Riluzole

Riluzole

Clinical data
Trade names	Rilutek, Teglutik
AHFS/Drugs.com	Monograph
MedlinePlus	a696013
License data	US FDA: Riluzole
Pregnancy category	AU: B3 US: C (Risk not ruled out)
Routes of administration	Oral
ATC code	N07XX02 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	60±18%
Protein binding	97%
Metabolism	Hepatic (CYP1A2)
Biological half-life	9-15 hours
Excretion	Urine (90%)
Identifiers
IUPAC name 6-(trifluoromethoxy)benzothiazol-2-amine
CAS Number	1744-22-5 Y
PubChem (CID)	5070
IUPHAR/BPS	2326
DrugBank	DB00740 Y
ChemSpider	4892 Y
UNII	7LJ087RS6F Y
KEGG	D00775 Y
ChEMBL	CHEMBL744 Y
ECHA InfoCard	100.124.754
Chemical and physical data
Formula	C8H5F3N2OS
Molar mass	234.199 g/mol
3D model (Jmol)	Interactive image
SMILES FC(F)(F)Oc1ccc2nc(sc2c1)N
InChI InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13) Y Key:FTALBRSUTCGOEG-UHFFFAOYSA-N Y

Riluzole (Rilutek, Teglutik) is a drug used to treat amyotrophic lateral sclerosis. These are marketed by Sanofi Pharmaceuticals and Martindale Pharma respectively. Riluzole delays the onset of ventilator-dependence or tracheostomy in selected patients and may increase survival by approximately two to three months.

Riluzole is available in tablet (Rilutek, riluzole) and liquid (Teglutik) form. The liquid formulation may be more suitable for patients with swallowing difficulties.

There has been some evidence to show that higher doses might produce more significant improvements in ALS patients but at almost £6 (US$10) per tablet it is at risk of being prohibitively expensive given the modest benefit to patients. One study in the Netherlands found that riluzole is metabolized differently by males and females, and its levels in plasma are decreased in patients who smoke cigarettes or take omeprazole. A Cochrane Library review states a 9% gain in the probability of surviving one year.

A number of recent case studies have indicated that riluzole may have clinical use in mood and anxiety disorders. It has been shown to have antidepressant properties in the treatment of refractory depression and act as an anxiolytic in obsessive-compulsive disorder and in generalized anxiety disorder.

A clinical study on mice has shown riluzole to compensate for harmful glutamate levels and promote dendritic spine clustering in hippocampal circuits implicated in memory and emotion. Therefore, the drug may act as an effective treatment for age-related memory loss and other forms of cognitive decline. The effect of riluzole on glutamate dysfunction in humans with Alzheimer's disease is unknown; however, a clinical trial is taking place to investigate this.