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.


(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 ?
Biopharmaceutical company Biohaven Pharmaceutical Holding Company Ltd (NYSE:BHVN) and its wholly owned subsidiary Biohaven Pharmaceuticals Inc, on Friday jointly announced the treatment of the first subject to demonstrate the pharmacokinetic equivalence of sublingual BHV-0223 compared to Rilutek (riluzole) as a potential treatment for Amyotrophic Lateral Sclerosis (ALS) under a bioequivalence study.
5 mg, 5 mg Tablets Voriconazole For Oral Suspension, Wend for Oral 40 mg/ml Suspension JUNE 2013 RiluzoleTablets, 50 mg Rilutek Tablets RiluzoleTablets USP, 50 mg Rilutek Tablets RiluzoleTablets LISP, 50 mg Rilutek Tablets JULY 20 Rasagiline MesylateTablets, Azilect Tablets 0.
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.
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.