Pharmacology · Neuroprotective agents for ALS
Riluzole !
The first drug shown to prolong life in ALS, by a few months. It reduces glutamate signalling; liver tests are checked.
Updated 2026-11-01
Mechanism of action
Riluzole is a benzothiazole with several actions: it inhibits glutamate release, blocks NMDA- and kainate-type glutamate receptors and inhibits voltage-gated sodium channels. Reducing glutamate excitotoxicity is thought to slow motor neuron death, but the exact mechanism of benefit in ALS is unknown.
- Riluzole blocks sodium channels on nerve terminals
- Glutamate release falls; glutamate receptors are partly blocked
- Motor neurons face less excitotoxic stress
- Survival is extended by a few months
Pharmacokinetics
- Absorption
- Absorbed by mouth; a high-fat meal lowers absorption, so it is given apart from meals
- Distribution
- Highly protein bound
- Metabolism
- Extensive liver metabolism, mainly CYP1A2, then glucuronidation
- Half-life
- About 12 hours
Indications
- Amyotrophic lateral sclerosis Amyotrophic lateral sclerosis →
Adverse effects
Common
- Weakness and fatigue
- Nausea, diarrhoea, abdominal pain
- Dizziness and somnolence
Contraindications
- History of severe hypersensitivity to riluzole
Key interactions
- Ciprofloxacin and other strong or moderate CYP1A2 inhibitors
- More riluzole adverse effects
- Strong or moderate CYP1A2 inducers
- Lower levels and possibly less effect
- Other liver-toxic drugs
- Added risk of liver injury
What is monitored
- Serum aminotransferases before and regularly during treatment; it is stopped if liver dysfunction appears
- Blood count if fever occurs (neutropenia)
- Cough or breathlessness (interstitial lung disease)
Administration and safety
- Given at least an hour before or two hours after a meal
- Tablets, oral suspension and oral film exist; the suspension is shaken well; the film dissolves on the tongue
- Liquid forms help patients with swallowing problems
Nursing care
- Check that liver tests are scheduled
- Teach to report fever, jaundice, dark urine or cough
- Assess swallowing and choose the right formulation
- Explain that it slows ALS but does not reverse weakness
Pregnancy and breastfeeding
There are no studies in pregnant women and the risk is not known.
Test yourself
Think of the answer, then tap the question to see it.
Which disease is riluzole used for, and what benefit has it shown?
Amyotrophic lateral sclerosis; it prolongs survival by a few months.
Which neurotransmitter does riluzole reduce?
Glutamate (it inhibits release, blocks glutamate receptors and sodium channels).
Which laboratory tests are followed with riluzole?
Liver aminotransferases; and a blood count if fever suggests neutropenia.
Related drugs
Related conditions
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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - RILUZOLE tablet (DailyMed (U.S. National Library of Medicine), 2026); Riluzole: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2022); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 21 (McGraw Hill, 2023).
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Representative model, for educational purposes only.