Treatment with Dimethyl Fumarate Enhances Cholinergic Transmission in Multiple Sclerosis

CNS Drugs. 2019 Nov;33(11):1133-1139. doi: 10.1007/s40263-019-00676-6.

Abstract

Background: Dimethyl fumarate (DMF) exerts anti-inflammatory effects in multiple sclerosis by activating the Nrf2 antioxidant pathway, which is also stimulated by acetylcholine via alpha-7 nicotinic acetylcholine receptors. In animal models, Nrf2 potentiates cholinergic synaptic plasticity.

Objective: The aim of this study was to test whether treatment with DMF modulates cholinergic pathways in relapsing-remitting multiple sclerosis (RRMS).

Methods: Patients starting DMF (20) or IFN-β 1a (20) and healthy subjects (20) were enrolled. Short-latency afferent inhibition (SAI), which is a transcranial stimulation measure of central cholinergic transmission, was recorded in patients and controls at baseline and, in patients only, after 6 months of treatment. Patients treated with DMF also underwent autonomic function testing to further explore peripheral and central cholinergic tone.

Results: At baseline, SAI was similar in patients and in controls (p = 0.983). Treatment with DMF significantly increased SAI (p = 0.01), while IFNβ had no effect (p = 0.80). In the cold face test, DMF treatment also increased reflex bradycardia (p = 0.013), and reduced diastolic blood pressure variation (p = 0.010), further indicating its ability to stimulate cholinergic transmission.

Conclusions: Treatment of MS patients with DMF results in increased cholinergic stimulation, with possible implications for neuroinflammation and neuroprotection.

MeSH terms

  • Acetylcholine / therapeutic use*
  • Adult
  • Cholinergic Agents / therapeutic use*
  • Dimethyl Fumarate / therapeutic use*
  • Female
  • Humans
  • Immunosuppressive Agents / therapeutic use*
  • Interferon-beta / metabolism
  • Male
  • Multiple Sclerosis, Relapsing-Remitting / drug therapy*
  • Multiple Sclerosis, Relapsing-Remitting / metabolism
  • NF-E2-Related Factor 2 / metabolism
  • Treatment Outcome

Substances

  • Cholinergic Agents
  • Immunosuppressive Agents
  • NF-E2-Related Factor 2
  • Interferon-beta
  • Dimethyl Fumarate
  • Acetylcholine