Riluzole — The Glutamate Modulator
Riluzole is a neuroprotective medication primarily used to delay disease progression in amyotrophic lateral sclerosis (ALS). While it is not a direct longevity therapeutic, its ability to modulate glutamate excitotoxicity and protect motor neurons makes it a critical intervention in neurodegenerative disease management.
Mechanism of Action
Riluzole acts primarily by inhibiting the release of glutamic acid from presynaptic nerve terminals and enhancing glutamate reuptake. It also inactivates voltage-dependent sodium channels, which reduces neuronal excitability. By dampening glutamatergic neurotransmission, riluzole mitigates excitotoxicity, a key driver of motor neuron death in ALS. Its neuroprotective effects may also involve the activation of small conductance calcium-activated potassium (SK) channels.
Human Trial Evidence
No published human longevity trials. Animal/in-vitro evidence only. In humans, riluzole is exclusively studied and approved for ALS, where large randomized controlled trials have shown it extends tracheostomy-free survival by approximately 2 to 3 months.
Dosing Protocol
The standard approved dose for ALS is 50 mg twice daily (100 mg/day total), taken orally on an empty stomach. Riluzole is a prescription-only medication. Dose-finding studies indicate that 100 mg/day offers the best benefit-to-risk ratio.
Safety & Contraindications
Common adverse effects include asthenia (weakness), nausea, dizziness, and decreased lung function. Riluzole can cause dose-related elevations in liver transaminases (ALT); regular monitoring of liver function is required. It is contraindicated in patients with a history of severe hypersensitivity to the drug or significant hepatic impairment. Prescription required.