riluzole

riluzole /ril·u·zole/ (ril´u-zol) 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 (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.