Riluzole tablet is indicated to extend life or delay the need for mechanical ventilation in patients with amyotrophic lateral sclerosis (ALS).

The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not fully understood, although several hypotheses exist. One theory suggests that motor neurons become vulnerable due to genetic predisposition or environmental factors and are damaged by glutamate toxicity. In some familial ALS cases, defects in the enzyme superoxide dismutase have been identified.

The exact mechanism of action of Riluzole is not fully known. Its pharmacological effects include:

• inhibition of glutamate release
• inactivation of voltage-dependent sodium channels
• interference with intracellular processes following excitatory amino acid receptor activation

Riluzole has shown neuroprotective effects in experimental models of neuronal injury involving excitotoxicity. It also protected cultured motor neurons from glutamate-induced toxicity and prevented cortical neuron death induced by anoxia. In animal studies, it demonstrated myorelaxant, sedative, and anticonvulsant properties at higher doses.

The recommended daily dose of Riluzole tablet in adults or older people is 100 mg (50 mg tablet every 12 hours).
Riluzole tablet should be taken at least one hour before, or two hours after a meal, to avoid a decrease in Riluzole bioavailability.

Paediatric use: Riluzole is not recommended for use in paediatric population.

No clinical studies have been conducted to evaluate interactions of riluzole with other medicinal products. In vitro studies suggest that CYP1A2 is the main enzyme involved in the oxidative metabolism of riluzole. CYP1A2 inhibitors (e.g. caffeine, diclofenac, diazepam, fluvoxamine, theophylline, amitriptyline, quinolones, etc.) may decrease riluzole elimination, leading to increased drug levels. CYP1A2 inducers (e.g. cigarette smoke, charcoal-grilled food, rifampicin, omeprazole) may increase riluzole elimination, reducing its effect.

Hypersensitivity to riluzole or any excipients. Hepatic disease or baseline transaminase levels greater than 3 times the upper limit of normal.

Common side effects include nausea, abnormal liver function tests, asthenia, headache, dizziness, oral paraesthesia, somnolence, tachycardia, diarrhoea, abdominal pain, vomiting, anaemia, allergic reactions, angioedema, pancreatitis, and interstitial lung disease.

Riluzole is contraindicated during pregnancy and breastfeeding.

Liver impairment: Riluzole should be used with caution in patients with a history of abnormal liver function or mildly elevated liver enzymes (ALT/SGPT, AST/SGOT up to 3× ULN), bilirubin, or GGT levels. Patients with significant baseline liver test abnormalities, especially elevated bilirubin, should not receive riluzole.

Due to the risk of hepatitis, liver enzymes including ALT must be checked before starting treatment and during therapy. ALT should be monitored monthly for the first 3 months, every 3 months for the rest of the first year, and periodically thereafter. More frequent monitoring is required if ALT becomes elevated. Riluzole should be discontinued if ALT increases to 5 times the upper limit of normal.

Renal impairment: Riluzole is not recommended in patients with impaired kidney function. Patients should report any fever promptly; treatment should be stopped if neutropenia occurs.

Interstitial lung disease: Cases have been reported in patients receiving riluzole. If interstitial lung disease develops, the drug must be discontinued immediately.

Effects on ability to drive and use machines: Patients should be warned about dizziness or vertigo and advised not to drive or operate machinery if these symptoms occur.

Neurodegenerative Disease Drugs / Neuromuscular Disorder Drugs

Store in a cool, dry place, protected from light. Do not store above 30°C.