Riluzole is a medication used to treat amyotrophic lateral sclerosis (ALS) and other motor neuron diseases. Riluzole delays the onset of ventilator-dependence or tracheostomy in some people and may increase survival by two to three months.
Medical uses
Amyotrophic lateral sclerosis
Riluzole was approved in the United States for the treatment of ALS by the US Food and Drug Administration (FDA) in 1995.
In 1996, riluzole was approved for use in treating ALS by the European Medicines Agency (EMA).
A
Cochrane Library review states a 9% gain in the probability of surviving one year.
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Contraindications
Contraindications for riluzole include: known prior hypersensitivity to riluzole or any of the excipients inside the preparations, liver disease, pregnancy or lactation.
Adverse effects
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Very common (>10% frequency):
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Common (1–10% frequency):
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Uncommon (0.1–1% frequency):
[ pancreatitis; interstitial lung disease
]
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Rare (<0.1% frequency):
[ neutropenia; allergic reaction (including angiooedema, anaphylactoid reaction)
]
Overdose
Symptoms of overdose include: neurological and psychiatric symptoms, acute toxic encephalopathy with stupor, coma and methemoglobinemia.[ Severe methemoglobinemia may be rapidly reversible after treatment with methylene blue.][
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Interactions
CYP1A2 substrates, inhibitors and inducers would probably interact with riluzole, due its dependency on this cytochrome for metabolism.[
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Mechanism of action
Riluzole preferentially blocks Tetrodotoxin-sensitive , which are associated with damaged .
Synthesis
Riluzole can be prepared beginning with the reaction of 4-(trifluoromethoxy)aniline with potassium thiocyanate followed by reaction with bromine, forming the thiazole ring.[; ]
Society and culture
Legal status
Riluzole was approved for medical use in the European Union in October 1996.
Research
A number of Case study and randomized controlled trials have indicated that riluzole, which is Neuroprotection and a glutamate modulator, may have use in Mood disorder and .
Riluzole has been investigated in rodent models for its potential ability to protect against noise-induced hearing loss (NIHL) and cisplatin-induced . These protective effects are believed to be caused by riluzole's antioxidant and anti-apoptotic properties, but other mechanisms, including modulation of glutamate signaling, are also being investigated.
A sublingual reformulation of riluzole that originated at Yale University and is known by the code name BHV-0223
