Riluzole

Category: pharmacological

Aliases: Rilutek

Pharmacological Mechanism

Glutamate release inhibitor — blocks voltage-gated Na+ channels presynaptically + reduces glutamate-induced excitotoxicity. First FDA-approved drug for ALS; modest survival benefit (~3 months). CYP1A2 substrate.

Half-Life (t½)

PO: 12h

Dosing Guidelines

• PO: Typical 100 mg (Range: 50–100 mg)

Target Organ Systems

• nervous
• digestive

Pathways It Modulates

• Glutamate receptor pharmacology (inhibitor) — presynaptic glutamate release + Na+ channel block
• Metabotropic glutamate receptors (inhibitor) — ↓glutamate release; partial mGluR I modulation; ALS

Chemical Identifiers

• PubChem CID: 5070
• Formula: C8H5F3N2OS
• Molecular weight: 234.2 g/mol
• InChIKey: FTALBRSUTCGOEG-UHFFFAOYSA-N
• SMILES: C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N

References

• PMID 9549636