Pharmacokinetic drug evaluation of safinamide mesylate for the treatment of mid-to-late stage Parkinson's disease

Expert Opin Drug Metab Toxicol. 2017 Jun;13(6):693-699. doi: 10.1080/17425255.2017.1329418.

Abstract

Patients with Parkinson's disease suffer from a heterogeneous expression of neurotransmitter deficits. They cause an individual variable expression of motor and non-motor symptoms. Thus, drugs with various mechanisms of actions are suitable to counteract these disease related neurotransmitter alterations. Areas covered: This invited review suggests safinamide as an ideal compound for therapy of Parkinson's disease, as its pharmacological profile includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent sodium channels, modulation of calcium channels and abnormal glutamate release. Safinamide may provide benefits effects on non-motor symptoms in addition to the demonstrated amelioration of motor impairment in levodopa treated patients with Parkinson's disease. Safinamide was well tolerated and safe when administered in dose of 50 or 100 mg daily in pivotal trials. Expert opinion: Clinical handling, safety and tolerability of Safinamide are better than of dopamine agonists or levodopa. Safinamide supplements the existing armamentarium of drugs for Parkinson's disease. Safinamide will help to reduce dosing of levodopa but also of dopamine agonists during long term treatment in patients with Parkinson's disease.

Keywords: MAO-B inhibition; Parkinson’s disease; Safinamide; dopamine substitution; glutamate; glutamate release inhibition.

Publication types

  • Review

MeSH terms

  • Alanine / analogs & derivatives*
  • Alanine / pharmacokinetics
  • Alanine / pharmacology
  • Alanine / therapeutic use
  • Animals
  • Antiparkinson Agents / pharmacokinetics
  • Antiparkinson Agents / pharmacology
  • Antiparkinson Agents / therapeutic use*
  • Benzylamines / pharmacokinetics
  • Benzylamines / pharmacology
  • Benzylamines / therapeutic use*
  • Dopamine Agonists / administration & dosage
  • Dopamine Agonists / adverse effects
  • Dose-Response Relationship, Drug
  • Humans
  • Levodopa / administration & dosage
  • Levodopa / adverse effects
  • Monoamine Oxidase Inhibitors / pharmacokinetics
  • Monoamine Oxidase Inhibitors / pharmacology
  • Monoamine Oxidase Inhibitors / therapeutic use
  • Parkinson Disease / drug therapy*
  • Parkinson Disease / physiopathology

Substances

  • Antiparkinson Agents
  • Benzylamines
  • Dopamine Agonists
  • Monoamine Oxidase Inhibitors
  • Levodopa
  • safinamide
  • Alanine