Safinamide

Products

Safinamide is commercially available in the form of film-coated tablets (Xadago). It was approved in many countries and in the EU in 2015 and in the US in 2017.

Structure and properties

Safinamide (C17H19FN2O2, Mr = 302.3 g/mol) is an α-aminoamide derivative.

Effects

Safinamide (ATC N04BD03) has indirect dopaminergic properties. It is a selective and reversible inhibitor of monoaminooxidase-B, increasing extracellular concentrations of dopamine in the striatum. Safinamide additionally inhibits voltage-gated sodium channels and stimulated glutamate release. The half-life ranges from 20 to 26 hours.

Indications

For the treatment of patients with idiopathic Parkinson’s disease as add-on therapy to a stable dose of levodopa alone or in combination with other Parkinson’s drugs in mid- to late-stage patients with fluctuations.

Dosage

According to the SmPC. Tablets are taken once daily, independent of meals. Treatment is started gradually.

Contraindications

  • Hypersensitivity
  • Concurrent treatment with an MAO inhibitor or pethidine.
  • Severe impairment of liver function
  • Patients with albinism, retinal degeneration, uveitis, hereditary retinopathy, or severe progressive diabetic retinopathy

Full details of precautions and interactions can be found in the drug label.

Interactions

Safinamide, as an MAO inhibitor, may cause several drug-drug interactions.

Adverse effects

The most common possible adverse effects include movement disorders, drowsiness, dizziness, headache, insomnia, nausea, and low blood pressure.