(ril-yoo-zole) ,


(trade name)


Therapeutic: agents amyotrophic lateral sclerosis
Pregnancy Category: C


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.

Therapeutic effects

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).

Time/action profile



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)
  • headache


  • decreased lung function (most frequent)
  • hypersensitivity pneumonitis
  • interstitial lung disease


  • hypertension
  • peripheral edema


  • hepatitis (life-threatening)
  • abdominal pain (most frequent)
  • nausea (most frequent)
  • anorexia
  • diarrhea
  • dyspepsia
  • flatulence
  • ↑ liver enzymes
  • vomiting


  • neutropenia


  • weight loss


  • arthralgia
  • back pain


  • circumoral paresthesia


Drug-Drug interaction

Effects 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

Nursing implications

Nursing assessment

  • 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 Diagnoses

Impaired physical mobility (Indications)
Diarrhea (Adverse Reactions)


  • Oral: Administer on an empty stomach 1 hr before or 2 hr after meals.

Patient/Family Teaching

  • 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.

Evaluation/Desired Outcomes

  • Extended survival or time to tracheostomy in ALS patients.

Riluzole (Rilutek)

The first drug approved in the United States for the treatment of ALS.
References in periodicals archive ?
However, the patent expiry of Rilutek could pose a challenge to the growth of this market.
WAY BACK in 2005, Kai Tiaki Nursing New Zealand published a letter about the Motor Neurone Disease (MND) Association lobbying Pharmac to consider subsidising Rilutek, also known as Riluzole.
Current treatment options are limited to off-label medications that offer symptomatic relief, and Rilutek (riluzole), the only approved disease-modifying treatment for ALS.
RILUTEK is an NMDA receptor antagonist and has been shown to prolong life in patients with ALS by 3 months.
Rilutek (riluzole) has demonstrated promise among ALS patients.
The cause is unknown and there is no cure though the drug Rilutek can slow the progression.
The Phase II clinical trial will evaluate the safety and efficacy of EHT 0201 as a potential treatment in addition to Rilutek (riluzole, Aventis) therapy for patients suffering from ALS.
Left in the dark to fight the disease, they have discovered there is one drug, Rilutek, that has shown to be of some benefit to people with MND.
We also focused on taxol (ovarian cancer), taxotere (breast cancer), irinotecan (bowel cancer), temodal (brain cancer), rilutek (motor neurone disease), beta interferon (multiple sclerosis) and aricept (Alzheimer's).
It will make it easier for doctors to assess the chances of success before prescribing expensive drugs such as Rebif for multiple sclerosis or Rilutek for motor neurone disease.
Rilutek could also be wonderful news for the millions of sufferers from Parkinson's Disease around the world.
The only FDA approved medicine is Rilutek which costs more than $700 a month and does not cure but just delays the end, thus prolonging the misery.