Rilutek
riluzole
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.
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.
See 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.
riluzole
(ril-yoo-zole) riluzole,Rilutek
(trade name)Classification
Therapeutic: agents amyotrophic lateral sclerosisIndications
Action
- Inhibition of glutamate release,
- Inactivation of sodium channels or,
- Interference with neurotransmitter binding at receptor sites.
Therapeutic effects
Pharmacokinetics
Time/action profile
ROUTE | ONSET | PEAK | DURATION |
PO | unknown | unknown | unknown |
Contraindications/Precautions
Adverse Reactions/Side Effects
Central nervous system
- dizziness (most frequent)
- weakness (most frequent)
- headache
Respiratory
- decreased lung function (most frequent)
- hypersensitivity pneumonitis
- interstitial lung disease
Cardiovascular
- hypertension
- peripheral edema
Gastrointestinal
- hepatitis (life-threatening)
- abdominal pain (most frequent)
- nausea (most frequent)
- anorexia
- diarrhea
- dyspepsia
- flatulence
- ↑ liver enzymes
- vomiting
Hematologic
- neutropenia
Metabolic
- weight loss
Musculoskeletal
- arthralgia
- back pain
Neurologic
- circumoral paresthesia
Interactions
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.Route/Dosage
Availability (generic available)
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)
Implementation
- 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.