RILUZOLE

Table 2 displays the pharmacokinetic parameters of riluzole. Table 2. Pharmacokinetic Parameters of Riluzole

AbsorptionBioavailability (oral) Approximately 60% Dose Proportionality Linear over a dose range of 25 mg to 100 mg every 12 hours (1/2 to 2 times the recommended dosage) Food effect AUC ↓ 20% and C max ↓ 45% (high fat meal)

DistributionPlasma Protein Binding 96% (Mainly to albumin and lipoproteins)

EliminationElimination half-life 12 hours (CV=35%) The high interindividual variability...

The efficacy of riluzole was demonstrated in two studies (Study 1 and 2) that evaluated riluzole 50 mg twice daily in patients with amyotrophic lateral sclerosis (ALS). Both studies included patients with either familial or sporadic ALS, a disease duration of less than 5 years, and a baseline forced vital capacity greater than or equal to 60% of normal. Study 1 was a randomized, double-blind, placebo-controlled clinical study that enrolled 155 patients with ALS. Patients were randomized to receive riluzole 50 mg twice daily (n=77) or placebo (n=78) and were followed for at least 13 months (up ...

The following adverse reactions are described below and elsewhere in the labeling: Hepatic Injury [see Warnings and Precautions (5.1) ] Neutropenia [see Warnings and Precautions (5.2) ] Interstitial lung disease [see Warnings and Precautions (5.3) ] Most common adverse reactions (incidence greater than or equal to 5% and greater than placebo) were asthenia, nausea, dizziness, decreased lung function, and abdominal pain ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sun Pharmaceutical ...

Riluzole tablets are contraindicated in patients with a history of severe hypersensitivity reactions to riluzole or to any of its components (anaphylaxis has occurred) [see Adverse Reactions (6.1) ] . Patients with a history of severe hypersensitivity reactions to riluzole or to any of its components (4)

Hepatic injury: Use of riluzole is not recommended in patients with baseline elevations of serum aminotransferases greater than 5 times upper limit of normal; discontinue riluzole if there is evidence of liver dysfunction (5.1) Neutropenia: Advise patients to report any febrile illness (5.2) Interstitial lung disease: Discontinue riluzole if interstitial lung disease develops (5.3) 5.1 Hepatic Injury Cases of drug-induced liver injury, some of which were fatal, have been reported in patients tak...

7 DRUG INTERACTIONS Strong to moderate CYP1A2 inhibitors: Coadministration may increase riluzole-associated adverse reactions (7.1) Strong to moderate CYP1A2 inducers: Coadministration may result in decreased efficacy (7.2) Hepatotoxic drugs: Riluzole-treated patients that take other hepatotoxic drugs may be at increased risk for hepatotoxicity (7.3) 7.1 Agents that may Increase Riluzole Blood Con...