Medically reviewed by Drugs.com. Last updated on Aug 24, 2019.
(RIL yoo zole)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tiglutik: 50 mg/10 mL (300 mL) [contains saccharin sodium]
Rilutek: 50 mg
Generic: 50 mg
Brand Names: U.S.
- Glutamate Inhibitor
Mechanism of action is not known. Pharmacologic properties include inhibitory effect on glutamate release, inactivation of voltage-dependent sodium channels; and ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors
Suspension: High-fat meal decreases AUC by 9% and peak blood levels by 55%.
Tablets: High-fat meal decreases AUC by 20% and peak blood levels by 45%.
Vd: ~3.4 L/kg
Hepatic via CYP1A2 and UGT-HP4
Urine (90%; 2% as unchanged drug) and feces (5%)
Time to Peak
Suspension: 0.8 hours
Plasma: 96%, primarily to albumin and lipoproteins
Special Populations: Hepatic Function Impairment
AUC increased by about 1.7- and 3-fold in patients with mild and moderate chronic hepatic insufficiency, respectively. The pharmacokinetics have not been studied in patients with severe hepatic impairment.
Special Populations: Gender
Mean AUC was found to be 45% higher in women compared with men.
Special Populations: Race
Clearance was 50% lower in male Japanese patients than in white patients.
Special Populations Note
Smoking: Clearance was 20% greater in smokers compared to nonsmokers.
Use: Labeled Indications
Amyotrophic lateral sclerosis: Treatment of patients with amyotrophic lateral sclerosis (ALS); may extend survival and/or time to tracheostomy
Hypersensitivity to riluzole or any component of the formulation
Canadian labeling: Additional contraindications (not in US labeling): Hepatic disease or baseline serum transaminases >3 times ULN; pregnancy; breast-feeding
Amyotrophic lateral sclerosis (ALS): Oral: 50 mg twice daily.
Refer to adult dosing.
Dosing: Adjustment for Toxicity
Pulmonary toxicity: If interstitial lung disease develops, discontinue riluzole immediately.
Oral: Administer at the same time each day, at least 1 hour before or 2 hours after a meal. Gently shake suspension for ≥30 seconds prior to administration.
Store at 20°C to 25°C (68°F to 77°F). Protect from bright light. Use suspension within 15 days after opening bottle; discard unused suspension after 15 days.
CYP1A2 Inducers (Moderate): May decrease the serum concentration of Riluzole. Monitor therapy
Tobacco (Smoked): May decrease the serum concentration of Riluzole. Monitor therapy
Gastrointestinal: Nausea (16%)
Neuromuscular & skeletal: Weakness (19%)
1% to 10%:
Cardiovascular: Hypertension (5%), peripheral edema (3%), tachycardia (3%)
Central nervous system: Dizziness (4%), drowsiness (2%), vertigo (2%), malaise (1%)
Dermatologic: Pruritus (4%), eczema (2%), exfoliative dermatitis (1%)
Gastrointestinal: Abdominal pain (5%), vomiting (4%), flatulence (3%), oral paresthesia (2%), dental caries (1%), oral candidiasis (1%), stomatitis (1%)
Genitourinary: Urinary tract infection (3%), dysuria (1%)
Hepatic: Increased liver enzymes (>3 x ULN: 8%; >5 x ULN: 2%)
Neuromuscular & skeletal: Arthralgia (4%), tremor (1%)
Respiratory: Decreased lung function (10%), cough (3%)
<1%, postmarketing, and/or case reports (Limited to important or life-threatening): Amblyopia, anaphylactoid reaction, anaphylaxis, angioedema, aplastic anemia, arthropathy, asthma, ataxia, bradycardia, bundle branch block, cardiac failure, cataract, cerebral hemorrhage, deafness, dementia, diabetes mellitus, diabetes insipidus, drug-induced extrapyramidal reaction, edema, erythema multiforme, facial paralysis, gastrointestinal hemorrhage, gastrointestinal ulcer, glaucoma, hallucination, hematemesis, hematuria, hemoptysis, hepatitis, hypercalcemia, hypokalemia, hypokinesia, hyponatremia, hypotension, hypersensitivity pneumonitis, increased gamma-glutamyl transferase, increased lactate dehydrogenase, increased serum alkaline phosphatase, interstitial pulmonary disease, jaundice, leukocytosis, leukopenia, lymphadenopathy, mania, myoclonus, neutropenia, osteonecrosis, osteoporosis, pancreatitis, peripheral neuritis, pleural effusion, pseudomembranous colitis, purpura, respiratory acidosis, seizure, subarachnoid hemorrhage, thrombosis, urinary retention, urticaria, uterine hemorrhage, ventricular fibrillation, ventricular tachycardia
Concerns related to adverse effects:
• CNS depression: May cause dizziness or somnolence; caution should be used performing tasks which require alertness (operating machinery or driving).
• Hepatic effects: May cause drug-induced hepatic injury (including fatality); asymptomatic elevations of hepatic transaminases may also occur. Elevations of transaminases may occur within 3 months of use. Use is not recommended in patients who develop hepatic transaminases >5 times the upper limit of normal. Monitor for signs and symptoms of hepatic injury every month for the first 3 months and periodically thereafter; discontinue use if evidence of hepatic dysfunction occurs (eg, elevated bilirubin).
• Neutropenia: Severe neutropenia has been reported (ANC <500/mm3) within the first 2 months of therapy. Evaluate patients with febrile illnesses.
• Pulmonary disorders: Interstitial lung disease (ILD), including hypersensitivity pneumonitis, has occurred. Discontinue therapy immediately if ILD occurs.
• Hepatic impairment: Use with caution in patients with hepatic impairment.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Serum aminotransferases including ALT levels before and during therapy; signs and symptoms of hepatic injury every month for the first 3 months and periodically thereafter.
Adverse events have been observed in animal reproduction studies.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience nausea, loss of strength and energy, or abdominal pain. Have patient report immediately to prescriber signs of infection, signs of a severe pulmonary disorder (lung or breathing problems like difficulty breathing, shortness of breath, or a cough that is new or worse), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), severe dizziness, passing out, vision changes, or severe headache (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: miscellaneous central nervous system agents