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Riluzole

Antiglutamatergic · Amyotrophic Lateral Sclerosis (ALS) agent

AntiglutamatergicAmyotrophic Lateral Sclerosis (ALS) agent
CDSCO approvedSchedule H
EXCRETION
—
not curated
INTERACTIONS
5 major
SEVERE in our sources
PREGNANCY
l BREAST FEEDING
FDA category + note
Top interactionssee all 5 →
  • LeflunomideSevereDatabaseDDInter
  • LomitapideSevereDatabaseDDInter
  • MipomersenSevereDatabaseDDInter
  • PexidartinibSevereDatabaseDDInter

Mechanism

Riluzole is thought to exert its effects primarily by inhibiting glutamatergic transmission in the central nervous system. It is also believed to act by stabilizing the inactivated state of voltage-dependent sodium channels. Additionally, Riluzole inhibits Cav 2.2 (N-type) calcium channels, which play a role in neurotransmitter release.

Indications

Amyotrophic lateral sclerosis (to extend life or to extend the time to mechanical ventilation)Amyotrophic lateral sclerosis (ALS)

Dosing

Adult
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Pharmacokinetics

Half-life
approximately 12 h
Bioavailability
64 (30–100)%
Protein binding
Highly protein bound
Metabolism
Extensive metabolism in the liver by CYP-mediated hydroxylation and glucuronidation
Excretion
<1%

Side effects

Common
nauseadiarrhea
Serious
  • hepatic injury with elevations of serum transaminases

Pregnancy & lactation

Pregnancy

l BREAST FEEDING

Drug interactions

Leflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Lomitapide
Severe
Database

Clinical effect not specified

Source: DDInter

Mipomersen
Severe
Database

Clinical effect not specified

Source: DDInter

Pexidartinib
Severe
Database

Clinical effect not specified

Source: DDInter

Teriflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

7 additional unreviewed or low-confidence interactions hidden because their provenance or source detail is insufficient.

Related guidelines

Venous thromboembolism prophylaxis
ASH · Haematology · 2018

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Textbook-sourced·Sources: Goodman & Gilman 14e, BNF·Updated: 2026-05-13