Generic
Riluzole
3 brands available in the market
At a glance
Riluzole is a glutamate inhibitor used to slow disease progression and prolong survival in patients with amyotrophic lateral sclerosis (ALS). It inhibits glutamate release, inactivates voltage-dependent Na channels, and interferes with intracellular events following transmitter binding at excitatory amino acid receptors.
Description
The mode of action of riluzole is not fully known. Its pharmacological properties include inhibitory effect on glutamate release, inactivation of voltage-dependent sodium channels, and ability to interfere with intracellular events following transmitter binding at excitatory amino acid receptors. It is neuroprotective and exhibits anticonvulsant and myorelaxant properties in animal models.
Indications
- Amyotrophic lateral sclerosis (ALS) - to extend life or delay time to mechanical ventilation
Therapeutic class
Neurodegenerative Disease Drugs / Neuromuscular Disorder Drugs
Pharmacological class
Glutamate Inhibitor (Neuroprotective)
Pharmacology
Riluzole inhibits glutamate release, inactivates voltage-dependent Na channels, and interferes with intracellular events following transmitter binding at excitatory amino acid receptors. It is neuroprotective and exhibits anticonvulsant and myorelaxant properties in animal models.
Mechanism of action
Reduces neuronal damage by inhibiting glutamate release and inactivating sodium channels.
Dosage
Adult Dose (Oral):
- ALS: 50 mg twice daily
- Take at least 1 hour before or 2 hours after meals
- Discontinue if ALT levels increase to 5 times ULN
- Hepatic impairment (mild-moderate): Increased AUC; risk of adverse reactions
- Severe hepatic impairment: Unknown; not recommended
Administration
- Take on an empty stomach (1 hour before or 2 hours after meals)
- Avoid high-fat meals
- Take at the same time each day
- Swallow tablet whole
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Weakness
- Headache
- Dizziness
- Nausea
- Abdominal pain
- Diarrhea
- Decreased pulmonary function
- Paresthesia
- Sleepiness
- Tachycardia
- Abnormal liver function tests
Precautions & warnings
- Monitor liver function; measure ALT before and during therapy; monthly for first 3 months, then every 3 months
- Smoking reduces riluzole efficacy; quit smoking
- May affect driving ability; do not drive if dizziness or vertigo occurs
- Neutropenia: Report febrile illness; discontinue if neutropenia occurs
- Interstitial lung disease: Discontinue if occurs
Contraindications
- Hypersensitivity to riluzole or any excipient
- Hepatic disease or baseline transaminases >3 times ULN
- Pregnancy and lactation
Drug interactions
- CYP1A2 inhibitors (caffeine, ciprofloxacin, oral contraceptives): Decreased rate of elimination
- CYP1A2 inducers (rifampicin, omeprazole, cigarette smoke): Increased rate of elimination
- Hepatotoxic drugs (allopurinol, methyldopa, sulfasalazine): Increased risk of hepatotoxicity
Food interactions
Caution is advised when consuming alcohol with Riluzole.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects; consult your doctor; contraindicated in pregnancy.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited human data suggests drug may pass into breast milk; contraindicated in breastfeeding.
Pediatric use
Not recommended for use in pediatric population.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Limited information on use in kidney disease; not recommended in impaired renal function; consult your doctor.
Hepatic Impairment: Caution in liver disease; do not use if baseline transaminases >3x ULN; discontinue if ALT >5x ULN; consult your doctor.
Overdose effects
No overdose information available; consult your doctor if taken in excess.
Storage conditions
Store in a cool and dry place, protected from light; do not store above 30°C.
Chemical structure
Riluzole