Riluzole
RILUTEK
What it isGlutamate release inhibitor; amyotrophic lateral sclerosis.
Why this oneIt extends survival by a few months, and it was the first disease-modifying agent in ALS.
What limits itHepatotoxicity requires monthly liver tests initially. Take on an empty stomach; CYP1A2-dependent, so smoking lowers levels.
FDA-approved for
- ALS (1995)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Amyotrophic lateral sclerosis (ALS) | adult | 50 mg BID | 50 mg BID | 50 mg BID |
Renal Undefined
Hepatic Mild-moderate (Child-Pugh A/B): increased exposure, higher risk of adverse reactions; severe: unknown. Not recommended if baseline aminotransferases >5x ULN or evidence of liver dysfunction
Instructions
- Take at least 1 hour before or 2 hours after a meal
- Measure serum aminotransferases before and during treatment
Cautions
- Hepatic injury (drug-induced, some fatal); monitor ALT monthly x3 mo then periodically; not recommended if ALT >5x ULN; discontinue for liver dysfunction
- Neutropenia (ANC <500); advise reporting febrile illness
- Interstitial lung disease; discontinue if it develops
- Pancreatitis (postmarketing); discontinue if suspected
Adverse reactions
- Asthenia
- Nausea
- Dizziness
- Decreased lung function
- Abdominal pain
Pregnancy Based on animal data, may cause fetal harm
Lactation Unknown if excreted in human milk; detected in rat milk
NO BOXED WARNINGS
Principal riskHepatotoxicity needing monthly liver tests initially
Cost, est. cash$1,000–$20,000/month
Generic entry2003
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Riluzole ballicule
Open Riluzole in the interactive console ↗
Memory aids: mascots and interaction avatars
integrated augmentative communication wheelchair → ALS medication
