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Clinical Pharmacokinetics and Pharmacodynamics of Safinamide

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Abstract

The symptoms of Parkinson’s disease (PD) reflect disruptions of a number of brain neurotransmitter systems of varying type and degree. Pharmacological agents with multiple neurochemical mechanisms of action are therefore promising candidates for countering these problems and providing comprehensive symptomatic relief for patients. The pharmacological profile of safinamide includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent Na+ channels, modulation of Ca2+ channels, and inhibition of glutamate release. Safinamide is administered once daily at oral doses of 50–100 mg; it is well-tolerated and safe. Clinical trials have found that it ameliorates motor symptoms when added to established levodopa or single dopamine receptor agonist therapy. The future role of safinamide in PD may be that it enables a reduction in the dosage of dopamine replacement therapies, thereby reducing the adverse effects associated with these treatments. The clinical convenience (once-daily administration), safety, and tolerability of safinamide are better than those of dopamine receptor agonists. The introduction of safinamide reflects a change of approach to drug development for anti-parkinsonian agents in that its broad spectrum of action corresponds to the multiple heterogeneous alterations of brain neurochemistry in PD, rather than being targeted at a single receptor type or neurochemical process. Safinamide is a promising new instrument for the effective symptomatic therapy of PD.

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Authors and Affiliations

  1. Department of Neurology, St. Joseph Hospital Berlin-Weißensee, Gartenstr. 1, 13088, Berlin, Germany

    Thomas Müller & Paul Foley

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  1. Thomas Müller
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  2. Paul Foley
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Correspondence to Thomas Müller.

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No external funding was used in the preparation of this manuscript.

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Thomas Müller has received consulting fees for serving on the international advisory board of Zambon and received lecture fees from Zambon. Paul Foley has no conflicts of interest that might be relevant to the contents of this manuscript.

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Müller, T., Foley, P. Clinical Pharmacokinetics and Pharmacodynamics of Safinamide. Clin Pharmacokinet 56, 251–261 (2017). https://doi.org/10.1007/s40262-016-0449-5

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