Pharmacologic class: Glutamate antagonist

Therapeutic class: Amyotrophic lateral sclerosis (ALS) agent

Pregnancy risk category C


Unknown. Thought to inhibit amino acid accumulation on motor neurons of CNS, improving nerve impulse transmission.


Tablets: 50 mg

Indications and dosages


Adults: 50 mg P.O. q 12 hours

Off-label uses

• Cervical dystonia

• Huntington's disease


• Hypersensitivity to drug or its components


Use cautiously in:

• hepatic or renal insufficiency, neutropenia, febrile illness

• elderly patients

• female patients and Japanese patients (may have decreased metabolic capacity to eliminate drug)

• pregnant or breastfeeding patients

• children.


• Give at least 1 hour before or 2 hours after a meal to maximize absorption.

Adverse reactions

CNS: headache, dizziness, drowsiness, asthenia, hypertonia, depression, insomnia, malaise, vertigo, circumoral paresthesia

CV: hypertension, orthostatic hypotension, tachycardia, palpitations, peripheral edema, phlebitis, cardiac arrest

EENT: rhinitis, sinusitis, oral candidiasis

GI: nausea, vomiting, diarrhea, abdominal pain, dyspepsia, flatulence, stomatitis, dry mouth, anorexia

GU: urinary tract infection, dysuria

Hematologic: neutropenia

Musculoskeletal: back pain, joint pain

Respiratory: decreased lung function, increased cough, pneumonia

Skin: pruritus, eczema, alopecia, exfoliative dermatitis

Other: tooth disorders, weight loss


Drug-drug. Allopurinol, methyldopa, sulfasalazine: increased risk of hepatotoxicity

CYP450-1A2 inducers (such as omeprazole, rifampin): increased riluzole elimination

CYP450-1A2 inhibitors (such as amitriptyline, phenacetin, quinolones, theophylline): decreased riluzole elimination

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, bilirubin, gamma-glutamyltransferase: increased levels

Drug-food. High-fat foods: decreased riluzole absorption

Drug-behaviors. Alcohol use: increased risk of hepatotoxicity

Patient monitoring

• Monitor liver function tests and CBC.

• Assess vital signs and cardiovascular status, particularly for hypertension, orthostatic hypotension, and peripheral edema.

• Closely monitor respiratory status for decreased lung function and pneumonia.

• Monitor weight, nutritional status, and hydration.

• Closely monitor females and patients of Japanese origin, who are at increased risk for adverse reactions.

Patient teaching

• Tell patient to take 1 hour before or 2 hours after a meal, at same time each day.

• Instruct patient to take his temperature regularly and report fever.

Teach patient to immediately report arm or leg swelling, difficulty breathing, and other signs of decreased lung function.

• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.

• Caution patient to avoid high-fat foods and alcohol.

• Instruct patient to move slowly when sitting up or standing, to avoid dizziness from sudden blood pressure decrease.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


(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.
Drug Guide, © 2015 Farlex and Partners

Riluzole (Rilutek)

The first drug approved in the United States for the treatment of ALS.
Gale Encyclopedia of Medicine. Copyright 2008 The Gale Group, Inc. All rights reserved.
References in periodicals archive ?
According to BioSpace, Sanofi (SNY) makes a drug to treat ALS by the name of Rilutek. It was the first drug approved by the FDA to treat ALS, but "it's no cure for ALS," though it can slow progression of the disease.
Based on the company's PharmFilm technology, the development of ROF included studies demonstrating its pharmacokinetic bioequivalence to the reference listed drug, Rilutek, as well as additional studies to assess patients' ability to swallow ROF.
The algorithm helps classify individual persons as having actual, potential, or non-ALS cases using variables including the International Classification of Diseases--Ninth Revision (ICD-9) diagnostic code for ALS, frequency of visits to neurologists, and use of prescription drugs (e.g., Rilutek) (8).
The only US Food and Drug Administration-approved disease-modifying medication is riluzole (Rilutek), an oral pill taken twice daily, which may slow ALS progression but only minimally increases survival time.
To date, there is no cure for the disease, although two FDA-approved medications, riluzole (Rilutek) and edaravone (Radicava), can slow its progression.
There currently are two FDA-approved drugs, riluzole (Rilutek) and edaravone (Radicava), that slow progression of the disease, while physical therapy can help strengthen unaffected muscles.
(34.) National Institute for Clinical Excellence Guidance on the use of riluzole (Rilutek) for the treatment of motor neurone disease London: NICE, 2001 20.
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.
RILUTEK is an NMDA receptor antagonist and has been shown to prolong life in patients with ALS by 3 months.
Emmanuelle Waubant, MD, PhD, and investigators at the University of California, San Francisco, are studying the possible nerve-protecting effects of oral riluzole (Rilutek) in people at high risk for MS or early MS, when combined with Avonex (interferon beta-1a).
This third edition is updated to reflect the latest research and treatment options, with new information on noninvasive ventilators, the use of riluzole (Rilutek), and new patient guidelines developed by the American Academy of Neurology.