Pregnancy Category: C
ClassificationTherapeutic: agents amyotrophic lateral sclerosis
Treatment of patients with amyotrophic lateral sclerosis (ALS).
Action may be related to: :
- Inhibition of glutamate release,
- Inactivation of sodium channels or,
- Interference with neurotransmitter binding at receptor sites.
Extended survival or time to tracheostomy in ALS patients.
Absorption: Well absorbed (90%) after oral administration, but bioavailability is 50%.
Distribution: Readily penetrates brain.
Protein Binding: 96%.
Metabolism and Excretion: Highly metabolized by the liver (some metabolites are pharmacologically active); 2% excreted unchanged in urine.
Half-life: 12 hr (after multiple doses).
Contraindicated in: Severe hypersensitivity.
Use Cautiously in: Hepatic or renal impairment; Female patients (↓ metabolism); Obstetric / Lactation / Pediatric: Safety not established.
Adverse Reactions/Side Effects
Central nervous system
- dizziness (most frequent)
- weakness (most frequent)
- decreased lung function (most frequent)
- hypersensitivity pneumonitis
- interstitial lung disease
- peripheral edema
- hepatitis (life-threatening)
- abdominal pain (most frequent)
- nausea (most frequent)
- ↑ liver enzymes
- weight loss
- back pain
- circumoral paresthesia
Drug-Drug interactionEffects may be ↑ by amitriptyline, caffeine, fluoroquinolones, or theophylline.Effects may be ↓ by cigarette smoke (nicotine ), rifampin, or omeprazole.St. John's wort may ↓ levels and effectiveness.Effects may be ↓ by charcoal-broiled foods.High-fat meals ↓ absorption.
Oral (Adults) 50 mg q 12 hr.
Availability (generic available)
Tablets: 50 mg
- Assess patient for aggravation reaction causing worsening of ALS symptoms (unusual tiredness or weakness, spasticity, diarrhea, nausea, vomiting). May require dose reduction.
- Lab Test Considerations: Monitor AST, ALT, serum bilirubin, and GGT before and during therapy. Monitor serum ALT monthly for the first 3 mo, every 3 mo for the 1st yr, and periodically thereafter. Discontinue treatment if ALT is >5 times the upper limit of normal or if clinical jaundice develops.
- Monitor WBC in patients with febrile illness.
Potential Nursing DiagnosesImpaired physical mobility (Indications)
Diarrhea (Adverse Reactions)
- Oral: Administer on an empty stomach 1 hr before or 2 hr after meals.
- Instruct patient to take riluzole as directed at the same time each day on an empty stomach. Missed doses should be omitted; start again at next scheduled dose. Do not increase or double doses. Higher doses do not increase effectiveness but increase the incidence of side effects.
- May cause drowsiness or dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
- Advise patient to avoid drinking alcohol while taking riluzole.
- Instruct patient to notify health care professional of any febrile illnesses.
- Extended survival or time to tracheostomy in ALS patients.
The first drug approved in the United States for the treatment of ALS.
Mentioned in: Amyotrophic Lateral Sclerosis