riluzole

riluzole /ril·u·zole/ (ril´u-zōl) a compound used to prolong survival time in the treatment of amyotrophic lateral sclerosis.

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Riluzole (Rilutek)

The first drug approved in the United States for the treatment of ALS.

Mentioned in: Amyotrophic Lateral Sclerosis

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riluzole,

a glutamate antagonist.

indication This drug is used to treat amyotropic lateral sclerosis.

contraindication Known hypersensitivity to this drug prohibits its use.

adverse effects Neutropenia and exfoliative dermatitis are life-threatening effects. Other adverse effects are nausea, vomiting, dyspepsia, anorexia, diarrhea, flatulence, stomatitis, dry mouth, hypertonia, depression, dizziness, insomnia, somnolence, vertigo, pruritus, eczema, alopecia, decreased lung function, rhinitis, increased cough, hypertension, tachycardia, phlebitis, palpitations, postural hypertension, urinary tract infection, and dysuria.

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riluzole (ril´zōl´),

n brand name: Rilutek;
drug class: glutamate antagonist;
action: inhibits presynaptic release of glutamic acid in central nervous system;
use: treatment of amyotrophic lateral sclerosis (Lou Gehrig disease).

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riluzole

Rilutek

Pharmacologic class: Glutamate antagonist

Therapeutic class: Amyotrophic lateral sclerosis (ALS) agent

Pregnancy risk category C

Action

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

Availability

Tablets: 50 mg

⊘Indications and dosages

➣ ALS

Adults: 50 mg P.O. q 12 hours

Off-label uses

• Cervical dystonia
• Huntington's disease

Contraindications

• Hypersensitivity to drug or its components

Precautions

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.

Administration

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

Route	Onset	Peak	Duration
P.O.	Unknown	Unknown	Unknown

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

Interactions

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.

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riluzole

Rilutek® Neurology A drug with some benefit to Parkinson's disease and amyotrophic lateral sclerosis. See Amyotrophic lateral sclerosis, Parkinsonism.