimas Hernando,Iria Cabo López,Jose Manuel Paz Gonález,Maria Gemma Alonso Losada,Maria José Gonzalez Palmás,Cristina Martínez Miró +8 more
TL;DR: The SAFINONMOTOR study as discussed by the authors, an open-label study of the effectiveness of safinamide on non-motor symptoms in Parkinson's disease patients, was conducted in five centers from Spain and the primary efficacy outcome was the change from baseline (V1) to the end of the observational period (6 months) (V4) in the NMSS) total score.
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