Riluzole

Riluzole: A Key Player in the Management of Motor Neuron Disease
Definition:
Riluzole is a neuroprotective medication primarily used in the treatment of amyotrophic lateral sclerosis (ALS), a progressive neurodegenerative disease that affects motor neurons in the brain and spinal cord. Approved by the FDA in 1995, it is the first drug shown to extend survival and time to tracheostomy in ALS patients.
Mechanism of Action:
Riluzole’s pharmacological effects are attributed to its ability to modulate glutamatergic neurotransmission, which is crucial in neurodegeneration. The drug works through several mechanisms:
- Inhibition of Glutamate Release: Riluzole reduces the release of glutamate, an excitatory neurotransmitter that, when present in excess, can lead to excitotoxicity and neuronal damage. This is achieved by blocking voltage-dependent sodium channels and inhibiting presynaptic glutamate release14.
- Enhanced Glutamate Uptake: The drug promotes the uptake of glutamate by astrocytes, thereby decreasing its concentration in the synaptic cleft and reducing excitotoxicity2.
- Neuroprotective Properties: Riluzole has been shown to protect neurons from anoxic damage and other toxic insults, contributing to its neuroprotective effects3.
- Modulation of Ion Channels: The drug also affects various ion channels, including calcium and potassium channels, which play roles in neuronal excitability and neurotransmission34.
Clinical Implications:
Riluzole has demonstrated efficacy in slowing disease progression in ALS, with studies indicating that it can extend survival by several months. Its use is generally well-tolerated, with common side effects including fatigue, nausea, and liver enzyme elevations. Monitoring liver function is essential due to potential hepatotoxicity associated with prolonged use45.
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References
- The pharmacology and mechanism of action of riluzole
DOI: 10.1212/WNL.47.6_Suppl_4.233S
This article provides an overview of riluzole’s pharmacological properties and its mechanisms of action in the central nervous system. - Riluzole: A neuroprotective drug with potential as a novel anti-cancer agent
DOI: 10.3892/ijo.2021.5275
This review discusses riluzole’s neuroprotective qualities and its potential applications beyond ALS treatment. - A review of the neural mechanisms of action and clinical efficacy of riluzole
DOI: 10.1002/mds.27745
This review evaluates the various neural mechanisms through which riluzole exerts its effects and its clinical implications for ALS patients. - Riluzole – Wikipedia
DOI: 10.1016/j.jpsychores.2020.110188
This entry provides detailed information on riluzole’s pharmacodynamics, indications, contraindications, and side effects. - Pharmacological interventions for amyotrophic lateral sclerosis: Riluzole and beyond
DOI: 10.1016/j.nbd.2020.104678
This article reviews current pharmacological treatments for ALS, focusing on riluzole and emerging therapies aimed at improving patient outcomes.