Products
Riluzole is commercially available in the form of film-coated tablets (Rilutek). It has been approved in many countries since 1996. In 2018, an additional oral suspension was registered (CH: Teglutik, USA: Tiglutik).
Structure and properties
Riluzole (C8H5F3N2OS, Mr = 234.2 g/mol) is a benzothiazole. It exists as a white to slightly yellow powder that is practically insoluble in water. Riluzole has an active metabolite (-hydroxyriluzole, RPR112512).
Effects
Riluzole (ATC N07XX02) has neuroprotective and antiglutamatergic properties. It may positively affect disease symptoms and prolong survival. Riluzole inhibits voltage-gated sodium channels at the presynaptic neuron, calcium influx, and glutamate release. The half-life ranges from 9 to 15 hours.
Indications
For the treatment of amyotrophic lateral sclerosis (ALS), a degenerative disease of the motor nervous system. Use in psychiatric disorders is discussed.
Dosage
According to the SmPC. Tablets are taken twice daily, 12 hours apart and fasting, that is, one hour before or two hours after a main meal.
Contraindications
Riluzole is contraindicated in hypersensitivity, liver disease, elevated transaminase levels, during pregnancy, and lactation. For complete precautions, see the drug label.
Interactions
Riluzole is metabolized by CYP1A2. CYP1A2 inhibitors and inducers may lead to drug-drug interactions.
Adverse effects
The most common potential adverse effects include weakness, nausea, increased ALT levels, headache, abdominal pain, pain, vomiting, dizziness, tachycardia, somnolence, and buccal paresthesias.
Trivia
In the TV series “Empire,” the protagonist and company founder Lucious Lyon, who suffers from ALS, is treated with riluzole.
