Understanding Lamotrigine's Role in the CNS and Possible Future Evolution

Int J Mol Sci. 2023 Mar 23;24(7):6050. doi: 10.3390/ijms24076050.

Abstract

The anti-epileptic drug lamotrigine (LTG) has been widely used to treat various neurological disorders, including epilepsy and bipolar disorder. However, its precise mechanism of action in the central nervous system (CNS) still needs to be determined. Recent studies have highlighted the involvement of LTG in modulating the activity of voltage-gated ion channels, particularly those related to the inhibition of neuronal excitability. Additionally, LTG has been found to have neuroprotective effects, potentially through the inhibition of glutamate release and the enhancement of GABAergic neurotransmission. LTG's unique mechanism of action compared to other anti-epileptic drugs has led to the investigation of its use in treating other CNS disorders, such as neuropathic pain, PTSD, and major depressive disorder. Furthermore, the drug has been combined with other anti-epileptic drugs and mood stabilizers, which may enhance its therapeutic effects. In conclusion, LTG's potential to modulate multiple neurotransmitters and ion channels in the CNS makes it a promising drug for treating various neurological disorders. As our understanding of its mechanism of action in the CNS continues to evolve, the potential for the drug to be used in new indications will also be explored.

Keywords: GABAergic neurotransmission; LTG; anti-epileptic drugs; cancer research; central nervous system.

Publication types

  • Review

MeSH terms

  • Anticonvulsants / pharmacology
  • Anticonvulsants / therapeutic use
  • Central Nervous System
  • Depressive Disorder, Major* / drug therapy
  • Epilepsy* / drug therapy
  • Glutamic Acid
  • Humans
  • Ion Channels
  • Lamotrigine / therapeutic use
  • Triazines / pharmacology
  • Triazines / therapeutic use

Substances

  • Lamotrigine
  • Anticonvulsants
  • Glutamic Acid
  • Ion Channels
  • Triazines

Grants and funding

This research was financed by Fundo Europeu de Desenvolvimento Regional (FEDER) funds through the COMPETE 2020 Operational Program for Competitiveness and Internationalization (POCI), Portugal 2020, and by Portuguese funds through Fundação para a Ciência e a Tecnologia (FCT) in the framework of projects IF/00092/2014/CP1255/CT0004 and CHAIR in Onco-Innovation from the Faculty of Medicine, University of Porto (FMUP).