Dosing and uses of Rilutek (riluzole)
Adult dosage forms and strengths
tablet
- 50mg
Amyotrophic Lateral Sclerosis (ALS)
50 mg PO q12hr on empty stomach
Monitor: LFTs
Huntington Disease (Orphan)
Orphan indication sponsor
- Rhone-Poulenc Rorer Pharmaceuticals, Inc; 500 Arcola Road, PO Box 5096; Collegeville, PA 19426-0800
Ataxia (Orphan)
Orphan designation for treatment of spinocelebellar ataxia
Sponsor
- Biohaven Pharmaceutical Holding Company, Ltd; 234 Church Street, Suite 304; New Haven, Connecticut 06511
Amyotrophic Lateral Sclerosis (Orphan)
Oral suspension (Teglutik [brand name]): Orphan desigation for amyotrophic lateral sclerosis (ALS)
Sponsor
- Italfarmaco SpA; 54 Via dei Lavoratori; Cinisello Balsamo, Italy
Pediatric dosage forms and strengths
Not recommended
Rilutek (riluzole) adverse (side) effects
>10%
Asthenia (16-20%)
Nausea (16-20%)
Skeletal weakness (19%)
Decreased lung function (11-15%)
1-10%
Headache (6-10%)
Abdominal pain (6-10%)
Diarrhea (6-10%)
Dizziness (6-10%)
Hypertension (6-10%)
Back pain (1-5%)
Vomiting (1-5%)
Anorexia (1-5%)
Somnolence (1-5%)
Vertigo (1-5%)
Circumoral paresthesia (1-5%)
Arthralgia (1-5%)
<1%
Interstitial lung disease and hypersensitivity pneumonitis
Angioedema
Bone necrosis
Edema
Erythema
Glaucoma
Hallucination
Warnings
Contraindications
Hypersensitivity to drug or any component of the formulation
Cautions
Caution in hepatic impairment; not recommended in patients with baseline elevations of serum aminotransferases greater than 5 times upper limit of normal; discontinue therapy if there is evidence of liver dysfunction
Case reports of clincial hepatitis reported
Interstitial lung disease reported (upon further investigation, many of these cases were hypersensitivity pneumonitis); discontinue immediately if dry cough or dyspnea develops
Neutropenia reported; advise patients to report any febrile illness
Caution in renal impairment
May cause drowsiness; use caution when performing hazardous tasks requiring alertness
Sedative effects may be potentiated when used concomitantly with other sedative drugs or ethanoL
Use with caution in the elderly and in females as clearance may be reduced
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown; avoid during breastfeeding
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Rilutek (riluzole)
Mechanism of action
Benzathiazole; inhibits glutamate release, inactivates voltage-dependent Na+ channels, inhibits effects of excitatory neurotransmitters
Pharmacokinetics
Half-Life: 12 hr
Bioavailability: 60%
Protein Bound: 96%
Metabolism: CYP1A2
Metabolites: 6 major metabolites, some active
Excretion: Feces (5%); urine (90%)
