Trade Names:Rilutek- Tablets 50 mg
Unknown; however, the following properties may be related to effects: inhibits glutamate release; inactivates voltage-dependent sodium channels; interferes with intra-cellular events following transmitter binding at excitatory amino acid receptors. These effects may protect neural tissues against degenerative changes.
Well absorbed (about 90%). Oral bioavailability is about 50%. High fat meals decrease absorption, decrease AUC about 20% and peak blood levels by about 45%. Steady state is less than 5 days.
Protein binding is 96%, mainly to albumin and lipoproteins. Penetrates brain readily.
Extensively metabolized to 6 major and a number of minor metabolites via CYP-450 dependent hydroxylation and glucuronidation. CYP-450 1A2 is the main isoenzyme involved in N-hydroxylation.
Eliminated in urine (more than 85% glucuronide metabolites; 2% unchanged) and small amount in feces. T ½ is 12 h (after multiple dosing).
Reduced clearance of riluzole and its metabolites leading to higher plasma levels.Hepatic Function Impairment
Reduced clearance of riluzole and its metabolites, leading to higher plasma levels.Elderly
Age-related decreased renal function will give higher plasma levels of riluzole and metabolites.Gender
CYP1A2 activity has been reported to be lower in women and may result in higher blood concentrations and metabolites.Race
Clearance of drug in Japanese subjects was found to be 50% lower; may possess a lower capacity (oxidative or conjugative) for metabolizing riluzole.Smoking
Induces CYP1A2 and will eliminate riluzole faster; no information on need to adjust dose in these patients.
Treatment of patients with amyotrophic lateral sclerosis (ALS; Lou Gehrig disease).
PO 50 mg every 12 h.
May reduce riluzole elimination.Cigarette smoke, rifampin, omeprazole
May enhance riluzole elimination.
None well documented.
Hypertension; tachycardia; palpitations; peripheral edema.
Headache; hypertonia; depression; dizziness; insomnia; somnolence; vertigo; circumoral paresthesia; aggravation reaction; agitation; tremor.
Pruritus; eczema; alopecia; exfoliative dermatitis.
Nausea; vomiting; dyspepsia; anorexia; diarrhea; constipation; flatulence; abdominal pain; stomatitis; dry mouth; oral moniliasis.
Urinary tract infection; dysuria.
Decreased lung function; cough.
Asthenia; arthralgia; back pain; malaise.
Measure serum aminotransferases before and during therapy. Evaluate serum SGPT levels every month during the first 3 mo of treatment, every 3 mo during the remainder of the first yr and periodically thereafter.
Category C .
Safety and efficacy not established.
Age-related compromised renal and hepatic function may cause a decrease in clearance of riluzole.
Use with caution in patients with renal impairment.
Use with caution in patients with current evidence or history of abnormal liver function indicated by significant elevations of liver enzymes. Baseline elevations of several LFTs (especially elevated bilirubin) should preclude use of riluzole.
Females and Japanese patients may possess a lower metabolic capacity to eliminate riluzole as compared to males and Caucasian subjects, respectively.
Copyright © 2009 Wolters Kluwer Health.